HDAC

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抑制剂选择性比较

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所有产品 HDAC抑制剂(58) HDAC激活剂(1) 新HDAC产品

产品目录	产品描述	文献引用	实验数据
S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。	Cancer Res, 2019, 79(7):1658-1670 Clin Cancer Res, 2018, 24(16):3941-3954 Nature, 2017, 551(7679):247-250	Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype).
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。	Sci Rep, 2017, 589:97-106 Int J Neuropsychopharmacol, 2016, 10.1093/ijnp/pyw035 BMC Cancer, 2016, 10.1186/s12885-016-2353-7	(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.
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。	Cell, 2018, 173(6):1413-1425 Clin Cancer Res, 2018, 24(16):3941-3954 Clin Cancer Res, 2018, 24(1):120-129.	LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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。	Nature, 2017, 551(7679):247-250 Cell, 2017, 171(4):824-835.e18 Biochem Biophys Res Commun, 2017, 485(2):454-460	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.
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。	Cell Signal, 2016, 28(8):1015-24 Nat Biotechnol, 2015, 10.1038/nbt.3130 Nucleic Acids Res, 2015, 10.1093/nar/gkv188	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.
S8743^New	SKLB-23bb SKLB-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。
S8769^New	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。
S8773^New	TH34 TH34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。
S5810^New	UF010 UF010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。
S5905^New	Suberohydroxamic acid Suberohydroxamic 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。
S9262^New	Raddeanin A Raddeanin A, a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity.
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。	Cell, 2018, 173(6):1413-1425 Clin Cancer Res, 2017, 23(12):3139-3149 Clin Cancer Res, 2017, 23(18):5573-5584	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.
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。	Blood, 2018, 131(4):397-407 Nature, 2017, 551(7679):247-250 Biochem Pharmacol, 2017, 127:90-100	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.
S1484	MC1568 MC1568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。	Biochim Biophys Acta, 2016, 1859(2):294-305 FEBS Lett, 2015, 589(10):1080-8 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	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.
S2627	Tubastatin A HCl Tubastatin 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)。	Inflamm Res, 2016, 65(12):995-1008 Methods Enzymol, 2016, 573:161-81 Oncotarget, 2016, 7(23):33484-97	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.
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。	Diabetologia, 2018, 61(2):389-398 J Biol Chem, 2015, 290(8):5028-40 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	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.
S1095	Dacinostat (LAQ824) Dacinostat (LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。	Cell Physiol Biochem, 2017, 41(3):1255-1266 J Hum Genet, 2016, 10.1038/jhg.2016.61 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	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.
S1194	CUDC-101 CUDC-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。	Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066 Biomed Res, 2015, 2(1):105-119 J Chem Inf Model, 2014, 54(3):881-93	(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.
S1096	Quisinostat (JNJ-26481585) 2HCl Quisinostat (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。	Cancer Lett, 2018, 428:160-172 Cell Death Dis, 2017, 8(6):e2879 J Clin Oncol, 2016, 10.1200/JCO.2016.66.5547	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.
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。	PLoS One, 2017, 12(3):e0174107 Blood Cells Mol Dis, 2016, 56(1):62-9 Oncotarget, 2016, 7(23):34384-94	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.
S2012	PCI-34051 PCI-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。	Stem Cells Transl Med, 2018, 10.1002/sctm.18-0057 Oncol Rep, 2018, 40(2):635-646 Virol Sin, 2018, 33(5):418-428	(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.
S1422	Droxinostat Droxinostat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。	Clin Cancer Res, 2017, 23(12):3139-3149 Int J Cancer, 2016, 138(1):125-36 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	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).
S1090	Abexinostat (PCI-24781) Abexinostat (PCI-24781)是一种新型的pan-HDAC抑制剂，靶向作用于HDAC1，K_i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。	Cancer Cell Int, 2016, 16:31 Oncotarget, 2016, 7(23):34384-94 Nat Biotechnol, 2015, 10.1038/nbt.3130	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.
S7229	RGFP966 RGFP966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。	Cell, 2019, 176(6):1447-1460 Endocrinology, 2018, 159(7):2520-2527 J Cell Physiol, 2018, 10.1002/jcp.27265	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.
S2244	AR-42 AR-42是一种HDAC抑制剂，IC50为30 nM。Phase 1。	J Cell Physiol, 2019, 234(4):5252-5263 J Cell Physiol, 2018, 233(1):559-571 Life Sci, 2018, 211:224-237	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.
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。	J Pathol, 2018, 246(2):141-153 Br J Cancer, 2018, 119(10):1278-1287 Mol Cancer Ther, 2018, 17(6):1280-1290	(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.
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。	Front Immunol, 2017, 7:696 Cell Death Dis, 2016, 7:e2221 Nat Biotechnol, 2015, 10.1038/nbt.3130	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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。	J Cell Physiol, 2018, 10.1002/jcp.27873 Anticancer Res, 2018, 38(1):271-277 Cell Reprogram, 2018, 20(3):205-213	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.
S2759	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。	J Cell Mol Med, 2018, 10.1111/jcmm.13935 Biochem Pharmacol, 2018, 148:13-26 Front Cell Infect Microbiol, 2018, 8:191	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.
S1999	Sodium butyrate Sodium 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。	Cancer Res, 2017, 77(18):5039-5053 Br J Haematol, 2014, 167(5):639-50 PLoS Biol, 2013, 12(1):e1001758	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.
S1848	Curcumin Curcumin 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。	J Exp Clin Cancer Res, 2018, 37(1):303 Front Pharmacol, 2018, 9:60 Neurourol Urodyn, 2018, 37(8):2470-2479
S2779	M344 M344是一种有效的HDAC抑制剂，IC50为100 nM，可以诱导细胞分化。	Biochem Biophys Res Commun, 2014, 445(2):320-6	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.
S2239	Tubacin Tubacin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。	Int J Cancer, 2019, 10.1002/ijc.32169 J Thorac Cardiovasc Surg, 2018, 10.1016/j.jtcvs.2018.10.136 Oncogene, 2016, 35(18):2333-44	Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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。	J Cell Physiol, 2019, 234(2):1088-1098 Sci Rep, 2017, 7:43575 Neurochem Res, 2016, 41(12):3192-3205	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.
S2693	Resminostat Resminostat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。	Int J Oncol, 2018, 53(4):1469-1480 Head Neck, 2017, 39(5):900-907	Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
S1703	Divalproex Sodium Divalproex 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。	CNS Neurosci Ther, 2018, 24(5):404-411	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
S8043	Scriptaid Scriptaid 是一种HDAC抑制剂，作用于乙酰化H4比作用于H3效果高很多。	Oncol Rep, 2018, 39(4):1999-2005 Hum Reprod, 2017, 32(1):76-87 Blood, 2017, 130(14):1628-1638	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).
S4125	Sodium Phenylbutyrate Sodium 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。	CNS Neurosci Ther, 2018, 24(5):404-411 J Thromb Haemost, 2018, 16(10):2035-2043 Onco Targets Ther, 2016, 9:2825-33	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.
S8049	Tubastatin A Tubastatin 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)。	Clin Sci , 2018, 132(3):339-359 J Cell Biochem, 2018, 119(8):6623-6632 Cancer Lett, 2017, 391:89-99	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.
S7324	TMP269 TMP269 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。	Clin Epigenetics, 2018, 10(1):100 J Cell Biochem, 2018, 119(4):3081-3090 Drug Des Devel Ther, 2017, 11:1369-1382	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
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。	Neurochem Res, 2018, 43(6):1161-1170	Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
S8502	TMP195 TMP195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。
S3944	Valproic acid Valproic 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.	J Trauma Acute Care Surg, 2017, 82(4):758-765
S7617	Tasquinimod Tasquinimod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。	J Mol Cell Biol, 2018, 10.1093/jmcb/mjy035 Oxid Med Cell Longev, 2017, 7150376 Oxid Med Cell Longev, 2017, 2017:7150376	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.
S7726	BRD73954 BRD73954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。
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。
S7593	Splitomicin Splitomicin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。
S7278	HPOB HPOB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。	Molecules, 2018, 23(5) Neurochem Int, 2016, 99:239-51	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.
S7569	LMK-235 LMK-235是HDAC4和HDAC5的选择性抑制剂， IC50分别为11.9 nM 和 4.2 nM。	Clin Epigenetics, 2018, 10(1):120 Int J Mol Sci, 2018, 19(10) Mol Med Rep, 2018, 17(1):1445-1452	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
S5438	Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
S7473	Nexturastat A Nexturastat 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。	Oncotarget, 2016, 7(39):63829-63838 Oncotarget, 2016, 7(23):34384-94	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.
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。
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。	Biochem Biophys Res Commun, 2018, 501(1):246-252 Oncol Rep, 2018, 39(3):1181-1190 J Neuroimmunol, 2017, 305:154-161	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
S8495	WT161 WT161是有效的、选择性的、具有口服活性的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。
S7596	CAY10603 CAY10603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。	Sci Rep, 2017, 7:45266 Cancer Lett, 2016, 379(1):134-42 Med Oncol, 2016, 33(5):50	U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
S8648	ACY-738 ACY-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。
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。
S7689	BG45 BG45 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。
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。

产品目录	产品描述	文献引用	实验数据
S1047	Vorinostat (SAHA, MK0683) Vorinostat (suberoylanilide hydroxamic acid, SAHA)是一种HDAC抑制剂，无细胞试验中IC50为~10 nM。	Cancer Res,2019, 79(7):1658-1670 Clin Cancer Res,2018, 24(16):3941-3954 Nature,2017, 551(7679):247-250	Western blot analysis of histone H3 acetylation in the spleen of untreated and vorinostat-treated hNF-E2 tg mice (n = 4 of each genotype).
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。	Sci Rep,2017, 589:97-106 Int J Neuropsychopharmacol,2016, 10.1093/ijnp/pyw035 BMC Cancer,2016, 10.1186/s12885-016-2353-7	(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.
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。	Cell,2018, 173(6):1413-1425 Clin Cancer Res,2018, 24(16):3941-3954 Clin Cancer Res,2018, 24(1):120-129.	LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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。	Nature,2017, 551(7679):247-250 Cell,2017, 171(4):824-835.e18 Biochem Biophys Res Commun,2017, 485(2):454-460	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.
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。	Cell Signal,2016, 28(8):1015-24 Nat Biotechnol,2015, 10.1038/nbt.3130 Nucleic Acids Res,2015, 10.1093/nar/gkv188	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.
S8743^New	SKLB-23bb SKLB-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。
S8769^New	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。
S8773^New	TH34 TH34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。
S5810^New	UF010 UF010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。
S5905^New	Suberohydroxamic acid Suberohydroxamic 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。
S9262^New	Raddeanin A Raddeanin A, a triterpenoid saponin from Anemone raddeana Regel, displays moderate inhibitory activity against histone deacetylases (HDACs) and has high antiangiogenic potency, antitumor activity.
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。	Cell,2018, 173(6):1413-1425 Clin Cancer Res,2017, 23(12):3139-3149 Clin Cancer Res,2017, 23(18):5573-5584	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.
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。	Blood,2018, 131(4):397-407 Nature,2017, 551(7679):247-250 Biochem Pharmacol,2017, 127:90-100	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.
S1484	MC1568 MC1568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。	Biochim Biophys Acta,2016, 1859(2):294-305 FEBS Lett,2015, 589(10):1080-8 Bioorg Med Chem,2015, 10.1016/j.bmc.2014.12.066	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.
S2627	Tubastatin A HCl Tubastatin 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)。	Inflamm Res,2016, 65(12):995-1008 Methods Enzymol,2016, 573:161-81 Oncotarget,2016, 7(23):33484-97	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.
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。	Diabetologia,2018, 61(2):389-398 J Biol Chem,2015, 290(8):5028-40 Bioorg Med Chem,2015, 10.1016/j.bmc.2014.12.066	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.
S1095	Dacinostat (LAQ824) Dacinostat (LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。	Cell Physiol Biochem,2017, 41(3):1255-1266 J Hum Genet,2016, 10.1038/jhg.2016.61 Bioorg Med Chem,2015, 10.1016/j.bmc.2014.12.066	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.
S1194	CUDC-101 CUDC-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。	Bioorg Med Chem,2015, 10.1016/j.bmc.2014.12.066 Biomed Res,2015, 2(1):105-119 J Chem Inf Model,2014, 54(3):881-93	(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.
S1096	Quisinostat (JNJ-26481585) 2HCl Quisinostat (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。	Cancer Lett,2018, 428:160-172 Cell Death Dis,2017, 8(6):e2879 J Clin Oncol,2016, 10.1200/JCO.2016.66.5547	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.
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。	PLoS One,2017, 12(3):e0174107 Blood Cells Mol Dis,2016, 56(1):62-9 Oncotarget,2016, 7(23):34384-94	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.
S2012	PCI-34051 PCI-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。	Stem Cells Transl Med,2018, 10.1002/sctm.18-0057 Oncol Rep,2018, 40(2):635-646 Virol Sin,2018, 33(5):418-428	(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.
S1422	Droxinostat Droxinostat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。	Clin Cancer Res,2017, 23(12):3139-3149 Int J Cancer,2016, 138(1):125-36 Bioorg Med Chem,2015, 10.1016/j.bmc.2014.12.066	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).
S1090	Abexinostat (PCI-24781) Abexinostat (PCI-24781)是一种新型的pan-HDAC抑制剂，靶向作用于HDAC1，K_i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。	Cancer Cell Int,2016, 16:31 Oncotarget,2016, 7(23):34384-94 Nat Biotechnol,2015, 10.1038/nbt.3130	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.
S7229	RGFP966 RGFP966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。	Cell,2019, 176(6):1447-1460 Endocrinology,2018, 159(7):2520-2527 J Cell Physiol,2018, 10.1002/jcp.27265	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.
S2244	AR-42 AR-42是一种HDAC抑制剂，IC50为30 nM。Phase 1。	J Cell Physiol,2019, 234(4):5252-5263 J Cell Physiol,2018, 233(1):559-571 Life Sci,2018, 211:224-237	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.
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。	J Pathol,2018, 246(2):141-153 Br J Cancer,2018, 119(10):1278-1287 Mol Cancer Ther,2018, 17(6):1280-1290	(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.
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。	Front Immunol,2017, 7:696 Cell Death Dis,2016, 7:e2221 Nat Biotechnol,2015, 10.1038/nbt.3130	Western blot analysis of Acetylated Histone and Histone. 0-10μM sodium valproate was added.
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。	J Cell Physiol,2018, 10.1002/jcp.27873 Anticancer Res,2018, 38(1):271-277 Cell Reprogram,2018, 20(3):205-213	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.
S2759	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。	J Cell Mol Med,2018, 10.1111/jcmm.13935 Biochem Pharmacol,2018, 148:13-26 Front Cell Infect Microbiol,2018, 8:191	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.
S1999	Sodium butyrate Sodium 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。	Cancer Res,2017, 77(18):5039-5053 Br J Haematol,2014, 167(5):639-50 PLoS Biol,2013, 12(1):e1001758	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.
S1848	Curcumin Curcumin 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。	J Exp Clin Cancer Res,2018, 37(1):303 Front Pharmacol,2018, 9:60 Neurourol Urodyn,2018, 37(8):2470-2479
S2779	M344 M344是一种有效的HDAC抑制剂，IC50为100 nM，可以诱导细胞分化。	Biochem Biophys Res Commun,2014, 445(2):320-6	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.
S2239	Tubacin Tubacin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。	Int J Cancer,2019, 10.1002/ijc.32169 J Thorac Cardiovasc Surg,2018, 10.1016/j.jtcvs.2018.10.136 Oncogene,2016, 35(18):2333-44	Verification of Hdac6 deletion in knockout MEFs. Expression of HDAC6 and acetylation of tubulin were analyzed by immunoblotting.
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。	J Cell Physiol,2019, 234(2):1088-1098 Sci Rep,2017, 7:43575 Neurochem Res,2016, 41(12):3192-3205	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.
S2693	Resminostat Resminostat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。	Int J Oncol,2018, 53(4):1469-1480 Head Neck,2017, 39(5):900-907	Assessment of apoptosis by flow cytometry. (A) SCC25 cells were treated with 2.5 μM and 5 μM resminostat. *Significant induction of cell death.
S1703	Divalproex Sodium Divalproex 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。	CNS Neurosci Ther,2018, 24(5):404-411	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
S8043	Scriptaid Scriptaid 是一种HDAC抑制剂，作用于乙酰化H4比作用于H3效果高很多。	Oncol Rep,2018, 39(4):1999-2005 Hum Reprod,2017, 32(1):76-87 Blood,2017, 130(14):1628-1638	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).
S4125	Sodium Phenylbutyrate Sodium 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。	CNS Neurosci Ther,2018, 24(5):404-411 J Thromb Haemost,2018, 16(10):2035-2043 Onco Targets Ther,2016, 9:2825-33	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.
S8049	Tubastatin A Tubastatin 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)。	Clin Sci ,2018, 132(3):339-359 J Cell Biochem,2018, 119(8):6623-6632 Cancer Lett,2017, 391:89-99	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.
S7324	TMP269 TMP269 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。	Clin Epigenetics,2018, 10(1):100 J Cell Biochem,2018, 119(4):3081-3090 Drug Des Devel Ther,2017, 11:1369-1382	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
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。	Neurochem Res,2018, 43(6):1161-1170	Effect of HDAC inhibitors on the expression of key cell cycle-related proteins in HepG2 and Huh7 cells. CAY: CAY10683
S8502	TMP195 TMP195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。
S3944	Valproic acid Valproic 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.	J Trauma Acute Care Surg,2017, 82(4):758-765
S7617	Tasquinimod Tasquinimod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。	J Mol Cell Biol,2018, 10.1093/jmcb/mjy035 Oxid Med Cell Longev,2017, 7150376 Oxid Med Cell Longev,2017, 2017:7150376	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.
S7726	BRD73954 BRD73954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。
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。
S7593	Splitomicin Splitomicin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。
S7278	HPOB HPOB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。	Molecules,2018, 23(5) Neurochem Int,2016, 99:239-51	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.
S7569	LMK-235 LMK-235是HDAC4和HDAC5的选择性抑制剂， IC50分别为11.9 nM 和 4.2 nM。	Clin Epigenetics,2018, 10(1):120 Int J Mol Sci,2018, 19(10) Mol Med Rep,2018, 17(1):1445-1452	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
S5438	Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
S7473	Nexturastat A Nexturastat 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。	Oncotarget,2016, 7(39):63829-63838 Oncotarget,2016, 7(23):34384-94	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.
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。
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。	Biochem Biophys Res Commun,2018, 501(1):246-252 Oncol Rep,2018, 39(3):1181-1190 J Neuroimmunol,2017, 305:154-161	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
S8495	WT161 WT161是有效的、选择性的、具有口服活性的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。
S7596	CAY10603 CAY10603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。	Sci Rep,2017, 7:45266 Cancer Lett,2016, 379(1):134-42 Med Oncol,2016, 33(5):50	U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
S8648	ACY-738 ACY-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。
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。
S7689	BG45 BG45 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。