HDAC

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S1047	Vorinostat (SAHA, MK0683)	<1 mg/mL	52 mg/mL	3 mg/mL
S1053	Entinostat (MS-275)	<1 mg/mL	75 mg/mL	<1 mg/mL
S1030	Panobinostat (LBH589)	<1 mg/mL	69 mg/mL	<1 mg/mL
S1045	Trichostatin A (TSA)	<1 mg/mL	23 mg/mL	<1 mg/mL
S1122	Mocetinostat (MGCD0103)	<1 mg/mL	13 mg/mL	<1 mg/mL
S5438	Biphenyl-4-sulfonyl chloride	-1 mg/mL	50 mg/mL	-1 mg/mL
S8495	WT161	<1 mg/mL	86 mg/mL	1 mg/mL
S8648	ACY-738	<1 mg/mL	54 mg/mL	1 mg/mL
S1085	Belinostat (PXD101)	<1 mg/mL	64 mg/mL	<1 mg/mL
S3020	Romidepsin (FK228, Depsipeptide)	<1 mg/mL	10 mg/mL	<1 mg/mL
S1484	MC1568	<1 mg/mL	13 mg/mL	<1 mg/mL
S2627	Tubastatin A HCl	<1 mg/mL	74 mg/mL	<1 mg/mL
S2170	Givinostat (ITF2357)	<1 mg/mL	95 mg/mL	3 mg/mL
S1095	Dacinostat (LAQ824)	<1 mg/mL	76 mg/mL	<1 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S1096	Quisinostat (JNJ-26481585) 2HCl	<1 mg/mL	79 mg/mL	<1 mg/mL
S1515	Pracinostat (SB939)	<1 mg/mL	72 mg/mL	27 mg/mL
S2012	PCI-34051	<1 mg/mL	59 mg/mL	<1 mg/mL
S1422	Droxinostat	<1 mg/mL	49 mg/mL	49 mg/mL
S1090	Abexinostat (PCI-24781)	<1 mg/mL	80 mg/mL	<1 mg/mL
S7229	RGFP966	<1 mg/mL	72 mg/mL	<1 mg/mL
S2244	AR-42	<1 mg/mL	63 mg/mL	63 mg/mL
S8001	Ricolinostat (ACY-1215)	<1 mg/mL	86 mg/mL	<1 mg/mL
S1168	Valproic acid sodium salt (Sodium valproate)	33 mg/mL	33 mg/mL	33 mg/mL
S2818	Tacedinaline (CI994)	<1 mg/mL	54 mg/mL	<1 mg/mL
S2759	CUDC-907	<1 mg/mL	102 mg/mL	<1 mg/mL
S1999	Sodium butyrate	22 mg/mL	<1 mg/mL	22 mg/mL
S1848	Curcumin	<1 mg/mL	73 mg/mL	<1 mg/mL
S2779	M344	<1 mg/mL	62 mg/mL	4 mg/mL
S2239	Tubacin	<1 mg/mL	100 mg/mL	<1 mg/mL
S7292	RG2833 (RGFP109)	<1 mg/mL	68 mg/mL	10 mg/mL
S2693	Resminostat	<1 mg/mL	70 mg/mL	70 mg/mL
S1703	Divalproex Sodium	62 mg/mL	62 mg/mL	62 mg/mL
S8043	Scriptaid	<1 mg/mL	65 mg/mL	<1 mg/mL
S4125	Sodium Phenylbutyrate	30 mg/mL	8 mg/mL	<1 mg/mL
S8049	Tubastatin A	<1 mg/mL	67 mg/mL	<1 mg/mL
S7324	TMP269	<1 mg/mL	100 mg/mL	2 mg/mL
S7595	Santacruzamate A (CAY10683)	<1 mg/mL	55 mg/mL	55 mg/mL
S8502	TMP195	<1 mg/mL	91 mg/mL	91 mg/mL
S7617	Tasquinimod	<1 mg/mL	81 mg/mL	11 mg/mL
S7726	BRD73954	<1 mg/mL	56 mg/mL	9 mg/mL
S8464	Citarinostat (ACY-241)	<1 mg/mL	41 mg/mL	93 mg/mL
S7593	Splitomicin	<1 mg/mL	39 mg/mL	39 mg/mL
S7278	HPOB	<1 mg/mL	62 mg/mL	38 mg/mL
S7569	LMK-235	<1 mg/mL	58 mg/mL	58 mg/mL
S7473	Nexturastat A	<1 mg/mL	68 mg/mL	2 mg/mL
S8567	Tucidinostat (Chidamide)	<1 mg/mL	78 mg/mL	2 mg/mL
S2341	(-)-Parthenolide	<1 mg/mL	49 mg/mL	49 mg/mL
S7596	CAY10603	<1 mg/mL	89 mg/mL	5 mg/mL
S7555	4SC-202	<1 mg/mL	89 mg/mL	<1 mg/mL
S7689	BG45	<1 mg/mL	42 mg/mL	2 mg/mL
S8323	ITSA-1 (ITSA1)	<1 mg/mL	58 mg/mL	5 mg/mL

特异性亚型抑制剂

HDAC抑制剂（53）
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。	Nature, 2011, 471(7337):235-9 Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130	Activity of vorinostat in Jurkat and Peer T-ALL cell lines in an MTT cell viability assay. Cells were treated with increasing drug concentrations for 72 h. The data are plotted as the mean % of DMSO-treated control cells against the corresponding drug concentration. The error bars are the standard error. For each drug and cell line, 3-4 independent experiments were performed with 6 replicates at each drug concentration.
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。	Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130 Nat Immunol, 2014, 15(5):439-48	(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。	Nat Biotechnol, 2011, 29(3):255-65 Nat Med, 2015, 10.1038/nm.3855 Cell, 2018, 173(6):1413-1425	(G) A375 parental and BRAFi-resistant ex vivo clones were treated with a panel of HDACi (1 μM vorinostat, 0.5 μM belinostat, and 6 nM panobinostat) in single treatment or in combination with 1 μM vemurafenib in a long-term colony formation assay.
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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 Cell, 2017, 171(4):824-835.e18 Cancer Cell, 2014, 26(4):534-48	Gck expression in WT primary hepatocytes transduced with FOXO1 and KR-FOXO1 adenoviruses in the presence or absence of trichostatinA (TSA).
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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 Circ Res, 2012, 110(5):739-48 Blood, 2014, 123(10):1535-43	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.
S5438^New	Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
S8495^New	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。
S3944^New	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.
S8648^New	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。
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。	Nat Biotechnol, 2011, 29(3):255-65 Cell, 2018, 173(6):1413-1425 Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384	A375DR and parental cells were seeded 50,000 cells per well in 6-well plates and treated with 1 mMvorinostat (Vor), 0.5 mMbelinostat (Bel), 5 nMpanobinostat (Pan), and/or combination of 5 nM trametinib and 0.125 mM dabrafenib.
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 Blood, 2018, 131(4):397-407 Clin Cancer Res, 2014, 10.1158/1078-0432.CCR-14-0384	Concentration over time for each dose cohort of romidepsin (B).
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。	Nat Commun, 2013, 4:2735 Proc Natl Acad Sci USA, 2012, 109(34):E2284-93 Diabetes, 2013, 63(2):645-54	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)。	Int J Cancer, 2013, 134(11):2560-71 J Med Chem, 2015, 58(2):785-800 J Biol Chem, 2013, 288(20):14400-7	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。	PLoS Pathog, 2014, 10(4):e1004071 J Neurosci, 2013, 33(17):7535-47 J Antimicrob Chemother, 2014, 69(1):28-33	Representative confocal images of motor axons directly posterior to brains in third instar larvae co-expressing a synaptotagmin-e-GFP fusion protein (syt-eGFP) along with dTip60E431Q under the control of the pan neuronal elav-GAL4 driver reared on food treated with either no drug, ms-275, Givinostat.
S1095	Dacinostat (LAQ824) Dacinostat (LAQ824)是新型HDAC抑制剂，IC50为32 nM，且激活p21启动子。	Nat Biotechnol, 2011, 29(3):255-65 Diabetologia, 2012, 55(9):2421-31 Cell Physiol Biochem, 2017, 41(3):1255-1266	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。	J Chem Inf Model, 2014, 54(3):881-93 ACS Med Chem Lett, 2013, 4(9):858-62 Bioorg Med Chem, 2015, 10.1016/j.bmc.2014.12.066	(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。	J Clin Oncol, 2016, 10.1200/JCO.2016.66.5547 Nat Commun, 2015, 6:8648 Nat Commun, 2013, 4:2735	In vitro drug sensitivity of (C) quisinostat. Acute lymphoblastic leukemia cell lines (NALM-6, KOPN-30bi) and primary cultured cells established from patient 21 were cultured with the indicated concentrations of anticancer drugs, and viability was measured at 48 hours. Data are presented as percentages of dimethylsulfoxide (DMSO) control and depict the mean 6 standard deviation.
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 Pathog, 2014, 10(4):e1004071 Antimicrob Agents Chemother, 2012, 56(7):3849-56 Cancer Cell Int, 2013, 13(1):32	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.
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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 BMC Biol, 2014, 12:95 Exp Mol Med, 2017, 49(2):e297	(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。	Nat Struct Mol Biol, 2013, 20(3):317-25 Int J Cancer, 2016, 138(1):125-36 Oncogenesis, 2014, 3:e127	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。	Nat Biotechnol, 2011, 29(3):255-65 Nat Biotechnol, 2015, 10.1038/nbt.3130 Genet Mol Biol, 2014, 37(4):716-24	Differential effects of HDAC inhibitors on histone and tubulin acetylation. Immunofluorescence analysis of histone H3 (K9ac/K14ac) and tubulin acetylation in HeLa cells treated for 4 h with vehicle, SAHA (10 μM), tacedinaline (50 μM), PCI-24781 (20 μM. (a) Mapping of histone acetylation in K562 cells treated with HDAC inhibitors by LC-MS/MS. Cells were treated with TSA (10 μM), SAHA (5 μM), PCI-24781 (2 μM), tacedinaline (50 μM) for 6 h. Histones were extracted from cells and acetylated peptides were quantified after isobaric tagging.
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。	Leukemia, 2017, 31(12):2761-2770 J Invest Dermatol, 2017, 137(9):1935-1944 J Immunol, 2015, 195(11):5421-31	Representative images of Fluoro-Jade C staining in each group. The histogram shows the numbers of degenerating neurons in the cortex 24 h (C) or 7 days (D) after MCAO (over 30 slices from five rats per group). ∗∗p < 0.01, ∗∗∗p < 0.001 versus MCAO group, ANOVA. Functional outcomes were assessed using the neurological deficits score (day 1, 4, and 7 after MCAO)
S2244	AR-42 AR-42是一种HDAC抑制剂，IC50为30 nM。Phase 1。	Sci Transl Med, 2014, 6(256):256ra135 J Cell Physiol, 2018, 233(1):559-571 J Cell Physiol, 2017, 10.1002/jcp.25916	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。	Oncogene, 2017, 10.1038/onc.2016.495 J Pathol, 2018, 246(2):141-153 Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0481	(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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Neurosci, 2013, 33(17):7535-47 Cell Death Dis, 2016, 7:e2221	(A,B) Wild-type C57BL/6 male mice were treated with vehicle (saline) or 10 mg/kg of paraquat (PQ) for 3 days, and mice received VPA (3.5 mg/kg) or anacardic acid (5 mg/kg) starting 24 and 1 h before PQ injection. IL-6 mRNA expression was determined by real-time PCR.
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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 J Biol Chem, 2016, 291(14):7386-95 J Biomol Screen, 2011, 16(10):1247-53	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。	PLoS Biol, 2013, 12(1):e1001758 Br J Haematol, 2014, 167(5):639-50	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 Enzyme Inhib Med Chem, 2013, 10.3109/14756366.2013.837901 Nanotechnology, 2016, 27(35):355101 Eur J Pharmacol, 2017, 803:167-173	Effect of NC1, NC1-CUR, NC2 and NC2-CUR on SH-SY5Y cell viability. The cells were treated for 24 h with different dilutions(1:1, 1:2 and 1:4) of empty nanocapsules (NC1 and NC2) and nanocapsules containing curcumin (NC1-CUR and NC2-CUR) followed by measurement of cell viability by MTT reduction assay (panel A) and cell toxicity by LDH release assay (panel B). Data after normalization to vehicle-treated cells (100%, MTT assay) or to total LDH release (TritonX100-treated cells, 100%) are presented as a mean±SEM from 3-8 independent experiments with five replicates. p < 0.05, p < 0.01 and **p<0.001 versus vehicle-treated cells; &&&p<0.001 NC1 versus NC1-CUR.
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。	Nat Biotechnol, 2015, 10.1038/nbt.3130 Leukemia, 2014, 28(3):680-9 PLoS Biol, 2013, 12(1):e1001758	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。	Neurochem Res, 2016, 41(12):3192-3205 The Winthrop McNair Research Bulletin, 2015, 1:17-22 Sci Rep, 2017, 7:43575	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。		Dose-response curves after treatment with resminostat alone or in combination with cisplatin. Head and neck squamous cell carcinoma cell lines SCC25, CAL27, and FaDu cells (A–C) were treated with increasing drug dosages of resminostat and cisplatin in a ratio 1.25:1. The human keratinocyte cell line HaCaT (D) was treated with increasing doses of resminostat (0-25 lM). Error bars indicate SEM.
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。		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。	J Antimicrob Chemother, 2014, 69(1):28-34 Hum Reprod, 2017, 32(1):76-87	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。	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)。	Nat Commun, 2014, 5:3479 Cell Rep, 2013, 5(6):1679-89 Int J Cancer, 2014, 134(11):2560-71	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 Biol Chem, 2016, 291(14):7386-95 J Cell Biochem, 2018, 119(4):3081-3090	B, 5×106 293T, HeLa, A549, and H1299 cells were seeded in 10-cm dishes on day 0 and treated with dimethyl sulfoxide, 10 μM TMP269, 10 μM LMK-235, or butyrate as indicated for 12 h. Cell lysates were collected for Western blotting analysis of Apaf-1 and β-actin.
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
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。
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。	Oxid Med Cell Longev, 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。	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。	J Biol Chem, 2016, 291(14):7386-95 Oncotarget, 2016, 7(25):37966-37978 Oncotarget, 2016, 7(39):63829-63838	Cells were exposed to HDAC Class II selective inhibitors LMK-235 or Nexturastat A (NA) at the indicated concentrations for 48 hrs and analyzed by Western blotting. Rom, romidepsin; Bel, belinostat, Pano, panobinostat; SAHA, suberoylanilide hydroxamic acid.
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	Cells were exposed to HDAC Class II selective inhibitors LMK-235 or Nexturastat A (NA) at the indicated concentrations for 48 hrs and analyzed by Western blotting. Rom, romidepsin; Bel, belinostat, Pano, panobinostat; SAHA, suberoylanilide hydroxamic acid.
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。	J Neuroimmunol, 2017, 305:154-161 Harvard University, 2014, Kimberly Stegmaier	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
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。	Cancer Lett, 2016, 379(1):134-42 Med Oncol, 2016, 33(5):50 Oncotarget, 2016, 7(34):54714-54722	U87 and U251 cells were treated with HDAC6 selective inhibitors and the cells were harvested for subsequent western blot analysis.
S7555	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。

研究领域

产品类型

HDAC

信号通路图

研究领域

特异性亚型抑制剂