HDAC
信号通路图
研究领域
抑制剂选择性比较
特异性亚型抑制剂
HDAC产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1047 |
Vorinostat (SAHA)Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。 |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
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| S1053 |
Entinostat (MS-275)Entinostat (MS-275)强烈抑制HDAC1和HDAC3，无细胞试验中IC50分别为0.51 μM和1.7 μM，抑制作用强于HDACs 4， 6， 8，和10。Phase 3。 |
(A) U87 cells were cultured in the presence of DMSO, 1 uM MS-275 alone, 100 ng/ml IFN-λ1 alone, or both for the course of 4 d. Cell numbers were manually determined by hemacytometer counting at the indicated time points. (B, F) Cell proliferation of U87 cells or U87 spheroids in 3D culture with indicated treatment were performed using the WST-1 assay, which measures active cellular metabolism. (C) U87 spheroid formation in 3D culture was photographed at day 14 in culture (representative images are shown; 200x magnification). (D-E) Quantification of the relative sizes and numbers of U87 spheroids in (C). (G) Cell cycle analysis was performed in U87 cells with indicated treatment using propidium iodide staining. Numbers in the histogram show fractions (percent) of sub-G1, N, 2N, and polyploidy from left to right. (H) U87 cells with indicated treatment were stained with Annexin V-FITC and 7-AAD. Numbers indicate the percentage of FITC-positive cells (upper left quadrant). FITC, fluorescein isothiocyanate; 7-AAD, 7-Aminoactinomycin. In all panels, data represent the mean and SEM of at least three experiments.
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| S1030 |
Panobinostat (LBH589)Panobinostat (LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Phase 3。 |
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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| S1045 |
Trichostatin A (TSA)Trichostatin A (TSA)是一种HDAC抑制剂，无细胞试验中IC50为1.8 nM左右。 |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h, and their expression of GRP78, PERK-eIF2α axis and ATF4, ATF3, CHOP and DR5 proteins. |
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| S1122 |
Mocetinostat (MGCD0103)Mocetinostat (MGCD0103)是一种有效的HDAC抑制剂，对HDAC1抑制作用最强，无细胞试验中IC50为0.15 μM，比作用于HDAC2， 3，和11选择性高2到10倍，对HDAC4， 5， 6， 7，和8没有抑制活性。Phase 2。 |
Comparison of MCAS ovarian cancer cells harboring control and CtBP2 knockdown shRNAs for sensitivity to chemotherapeutic agents. For each cell line, the MTT reading of the untreated cells was assigned as 100%. HDAC inhibitors: (a) Trichostatin A; (b) Vorinostat; (c) Belinostat; (d) MGCD0103; (e) valproic acid; and (f ) carboplatin, a non-HDAC inhibitor. |
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| S6687New |
SIS17SIS17是一种哺乳动物histone deacetylase 11 (HDAC 11)的特异性抑制剂，IC50值为0.83 μM。 SIS17抑制HDAC11底物丝氨酸羟甲基转移酶2的去甲酰化，而不抑制其他HDAC。 |
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| S6548New |
NKL 22NKL 22是一种选择性的HDAC抑制剂，IC50为78 µM。 |
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| S1073New |
BML-210 (CAY10433)BML-210是HDAC的小分子抑制剂。BML-210以剂量依赖的方式抑制HDAC4-VP16驱动的报告基因信号，IC50为∼5 µM。 |
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| S6738New |
TC-H 106TC-H 106是一种慢速、紧密结合的I类histone deacetylases(HDAC)抑制剂，对HDAC1, HDAC2, HDAC3的Ki值分别为148 nM, 约102 nM, 14 nM。 |
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| S2132New |
SR-4370SR-4370是一种有效、选择性的I类HDACs抑制剂，对HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6 的IC50分别为0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM。SR-4370抑制AR信号传导和体内前列腺肿瘤的生长。 |
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| S8743New |
SKLB-23bbSKLB-23bb是一种具有口服生物利用度的选择性HDAC6抑制剂，在所检测的多数细胞系中IC50小于100 nM。它还具有破坏微管的活性。 |
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| S8769New |
Tinostamustine(EDO-S101)Tinostamustine (EDO-S101)是首批烷基化脱乙酰酶抑制剂，对I类HDACs如HDAC1, HDAC2, HDAC3和HDAC8的IC50值分别为9 nM, 9 nM, 25 nM和107 nM；而对II类HDACs如HDAC6和HDAC10的IC50值分别为6 nM和72 nM。 |
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| S1085 |
Belinostat (PXD101)Belinostat (PXD101)是一种新型HDAC抑制剂，无细胞试验中IC50为27 nM，对耐Cisplatin的肿瘤具有活性。 |
Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h. |
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| S3020 |
Romidepsin (FK228, Depsipeptide)Romidepsin (FK228, Depsipeptide)是一种有效的HDAC1和HDAC2抑制剂，无细胞试验中IC50分别为36 nM和47 nM。 |
Effects of combination of bort/romidepsin on HDAC6 inhibition and activation of ER stress signaling. HA cells were treated with combination of 15 nM bortezomib and 5 nM romidepsin or either drug alone for 24 hr. Expression of CHOP/GADD153 (green signals) and cleaved PARP (red signals) was detected by immunofluorescent staining. DAPI (blue signals) stained the cell nuclei. |
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| S1484 |
MC1568MC1568是一种选择性的HDAC抑制剂，作用于玉米HD1-A，无细胞试验中IC50为100 nM，作用于HD1-A比作用于HD1-B选择性高34倍。 |
HDAC4 and OA1 expression correlate inversely during starvation, and HDAC4 inhibition or knockdown leads to OA1 transgene up-regulation. Quantification of OA1 mRNA expression by real-time PCR in HeLa-OA1myc cells at the indicated times of incubation with MC1568 (class II HDACi). Data are expressed as the fold change compared with the amount of the OA1 mRNA in mock conditions at each time point. |
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| S2627 |
Tubastatin A HClTubastatin A HCl是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM。选择性作用于所有其他同工酶（1000倍以上），除了HDAC8(57倍以上)。 |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S2170 |
Givinostat (ITF2357)Givinostat (ITF2357)是一种有效的HDAC抑制剂，作用于玉米HD2， HD1B和HD1A，无细胞试验中IC50分别为10 nM， 7.5 nM和16 nM。Phase 2。 |
Cells were treated with indicated HDAC inhibitors for 4 days and then cultured without drug for an additional 4 days. On day 8, HDAC inhibitors were added back to the culture for another 4 days. The percentage of GFP-positive cells was measured at days 4, 8 and 12. The concentrations of HDAC inhibitors used for the experiments are as follows: vorinostat, 1 uM; TsA, 200 nM; oxamflatin, 1 uM; scriptaid, 1 uM; belinostat, 200 nM; and givinostat, 200 nM. The fraction of GFP-positive cells was measured by flow cytometry at the indicated timepoints. The effect of HDAC inhibitors or anti-CD3 plus anti-CD28 antibodies over time was normalized to the effect of anti-CD3 plus anti-CD28 antibodies at day 2. Error bars represent SEM, n = 3. APHA, 3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxypropenamide.
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| S1095 |
Dacinostat (LAQ824)Dacinostat (LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。 |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S1194 |
CUDC-101CUDC-101是一种有效的，多靶点抑制剂，作用于HDAC，EGFR和HER2，IC50分别为4.4 nM， 2.4 nM，和15.7 nM，且抑制I/II型HDACs，但是对III型， Sir-type HDACs没有抑制作用。Phase 1。 |
(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). *, P < 0.05; **, P < 0.01.
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| S1096 |
Quisinostat (JNJ-26481585) 2HClQuisinostat (JNJ-26481585) 2HCl是一种新型的，第二代HDAC抑制剂，对HDAC1最有效，无细胞试验中IC50为0.11 nM，作用于HDACs 2，4，10，和11适度有效；比作用于HDACs 3，5，8，和9选择性强30倍，对HDACs 6和7作用效果最弱。Phase 2。 |
WT ESCs were treated with varying concentrations of the HDAC1 specific inhibitor JNJ-26481585 for 24 h. Lysates were collected for ChIP experiments, and a H3K27ac antibody was used for immunoprecipitation (IP). qPCR was performed using primers specific for Hoxa1 RARE2. ChIP with an IgG antibody (negative control) is included in each panel. Error bars represent standard error of independent experiments where n = 3 for biological repeats. *, p < 0.05.
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| S1515 |
Pracinostat (SB939)Pracinostat (SB939)是一种有效的pan-HDAC抑制剂，IC50为40-140 nM，除了HDAC6例外，对III型同工酶SIRT I没有抑制活性。Phase 2。 |
Hyperacetylation of P. falciparum proteins by SB939. Synchronous 3D7 trophozoite-stage P. falciparum parasites were treated with 50 or 500 nM chloroquine (CQ), SAHA, or SB939 or with vehicle only (control; 0.05% DMSO) for 3 h. Following saponin lysis, parasite protein lysates were prepared and SDS-PAGE and Western blotting carried out using anti-acetyl H4 or anti-pan-acetyl lysine (K103) antibodies. Coomassie blue staining was carried out as a loading control.
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| S2012 |
PCI-34051PCI-34051是一种有效的，特异性的HDAC8抑制剂，无细胞试验中IC50为10 nM。比作用于HDAC1和6选择性高200多倍，比作用于HDAC2， 3，和10选择性高1000倍。 |
(d) Effects of HDAC8 activity on ISO-induced augmentation of apoptosis and TIPRL expression. H1299 cells were sequentially treated with 10 μm PCI-34051 for 24 h, ISO for 30 min and 50 μM cisplatin for 48 h before the western blot analysis.
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| S1422 |
DroxinostatDroxinostat是一种选择性的HDAC抑制剂，最有效作用于HDACs 6和8，IC50为2.47μM和1.46 μM，比作用于HDAC3选择性高8倍，对HDAC1， 2， 4， 5， 7， 9，和10没有抑制作用。 |
Chemical inhibition of HDAC3, -6, and -8 with the selective HDAC inhibitor Droxinostat (2 uM) resulted in a significant increase in the percent of 2D10 cells expressing GFP in cells that had been depleted of HDAC3 but not HDAC1 or -2. (*p<0.05).
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| S1090 |
Abexinostat (PCI-24781)Abexinostat (PCI-24781)是一种新型的pan-HDAC抑制剂，靶向作用于HDAC1，Ki为7 nM，对HDACs 2， 3， 6，和10有适中的抑制性，但比作用于HDAC8选择性强40倍。Phase 1/2。 |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S7229 |
RGFP966RGFP966是一种HDAC3抑制剂，无细胞试验中IC50为0.08μM ，比作用于其他HDAC选择性高200倍以上。 |
THP-1 cells were treated with indicated concentrations of Ara-C and/or RGFP966 for 24 h, and lysates were immunoblotted for p-AKT473, AKT and γH2AX.
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| S2244 |
AR-42AR-42是一种HDAC抑制剂，IC50为30 nM。Phase 1。 |
One- to 2-month-old mice of both genotypes showed an increase in H3K4me3 (n = 5 to 6 per group) associated with a dose-dependent increase in neurogenesis in Kmt2d+/βGeo mice (monitored by normalized DCX expression) (n = 4 to 6 per group) upon treatment with the HDACi AR-42. There was no difference in either H3K4me3 or neurogenesis between Kmt2d+/βGeo and Kmt2d+/+ animals at a dose of 10 mg/kg per day.
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| S8001 |
Ricolinostat (ACY-1215)Ricolinostat (ACY-1215)是一种选择性HDAC6抑制剂，无细胞试验中IC50为5 nM，作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上，对HDAC8具有微弱的作用活性，对HDAC4/5/7/9/11， Sirtuin1和Sirtuin2具有最小的作用活性。Phase 2。 |
(a) Representative images from hTERT RPE-1 cells transiently transfected with siControl (siC), treated with vehicle (DMSO), alisertib (MLN8237) or rocilinostat (ACY1215) at the time of serum withdrawal for 48 h. Ciliation monitored by immunofluorescent staining using acetylated α-tubulin (cilia marker) and pericentrin (basal body marker). Nuclei counterstained using DAPI. Highlighted boxes show magnified cilia. Scale bar, 3 μM. |
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| S1168 |
Valproic acid sodium salt (Sodium valproate)Valproic acid sodium salt (Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。 |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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| S2818 |
Tacedinaline (CI994)Tacedinaline (CI994)是一种选择性的I型HDAC抑制剂，其对HDAC 1, 2, 3,和8的IC50分别为0.9, 0.9, 1.2, 和 >20 μM。Phase 3。 |
A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and -actin.
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| S2759 |
Fimepinostat（CUDC-907）CUDC-907是一种PI3K和HDAC双重抑制剂，作用于PI3Kα和HDAC1/2/3/10，IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。Phase 1。 |
Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
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| S1999 |
Sodium butyrateSodium butyrate, 是butyrate的钠盐形式。是histone deacetylase(HDAC)抑制剂，与I类和II类HDACs的锌区竞争性结合。 |
U87 cells were cultured with DMSO or 10 µM 5azadC for 72 h. For the latter, 1 µM Trichostatin A (TSA), 10 mM sodium butyrate (NaBu), 5 mM nicotinamide (NAM), or 0.5 µM apicidin were added in the last 24 h. IFNLR1 expression was determined by RT-qPCR. |
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| S1848 |
CurcuminCurcumin 是流行的印度香料姜黄的主要姜黄色素，属于姜科（Zingiberaceae）。它是p300 histone acetylatransferase（IC50~25 μM）和Histone deacetylase的抑制剂，能够激活Nrf2 pathway并抑制NF-κB的激活。 |
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| S2779 |
M344M344是一种有效的HDAC抑制剂，IC50为100 nM，可以诱导细胞分化。 |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h. ATF4, ATF3, CHOP and DR5 proteins were measured by Western blot. |
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| S2239 |
TubacinTubacin是一种高度有效的选择性的，可逆的，细胞渗透性HDAC6抑制剂，无细胞试验中IC50为4 nM，比作用于HDAC1的选择性高350倍。 |
Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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| S7292 |
RG2833 (RGFP109)RG2833 (RGFP109)是一种大脑渗透性HDAC抑制剂，作用于HDAC1和HDAC3，无细胞试验中IC50分别为60 nM和50 nM。 |
The cells were treated with 1 μM RG2833 (HDAC1/3 inhibitor), 2 μM RGFP966 (HDAC3 inhibitor), 1 μM TSA (pan-HDAC inhibitor), or vehicle for 16 h in serum-free medium. Cell lysates were analysed by Western blotting for expression of SREBP-2 activated fragment, HMG-CoA reductase and APP. Shown are representative blots and quantifications with means ± SEM of the indicated number of independent experiments performed in duplicate. *p < 0.05; **p < 0.01; n.s., not significant in one-sample t-test.
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| S2693 |
ResminostatResminostat剂量依赖性的选择性的抑制HDAC1/3/6， IC50为42.5 nM/50.1 nM/71.8 nM，作用于HDAC8效果弱，IC50为877 nM。 |
Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
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| S1703 |
Divalproex SodiumDivalproex Sodium是由肠溶包衣中丙戊酸钠和丙戊酸按1:1摩尔组成的化合物，是一种HDAC抑制剂，用于治疗癫痫。 |
Divalproex sodium increases the level of acetylated histone H3 level in ataxin-3-transfected HEK293 cells. Normal (15CAG) or expanded (77CAG) ataxin-3-transfected cells were treated with divalproex sodium (Selleck chemical, 0.3 mmol/L in DMSO, (+)) or with DMSO alone (−) 48 h after transfection. The cells were treated with divalproex sodium or DMSO over 6, 12, and 24 h. The Western blot was probed with antiacetylated histone H3, antihistone H3, and antiataxin-3. Antibodies include antihistone H3 and antiataxin-3 are used as controls. The x-axis shows the different treatment group. The y-axis represents the acetylated histone H3 values normalized to histone H3. Error bars represent the standard error of the mean. Data represent three independent experiments (n = 3). The data with a normal distribution were analyzed with Student’s t-test. *P < 0.05
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| S8043 |
ScriptaidScriptaid 是一种HDAC抑制剂，作用于乙酰化H4比作用于H3效果高很多。 |
The relative expression of Oct4, Nanog, Klf4 and Sox2 at the blastocyst stage in ICSI-, ROSI- and ROSI + incubation of zygotes with 250 nM Scriptaid for 10 h (ROSI-S)-derived embryos. Five blastocysts in each pool were examined to obtain the data set in each column. Q-PCR analysis was performed in triplicate. Different letters indicate significant differences between values (P < 0.05).
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| S4125 |
Sodium PhenylbutyrateSodium Phenylbutyrate是一种转录调节因子，通过调控HDAC活性来改变染色质结构从而发挥作用。 |
Representative images and quantitative analysis results of the transwell experiment. Notes: (A) Results of migration assay for DU145. (B) Results of invasion assay for DU145. (C) Results of migration assay for PC3. (D) Results of invasion assay for PC3. “*” Means significantly different from control group, P<0.05. Abbreviation: SPB, sodium phenylbutyrate.
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| S8049 |
Tubastatin ATubastatin A是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM，选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。 |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S7324 |
TMP269TMP269 是强效的选择性的IIa类HDAC抑制剂，其作用于HDAC4, HDAC5, HDAC7 和 HDAC9的IC50分别为126 nM, 80 nM, 36 nM 和 19 nM。 |
Staining of live (calcein-AM, green) and dead (PI, red) UCC cells after 72 h of treatment with TMP269. Data shown are a representative experiment of a set of 3
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| S7595 |
Santacruzamate A (CAY10683)Santacruzamate A（CAY10683）是一种强效的选择性HDAC抑制剂，其对HDAC2的IC50为119 pM ，比对其他HDACs高出 >3600倍的选择性。 |
Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
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| S8502 |
TMP195TMP195是一种选择性的class IIa HDAC抑制剂，在基于细胞的实验中，IC50为300 nM。 |
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| S3944 |
Valproic acidValproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers. |
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| S5810 |
UF010UF010是I类HDAC选择性抑制剂，对HDAC1、HDAC2、HDAC3、HDAC8、HDAC6和HDAC10的IC50值分别为0.5 nM、0.1 nM、0.06 nM、1.5 nM、9.1 nM和15.3 nM。 |
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| S7617 |
TasquinimodTasquinimod是一种口服有效的antiangiogenic药剂，通过变构抑制HDAC4信号发挥作用。Phase 3。 |
Western blot images suggested inhibition of HDAC4 increased the expression of NOX4 and MMP-9, and treatment with 10 μM SCM-198 reduced the raised levels of NOX4 and MMP-9. |
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| S9275 |
IsoguanosineIsoguanosine 抑制 FLT3 和 HDAC3/6 治疗AML。Isoguanosine 是巴豆（Croton tiglium）种子中天然存在的鸟苷的活性异构体。 |
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| S7726 |
BRD73954BRD73954是一种有效的选择性 HDAC 抑制剂，对HDAC6 和 HDAC8的 IC50 分别为 36 nM 和 120 nM。 |
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| S8464 |
Citarinostat (ACY-241)Citarinostat (ACY-241)是一种具有口服活性的、选择性HDAC6抑制剂，对HDAC6和HDAC3的IC50分别为2.6 nM和46 nM。对HDAC6的选择性是对HDAC1-3的选择性的13-18倍。 |
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| S5905 |
Suberohydroxamic acidSuberohydroxamic acid是竞争性HDAC抑制剂，对HDAC1和HDAC3的IC50分别为0.25 μM和0.3 μM。 |
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| S7593 |
SplitomicinSplitomicin是一种选择性的NAD(+)-dependent histone deacetylase Sir2p抑制剂，IC50为60 μM。在细胞中有着更高的活性。 |
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| S7278 |
HPOBHPOB是一种有效的，选择性 HDAC6抑制剂，IC50为56 nM，选择性比对其它HDACs高30多倍。 |
Effects of HPOB on GCs-induced apoptosis in PC12 and SH-SY5Y cells. (A) Effect of 48 h treatment with HPOB alone and (B) anti-apoptotic effect of HPOB pre-treatment for 24 h on Cort-induced apoptosis in PC12 cells. The results are expressed as the means ± SD of three independent experiments. ## indicates a significant difference from the control (P < 0.01). * indicates a significant difference from treatment with Cort alone at P < 0.05. ** indicates a significant difference from treatment with Cort alone at P < 0.01.
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| S7569 |
LMK-235LMK-235是HDAC4和HDAC5的选择性抑制剂， IC50分别为11.9 nM 和 4.2 nM。 |
Upper panel: qPCR analysis of CDX2-negative HT29 cells treated with increasing concentrations of the DNMTi decitabine (1.25 μM, 2.5 μM, 5 μM, 10 μM) for 48 h and increasing concentrations of the HDAC4/5i LMK-235 (5 nM, 10 nM, 20 nM, 40 nM, 80 nM). Data were normalized to the HMBS housekeeping gene and are shown as n-fold regulation compared with DMSO-treated cells. MWU: ***p < 0.001, (n = 4). Lower panel: CDX2 Western blot analysis of the three highest concentrations for both compounds of HT29 cells treated as above. Total protein is shown as a loading control. Percentage indicates amount of protein normalized to respective DMSO controls
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| S5438 |
Biphenyl-4-sulfonyl chlorideBiphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. |
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| S7473 |
Nexturastat ANexturastat A 是一种强效的选择性的HDAC抑制剂，IC50为5 nM,其选择性高于其他的HDACs190倍。 |
HDAC inhibitors disrupt SS18-SSX/TLE1 co-localization. A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells. |
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| S8773 |
TH34TH34是HDAC抑制剂，对HDAC6、HDAC8和HDAC10的选择性比HDAC1、HDAC2和HDAC3高。在 NanoBRET实验中，TH34与HDAC6/8/10紧密结合，IC50分别为4.6 μM、1.9 μM和7.7 μM。 |
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| S8567 |
Tucidinostat (Chidamide)Chidamide是HDAC1, 2, 3, 10的低摩尔浓度抑制剂，IC50分别为95、160、67、78 nM。 |
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| S2341 |
(-)-Parthenolide(-)-Parthenolide, Nuclear Factor-κB抑制剂，可特异性地耗尽HDAC1蛋白，而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。 |
-Parthenolide-S234101W0220161110.gif)
-Parthenolide-S234101W0220161110.gif)
G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells |
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| S8495 |
WT161WT161是有效的、选择性的HDAC6抑制剂，对HDAC6、HDAC1和HDAC2的IC50值分别为0.4 nM、8.35 nM和15.4 nM，比对其他HDACs的选择性高100倍以上。 |
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| S7596 |
CAY10603CAY10603是一种强效的选择性HDAC6抑制剂，IC50为2 pM，选择性比其它HDACs高200多倍。 |
U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
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| S8648 |
ACY-738ACY-738以低纳摩尔浓度抑制HDAC6，IC50为1.7 nM。其对HDAC6的选择性比对其他I类HDACs高60-1500倍。 |
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| S9262 |
Raddeanin ARaddeanin A, a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity. |
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| S7555 |
Domatinostat (4SC-202)4SC-202是一种选择性的I类HDAC抑制剂，对HDAC1，HDAC2，和HDAC3的IC50分别为1.20 μM，1.12 μM，和0.57 μM。也对Lysine specific demethylase 1 (LSD1)表现出抑制活性。Phase 1。 |
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| S7689 |
BG45BG45 是I类 HDAC 抑制剂，无细胞试验中对 HDAC3，HDAC1，HDAC2，和 HDAC6的 IC50 分别为 289 nM，2.0 µM，2.2 µM 和 >20 µM。 |
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| S8323 |
ITSA-1 (ITSA1)ITSA-1 (ITSA1)通过抑制TSA（曲古菌素A），激活HDAC。但对其他HDAC抑制剂没有活性。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1047 |
Vorinostat (SAHA)Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。 |
Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype). |
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| S1053 |
Entinostat (MS-275)Entinostat (MS-275)强烈抑制HDAC1和HDAC3，无细胞试验中IC50分别为0.51 μM和1.7 μM，抑制作用强于HDACs 4， 6， 8，和10。Phase 3。 |
(A) U87 cells were cultured in the presence of DMSO, 1 uM MS-275 alone, 100 ng/ml IFN-λ1 alone, or both for the course of 4 d. Cell numbers were manually determined by hemacytometer counting at the indicated time points. (B, F) Cell proliferation of U87 cells or U87 spheroids in 3D culture with indicated treatment were performed using the WST-1 assay, which measures active cellular metabolism. (C) U87 spheroid formation in 3D culture was photographed at day 14 in culture (representative images are shown; 200x magnification). (D-E) Quantification of the relative sizes and numbers of U87 spheroids in (C). (G) Cell cycle analysis was performed in U87 cells with indicated treatment using propidium iodide staining. Numbers in the histogram show fractions (percent) of sub-G1, N, 2N, and polyploidy from left to right. (H) U87 cells with indicated treatment were stained with Annexin V-FITC and 7-AAD. Numbers indicate the percentage of FITC-positive cells (upper left quadrant). FITC, fluorescein isothiocyanate; 7-AAD, 7-Aminoactinomycin. In all panels, data represent the mean and SEM of at least three experiments.
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| S1030 |
Panobinostat (LBH589)Panobinostat (LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Phase 3。 |
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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| S1045 |
Trichostatin A (TSA)Trichostatin A (TSA)是一种HDAC抑制剂，无细胞试验中IC50为1.8 nM左右。 |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h, and their expression of GRP78, PERK-eIF2α axis and ATF4, ATF3, CHOP and DR5 proteins. |
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| S1122 |
Mocetinostat (MGCD0103)Mocetinostat (MGCD0103)是一种有效的HDAC抑制剂，对HDAC1抑制作用最强，无细胞试验中IC50为0.15 μM，比作用于HDAC2， 3，和11选择性高2到10倍，对HDAC4， 5， 6， 7，和8没有抑制活性。Phase 2。 |
Comparison of MCAS ovarian cancer cells harboring control and CtBP2 knockdown shRNAs for sensitivity to chemotherapeutic agents. For each cell line, the MTT reading of the untreated cells was assigned as 100%. HDAC inhibitors: (a) Trichostatin A; (b) Vorinostat; (c) Belinostat; (d) MGCD0103; (e) valproic acid; and (f ) carboplatin, a non-HDAC inhibitor. |
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| S6687New |
SIS17SIS17是一种哺乳动物histone deacetylase 11 (HDAC 11)的特异性抑制剂，IC50值为0.83 μM。 SIS17抑制HDAC11底物丝氨酸羟甲基转移酶2的去甲酰化，而不抑制其他HDAC。 |
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| S6548New |
NKL 22NKL 22是一种选择性的HDAC抑制剂，IC50为78 µM。 |
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| S1073New |
BML-210 (CAY10433)BML-210是HDAC的小分子抑制剂。BML-210以剂量依赖的方式抑制HDAC4-VP16驱动的报告基因信号，IC50为∼5 µM。 |
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| S6738New |
TC-H 106TC-H 106是一种慢速、紧密结合的I类histone deacetylases(HDAC)抑制剂，对HDAC1, HDAC2, HDAC3的Ki值分别为148 nM, 约102 nM, 14 nM。 |
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| S2132New |
SR-4370SR-4370是一种有效、选择性的I类HDACs抑制剂，对HDAC 1, HDAC 2, HDAC 3, HDAC 8, HDAC 6 的IC50分别为0.13 µM, 0.58 µM, 0.006 µM, 2.3 µM, 3.7 µM。SR-4370抑制AR信号传导和体内前列腺肿瘤的生长。 |
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| S8743New |
SKLB-23bbSKLB-23bb是一种具有口服生物利用度的选择性HDAC6抑制剂，在所检测的多数细胞系中IC50小于100 nM。它还具有破坏微管的活性。 |
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| S8769New |
Tinostamustine(EDO-S101)Tinostamustine (EDO-S101)是首批烷基化脱乙酰酶抑制剂，对I类HDACs如HDAC1, HDAC2, HDAC3和HDAC8的IC50值分别为9 nM, 9 nM, 25 nM和107 nM；而对II类HDACs如HDAC6和HDAC10的IC50值分别为6 nM和72 nM。 |
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| S1085 |
Belinostat (PXD101)Belinostat (PXD101)是一种新型HDAC抑制剂，无细胞试验中IC50为27 nM，对耐Cisplatin的肿瘤具有活性。 |
Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h. |
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| S3020 |
Romidepsin (FK228, Depsipeptide)Romidepsin (FK228, Depsipeptide)是一种有效的HDAC1和HDAC2抑制剂，无细胞试验中IC50分别为36 nM和47 nM。 |
Effects of combination of bort/romidepsin on HDAC6 inhibition and activation of ER stress signaling. HA cells were treated with combination of 15 nM bortezomib and 5 nM romidepsin or either drug alone for 24 hr. Expression of CHOP/GADD153 (green signals) and cleaved PARP (red signals) was detected by immunofluorescent staining. DAPI (blue signals) stained the cell nuclei. |
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| S1484 |
MC1568MC1568是一种选择性的HDAC抑制剂，作用于玉米HD1-A，无细胞试验中IC50为100 nM，作用于HD1-A比作用于HD1-B选择性高34倍。 |
HDAC4 and OA1 expression correlate inversely during starvation, and HDAC4 inhibition or knockdown leads to OA1 transgene up-regulation. Quantification of OA1 mRNA expression by real-time PCR in HeLa-OA1myc cells at the indicated times of incubation with MC1568 (class II HDACi). Data are expressed as the fold change compared with the amount of the OA1 mRNA in mock conditions at each time point. |
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| S2627 |
Tubastatin A HClTubastatin A HCl是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM。选择性作用于所有其他同工酶（1000倍以上），除了HDAC8(57倍以上)。 |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S2170 |
Givinostat (ITF2357)Givinostat (ITF2357)是一种有效的HDAC抑制剂，作用于玉米HD2， HD1B和HD1A，无细胞试验中IC50分别为10 nM， 7.5 nM和16 nM。Phase 2。 |
Cells were treated with indicated HDAC inhibitors for 4 days and then cultured without drug for an additional 4 days. On day 8, HDAC inhibitors were added back to the culture for another 4 days. The percentage of GFP-positive cells was measured at days 4, 8 and 12. The concentrations of HDAC inhibitors used for the experiments are as follows: vorinostat, 1 uM; TsA, 200 nM; oxamflatin, 1 uM; scriptaid, 1 uM; belinostat, 200 nM; and givinostat, 200 nM. The fraction of GFP-positive cells was measured by flow cytometry at the indicated timepoints. The effect of HDAC inhibitors or anti-CD3 plus anti-CD28 antibodies over time was normalized to the effect of anti-CD3 plus anti-CD28 antibodies at day 2. Error bars represent SEM, n = 3. APHA, 3-(1-methyl-4-phenylacetyl-1H-2-pyrrolyl)-N-hydroxypropenamide.
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| S1095 |
Dacinostat (LAQ824)Dacinostat (LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。 |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S1194 |
CUDC-101CUDC-101是一种有效的，多靶点抑制剂，作用于HDAC，EGFR和HER2，IC50分别为4.4 nM， 2.4 nM，和15.7 nM，且抑制I/II型HDACs，但是对III型， Sir-type HDACs没有抑制作用。Phase 1。 |
(a) Decay-corrected microPET/CT scan of MDA-MB-231 tumor bearing mice (n = 4) at 2, 4, and 24 h after i.v. injection of [64Cu]7. The image obtained with coinjection of CUDC-101 (20 mg/kg body weight) is shown for a 24 h blockade. Tumors are indicated by arrows. (b) Decay-corrected region-of interest (ROI) analysis on microPET images of the tumor uptake of [64Cu]7 with or without coinjection of CUDC-101 (20 mg/kg body weight). *, P < 0.05; **, P < 0.01.
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| S1096 |
Quisinostat (JNJ-26481585) 2HClQuisinostat (JNJ-26481585) 2HCl是一种新型的，第二代HDAC抑制剂，对HDAC1最有效，无细胞试验中IC50为0.11 nM，作用于HDACs 2，4，10，和11适度有效；比作用于HDACs 3，5，8，和9选择性强30倍，对HDACs 6和7作用效果最弱。Phase 2。 |
WT ESCs were treated with varying concentrations of the HDAC1 specific inhibitor JNJ-26481585 for 24 h. Lysates were collected for ChIP experiments, and a H3K27ac antibody was used for immunoprecipitation (IP). qPCR was performed using primers specific for Hoxa1 RARE2. ChIP with an IgG antibody (negative control) is included in each panel. Error bars represent standard error of independent experiments where n = 3 for biological repeats. *, p < 0.05.
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| S1515 |
Pracinostat (SB939)Pracinostat (SB939)是一种有效的pan-HDAC抑制剂，IC50为40-140 nM，除了HDAC6例外，对III型同工酶SIRT I没有抑制活性。Phase 2。 |
Hyperacetylation of P. falciparum proteins by SB939. Synchronous 3D7 trophozoite-stage P. falciparum parasites were treated with 50 or 500 nM chloroquine (CQ), SAHA, or SB939 or with vehicle only (control; 0.05% DMSO) for 3 h. Following saponin lysis, parasite protein lysates were prepared and SDS-PAGE and Western blotting carried out using anti-acetyl H4 or anti-pan-acetyl lysine (K103) antibodies. Coomassie blue staining was carried out as a loading control.
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| S2012 |
PCI-34051PCI-34051是一种有效的，特异性的HDAC8抑制剂，无细胞试验中IC50为10 nM。比作用于HDAC1和6选择性高200多倍，比作用于HDAC2， 3，和10选择性高1000倍。 |
(d) Effects of HDAC8 activity on ISO-induced augmentation of apoptosis and TIPRL expression. H1299 cells were sequentially treated with 10 μm PCI-34051 for 24 h, ISO for 30 min and 50 μM cisplatin for 48 h before the western blot analysis.
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| S1422 |
DroxinostatDroxinostat是一种选择性的HDAC抑制剂，最有效作用于HDACs 6和8，IC50为2.47μM和1.46 μM，比作用于HDAC3选择性高8倍，对HDAC1， 2， 4， 5， 7， 9，和10没有抑制作用。 |
Chemical inhibition of HDAC3, -6, and -8 with the selective HDAC inhibitor Droxinostat (2 uM) resulted in a significant increase in the percent of 2D10 cells expressing GFP in cells that had been depleted of HDAC3 but not HDAC1 or -2. (*p<0.05).
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| S1090 |
Abexinostat (PCI-24781)Abexinostat (PCI-24781)是一种新型的pan-HDAC抑制剂，靶向作用于HDAC1，Ki为7 nM，对HDACs 2， 3， 6，和10有适中的抑制性，但比作用于HDAC8选择性强40倍。Phase 1/2。 |
Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50. |
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| S7229 |
RGFP966RGFP966是一种HDAC3抑制剂，无细胞试验中IC50为0.08μM ，比作用于其他HDAC选择性高200倍以上。 |
THP-1 cells were treated with indicated concentrations of Ara-C and/or RGFP966 for 24 h, and lysates were immunoblotted for p-AKT473, AKT and γH2AX.
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| S2244 |
AR-42AR-42是一种HDAC抑制剂，IC50为30 nM。Phase 1。 |
One- to 2-month-old mice of both genotypes showed an increase in H3K4me3 (n = 5 to 6 per group) associated with a dose-dependent increase in neurogenesis in Kmt2d+/βGeo mice (monitored by normalized DCX expression) (n = 4 to 6 per group) upon treatment with the HDACi AR-42. There was no difference in either H3K4me3 or neurogenesis between Kmt2d+/βGeo and Kmt2d+/+ animals at a dose of 10 mg/kg per day.
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| S8001 |
Ricolinostat (ACY-1215)Ricolinostat (ACY-1215)是一种选择性HDAC6抑制剂，无细胞试验中IC50为5 nM，作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上，对HDAC8具有微弱的作用活性，对HDAC4/5/7/9/11， Sirtuin1和Sirtuin2具有最小的作用活性。Phase 2。 |
(a) Representative images from hTERT RPE-1 cells transiently transfected with siControl (siC), treated with vehicle (DMSO), alisertib (MLN8237) or rocilinostat (ACY1215) at the time of serum withdrawal for 48 h. Ciliation monitored by immunofluorescent staining using acetylated α-tubulin (cilia marker) and pericentrin (basal body marker). Nuclei counterstained using DAPI. Highlighted boxes show magnified cilia. Scale bar, 3 μM. |
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| S1168 |
Valproic acid sodium salt (Sodium valproate)Valproic acid sodium salt (Sodium valproate)是一种HDAC选择性抑制剂，也会抑制HDAC2的蛋白酶体降解，用于治疗癫痫和躁郁症，并预防偏头痛。 |
Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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| S2818 |
Tacedinaline (CI994)Tacedinaline (CI994)是一种选择性的I型HDAC抑制剂，其对HDAC 1, 2, 3,和8的IC50分别为0.9, 0.9, 1.2, 和 >20 μM。Phase 3。 |
A, 5×106 HeLa, A549, 293T, and H1299 cells were seeded in 10-cm cell culture dishes on day 0 and treated with dimethyl sulfoxide, 10 μM CI994, or 1 μM RGFP966 for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and -actin.
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| S2759 |
Fimepinostat（CUDC-907）CUDC-907是一种PI3K和HDAC双重抑制剂，作用于PI3Kα和HDAC1/2/3/10，IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。Phase 1。 |
Representative Oil Red O staining of lipid-filled mature adipocytes on day 7 for uninduced cells (a), adipocyteinduced hMSCs exposed to the vehicle control (b) or CUDC-907-treated cells (500 nM) (c). Nile red staining (d and e) on day 7 of post-adipocytic induction in hMSCs and after exposure to CUDC-907. Images were captured at ×20 magnification using the FLoid Cell Imaging Station. The level of Nile red staining was quantified using the Molecular Devices M5 Microplate Reader (f). Data are presented as mean ± S.E (n = 16) from three independent experiments, ***P <0.0005.
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| S1999 |
Sodium butyrateSodium butyrate, 是butyrate的钠盐形式。是histone deacetylase(HDAC)抑制剂，与I类和II类HDACs的锌区竞争性结合。 |
U87 cells were cultured with DMSO or 10 µM 5azadC for 72 h. For the latter, 1 µM Trichostatin A (TSA), 10 mM sodium butyrate (NaBu), 5 mM nicotinamide (NAM), or 0.5 µM apicidin were added in the last 24 h. IFNLR1 expression was determined by RT-qPCR. |
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| S1848 |
CurcuminCurcumin 是流行的印度香料姜黄的主要姜黄色素，属于姜科（Zingiberaceae）。它是p300 histone acetylatransferase（IC50~25 μM）和Histone deacetylase的抑制剂，能够激活Nrf2 pathway并抑制NF-κB的激活。 |
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| S2779 |
M344M344是一种有效的HDAC抑制剂，IC50为100 nM，可以诱导细胞分化。 |
HCT116 p53 null cells were treated with different HDACIs (1 μM TSA, 5 μM M344, 1 μM MS-275, 5 mM But, 10 mM VPA) for 24 h. ATF4, ATF3, CHOP and DR5 proteins were measured by Western blot. |
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| S2239 |
TubacinTubacin是一种高度有效的选择性的，可逆的，细胞渗透性HDAC6抑制剂，无细胞试验中IC50为4 nM，比作用于HDAC1的选择性高350倍。 |
Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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| S7292 |
RG2833 (RGFP109)RG2833 (RGFP109)是一种大脑渗透性HDAC抑制剂，作用于HDAC1和HDAC3，无细胞试验中IC50分别为60 nM和50 nM。 |
The cells were treated with 1 μM RG2833 (HDAC1/3 inhibitor), 2 μM RGFP966 (HDAC3 inhibitor), 1 μM TSA (pan-HDAC inhibitor), or vehicle for 16 h in serum-free medium. Cell lysates were analysed by Western blotting for expression of SREBP-2 activated fragment, HMG-CoA reductase and APP. Shown are representative blots and quantifications with means ± SEM of the indicated number of independent experiments performed in duplicate. *p < 0.05; **p < 0.01; n.s., not significant in one-sample t-test.
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| S2693 |
ResminostatResminostat剂量依赖性的选择性的抑制HDAC1/3/6， IC50为42.5 nM/50.1 nM/71.8 nM，作用于HDAC8效果弱，IC50为877 nM。 |
Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
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| S1703 |
Divalproex SodiumDivalproex Sodium是由肠溶包衣中丙戊酸钠和丙戊酸按1:1摩尔组成的化合物，是一种HDAC抑制剂，用于治疗癫痫。 |
Divalproex sodium increases the level of acetylated histone H3 level in ataxin-3-transfected HEK293 cells. Normal (15CAG) or expanded (77CAG) ataxin-3-transfected cells were treated with divalproex sodium (Selleck chemical, 0.3 mmol/L in DMSO, (+)) or with DMSO alone (−) 48 h after transfection. The cells were treated with divalproex sodium or DMSO over 6, 12, and 24 h. The Western blot was probed with antiacetylated histone H3, antihistone H3, and antiataxin-3. Antibodies include antihistone H3 and antiataxin-3 are used as controls. The x-axis shows the different treatment group. The y-axis represents the acetylated histone H3 values normalized to histone H3. Error bars represent the standard error of the mean. Data represent three independent experiments (n = 3). The data with a normal distribution were analyzed with Student’s t-test. *P < 0.05
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| S8043 |
ScriptaidScriptaid 是一种HDAC抑制剂，作用于乙酰化H4比作用于H3效果高很多。 |
The relative expression of Oct4, Nanog, Klf4 and Sox2 at the blastocyst stage in ICSI-, ROSI- and ROSI + incubation of zygotes with 250 nM Scriptaid for 10 h (ROSI-S)-derived embryos. Five blastocysts in each pool were examined to obtain the data set in each column. Q-PCR analysis was performed in triplicate. Different letters indicate significant differences between values (P < 0.05).
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| S4125 |
Sodium PhenylbutyrateSodium Phenylbutyrate是一种转录调节因子，通过调控HDAC活性来改变染色质结构从而发挥作用。 |
Representative images and quantitative analysis results of the transwell experiment. Notes: (A) Results of migration assay for DU145. (B) Results of invasion assay for DU145. (C) Results of migration assay for PC3. (D) Results of invasion assay for PC3. “*” Means significantly different from control group, P<0.05. Abbreviation: SPB, sodium phenylbutyrate.
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| S8049 |
Tubastatin ATubastatin A是一种有效的，选择性HDAC6抑制剂，无细胞试验中IC50为15 nM，选择性远高于所有其他同工酶(1000倍)除了HDAC8(57倍)。 |
Control and MEC17 KD macrophages (RAW264.7) were treated with TBSA or DMSO for 12 hours followed by LPS treatment for indicated time. p38 phosphorylation were determined by immuno-blotting.
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| S7324 |
TMP269TMP269 是强效的选择性的IIa类HDAC抑制剂，其作用于HDAC4, HDAC5, HDAC7 和 HDAC9的IC50分别为126 nM, 80 nM, 36 nM 和 19 nM。 |
Staining of live (calcein-AM, green) and dead (PI, red) UCC cells after 72 h of treatment with TMP269. Data shown are a representative experiment of a set of 3
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| S7595 |
Santacruzamate A (CAY10683)Santacruzamate A（CAY10683）是一种强效的选择性HDAC抑制剂，其对HDAC2的IC50为119 pM ，比对其他HDACs高出 >3600倍的选择性。 |
Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
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| S8502 |
TMP195TMP195是一种选择性的class IIa HDAC抑制剂，在基于细胞的实验中，IC50为300 nM。 |
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| S3944 |
Valproic acidValproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers. |
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| S5810 |
UF010UF010是I类HDAC选择性抑制剂，对HDAC1、HDAC2、HDAC3、HDAC8、HDAC6和HDAC10的IC50值分别为0.5 nM、0.1 nM、0.06 nM、1.5 nM、9.1 nM和15.3 nM。 |
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| S7617 |
TasquinimodTasquinimod是一种口服有效的antiangiogenic药剂，通过变构抑制HDAC4信号发挥作用。Phase 3。 |
Western blot images suggested inhibition of HDAC4 increased the expression of NOX4 and MMP-9, and treatment with 10 μM SCM-198 reduced the raised levels of NOX4 and MMP-9. |
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| S9275 |
IsoguanosineIsoguanosine 抑制 FLT3 和 HDAC3/6 治疗AML。Isoguanosine 是巴豆（Croton tiglium）种子中天然存在的鸟苷的活性异构体。 |
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| S7726 |
BRD73954BRD73954是一种有效的选择性 HDAC 抑制剂，对HDAC6 和 HDAC8的 IC50 分别为 36 nM 和 120 nM。 |
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| S8464 |
Citarinostat (ACY-241)Citarinostat (ACY-241)是一种具有口服活性的、选择性HDAC6抑制剂，对HDAC6和HDAC3的IC50分别为2.6 nM和46 nM。对HDAC6的选择性是对HDAC1-3的选择性的13-18倍。 |
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| S5905 |
Suberohydroxamic acidSuberohydroxamic acid是竞争性HDAC抑制剂，对HDAC1和HDAC3的IC50分别为0.25 μM和0.3 μM。 |
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| S7593 |
SplitomicinSplitomicin是一种选择性的NAD(+)-dependent histone deacetylase Sir2p抑制剂，IC50为60 μM。在细胞中有着更高的活性。 |
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| S7278 |
HPOBHPOB是一种有效的，选择性 HDAC6抑制剂，IC50为56 nM，选择性比对其它HDACs高30多倍。 |
Effects of HPOB on GCs-induced apoptosis in PC12 and SH-SY5Y cells. (A) Effect of 48 h treatment with HPOB alone and (B) anti-apoptotic effect of HPOB pre-treatment for 24 h on Cort-induced apoptosis in PC12 cells. The results are expressed as the means ± SD of three independent experiments. ## indicates a significant difference from the control (P < 0.01). * indicates a significant difference from treatment with Cort alone at P < 0.05. ** indicates a significant difference from treatment with Cort alone at P < 0.01.
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| S7569 |
LMK-235LMK-235是HDAC4和HDAC5的选择性抑制剂， IC50分别为11.9 nM 和 4.2 nM。 |
Upper panel: qPCR analysis of CDX2-negative HT29 cells treated with increasing concentrations of the DNMTi decitabine (1.25 μM, 2.5 μM, 5 μM, 10 μM) for 48 h and increasing concentrations of the HDAC4/5i LMK-235 (5 nM, 10 nM, 20 nM, 40 nM, 80 nM). Data were normalized to the HMBS housekeeping gene and are shown as n-fold regulation compared with DMSO-treated cells. MWU: ***p < 0.001, (n = 4). Lower panel: CDX2 Western blot analysis of the three highest concentrations for both compounds of HT29 cells treated as above. Total protein is shown as a loading control. Percentage indicates amount of protein normalized to respective DMSO controls
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| S5438 |
Biphenyl-4-sulfonyl chlorideBiphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation. |
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| S7473 |
Nexturastat ANexturastat A 是一种强效的选择性的HDAC抑制剂，IC50为5 nM,其选择性高于其他的HDACs190倍。 |
HDAC inhibitors disrupt SS18-SSX/TLE1 co-localization. A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells A, B. is also confirmed by immunoprecipitation C. The decrease in PLA co-localization signal correlates with apoptosis induction by HDAC inhibitor FK228 in SYO-1 cells. |
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| S8773 |
TH34TH34是HDAC抑制剂，对HDAC6、HDAC8和HDAC10的选择性比HDAC1、HDAC2和HDAC3高。在 NanoBRET实验中，TH34与HDAC6/8/10紧密结合，IC50分别为4.6 μM、1.9 μM和7.7 μM。 |
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| S8567 |
Tucidinostat (Chidamide)Chidamide是HDAC1, 2, 3, 10的低摩尔浓度抑制剂，IC50分别为95、160、67、78 nM。 |
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| S2341 |
(-)-Parthenolide(-)-Parthenolide, Nuclear Factor-κB抑制剂，可特异性地耗尽HDAC1蛋白，而不影响其他I/II类 HDACs。促进MDM2的泛素化并激活p53的细胞功能。 |
G. To evaluate effects of IKBKE/TBK1 inhibition on NF-κB signaling in Ewing, TC32 cells were incubated with CYT387 for six hours prior to stimulation with TNF-α (30 ng/mL). IκBα degradation was measured by harvesting TC32 cells thirty minutes after stimulation with TNF-α. TNF-α stimulation resulted in degradation of IκBα, and this effect was attenuated with CYT387 treatment. Parthenolide, an inhibitor of IκBα phosphorylation was used as a positive control. Similar effects of CYT387 activity were seen in HEK-293T cells which also express IKBKΕ. Nuclear extracts were prepared from TC32 cells harvested following forty-five minutes of TNF-α stimulation. Treatment with CYT387 resulted in decreased nuclear localization of NF-κB family proteins RelA/p65 and c-Rel. There was a modest impairment of p50 nuclear localization as compared to parthenolide and DMSO controls and no change in p52 nuclear localization. RelB (not shown) is not expressed in TC32 cells |
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| S8495 |
WT161WT161是有效的、选择性的HDAC6抑制剂，对HDAC6、HDAC1和HDAC2的IC50值分别为0.4 nM、8.35 nM和15.4 nM，比对其他HDACs的选择性高100倍以上。 |
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| S7596 |
CAY10603CAY10603是一种强效的选择性HDAC6抑制剂，IC50为2 pM，选择性比其它HDACs高200多倍。 |
U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
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| S8648 |
ACY-738ACY-738以低纳摩尔浓度抑制HDAC6，IC50为1.7 nM。其对HDAC6的选择性比对其他I类HDACs高60-1500倍。 |
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| S9262 |
Raddeanin ARaddeanin A, a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity. |
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| S7555 |
Domatinostat (4SC-202)4SC-202是一种选择性的I类HDAC抑制剂，对HDAC1，HDAC2，和HDAC3的IC50分别为1.20 μM，1.12 μM，和0.57 μM。也对Lysine specific demethylase 1 (LSD1)表现出抑制活性。Phase 1。 |
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| S7689 |
BG45BG45 是I类 HDAC 抑制剂，无细胞试验中对 HDAC3，HDAC1，HDAC2，和 HDAC6的 IC50 分别为 289 nM，2.0 µM，2.2 µM 和 >20 µM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
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| S8323 |
ITSA-1 (ITSA1)ITSA-1 (ITSA1)通过抑制TSA（曲古菌素A），激活HDAC。但对其他HDAC抑制剂没有活性。 |
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