Cat. No. | Product Name | Target | Signaling Pathways |
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T8508 |
HDAC-IN-3
GSK3117391A |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-3 (GSK3117391A)是组蛋白脱乙酰酶抑制剂,可治疗慢性炎症性疾病。 | |||
T24131 |
HDAC3-IN-T247
HDAC3 inhibitor T247,HDAC3 inhibitor-T247,HDAC3 IN T247,T247 |
Histone Demethylase; Antiviral | Chromatin/Epigenetic; Immunology/Inflammation |
HDAC3-IN-T247 (HDAC3 inhibitor T247) 是一种具有选择性和有效性的组蛋白去乙酰化酶 3(HDAC3) 抑制剂,具有抗癌和抗病毒活性。HDAC3-IN-T247 以剂量依赖的方式诱导人结肠癌 HCT116 细胞中 NF-κB 乙酰化。HDAC3-IN-T247 抑制癌细胞增殖。 | |||
T39567 |
HDAC1/2-IN-3
HDAC1/2-IN-3 |
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HDAC1/2-IN-3 is an inhibitor of both HDAC1 and HDAC2, demonstrating IC50 values of 0-5 nM and 5-10 nM, respectively. | |||
T78880 |
Tubulin/HDAC-IN-3
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Tubulin/HDAC-IN-3(compound 12a)为一种高效的tubulin/HDAC汇合型抑制剂,能显著破坏微管蛋白聚合(IC50: 5.4 μM),并对HDAC1/8展现强效抑制作用,IC50值分别为0.155 μM和0.177 μM。该化合物通过阻断细胞周期、诱导细胞凋亡(apoptosis)及抑制集落形成以施展其生物学效用。 | |||
T63529 |
HDAC/HSP90-IN-3
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HDAC/HSP90-IN-3 是选择性的、有效的真菌 Hsp90 (IC50: 0.83 μM) 和 HDAC (IC50: 0.91 μM) 双重抑制剂,对耐唑白色念珠菌表现出抗真菌作用。HDAC/HSP90-IN-3 对重要毒力因子表现出抑制作用,能够下调耐药基因ERG11和CDR1。 | |||
T78906 | CDK/HDAC-IN-3 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
CDK/HDAC-IN-3 是一种口服活性的 HDAC/CDK 双重抑制剂,对 CDK9、CDK12、CDK13 及 HDAC1、HDAC2、HDAC3 表现出有效且选择性的抑制,IC50 值分别为 98.32 nM、98.85 nM、100 nM、62.12 nM、93.28 nM 和 82.87 nM。该化合物主要用于急性髓性白血病 (AML) 的相关研究。 | |||
T72777 |
c-Met/HDAC-IN-3
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c-Met/HDAC-IN-3 是一种c-Met 和HDAC 抑制剂,对 c-Met 和HDAC1的IC50分别为 12.50 nM 和 26.97 nM。 c-Met/HDAC-IN-3 诱导凋亡(apoptosis),导致细胞周期阻滞在 G2/M 期。 | |||
T36575 |
HDAC3 Inhibitor
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HDAC3 inhibitor is an allosteric inhibitor of histone deacetylase 3 (HDAC3; Ki = 0.16 nM). It is selective for HDAC3 over HDAC1 and HDAC2 (IC50s = 0.95, 11.81, and 95.45 nM, respectively, using recombinant HDACs). In addition, it is selective for acute myeloid, monocytic, and lymphoblastic leukemia cell lines (EC50s = 36.37, 76.64, and 151.7 nM, respectively) over chronic myeloid, acute promyelocytic, and acute lymphoblastic cells (EC50s = 2,160, >10,000, and >10,000 nM, respectively). | |||
T24132 |
HDAC3-IN-T326
HDAC3 inhibitor-T326,T326,HDAC3 IN T326,HDAC3 inhibitor T326,HDAC3INT326 |
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HDAC3-IN-T326 is a potent and selective HDAC3 inhibitor that acts by increasing NF-κB acetylation and activating HIV gene expression in latent HIV-infected cells. | |||
T62786 | HDAC1-IN-3 | ||
HDAC1-IN-3 是一种 Pf HDAC1 的有效抑制剂。HDAC1-IN-3 在野生型和耐多药寄生虫菌株中均具有抗疟作用。HDAC1-IN-3 对寄生虫所有生命周期表现出明显的体内杀伤效果。 | |||
T61139 | HDAC6-IN-3 | ||
HDAC6-IN-3 (Compound 14) is a potent anti-prostate cancer agent that acts as an orally active inhibitor of HDAC6. It has IC50 values ranging from 0.02-1.54 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10. Additionally, HDAC6-IN-3 also demonstrates effective inhibition of MAO-A (IC50 = 0.79 μM) and LSD1 [1]. | |||
T79714 |
HDAC3-IN-2
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC3-IN-2 (compound 4i) 是一种具有纳摩尔级效力的吡嗪酰肼基HDAC3抑制剂,IC50值为14 nM,针对三阴性乳腺癌细胞表现出高效抑制作用。该化合物在细胞内毒性测定中显示,对4T1细胞株的IC50为0.55 μM,对MDA-MB-231细胞株的IC50为0.74 μM。HDAC3-IN-2通过增加乙酰化水平(如H3K9、H3K27和H4K12),促进细胞凋亡(涉及caspase-3、caspase-7和细胞色素c的水平提升),并抑制细胞增殖相关蛋白(如Bcl-2、CD44、EGFR和Ki-67)的表达,从而在荷瘤小鼠模型中表现出显著的体内抗肿瘤作用。 | |||
T61858 | HDAC8-IN-3 | ||
HDAC8-IN-3 (compound P19) is a highly potent inhibitor of HDAC8, displaying an IC50 value of 9.3 μM and producing thermal stabilization. Moreover, HDAC8-IN-3 exhibits cytotoxicity and induces apoptosis specifically in leukemic cell lines [1]. | |||
T74003 |
HDAC3/6-IN-2
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HDAC3/6-IN-2 (化合物 15) 是一种高效的HDAC6和HDAC3抑制剂,IC50值分别为0.368 μM和0.635 μM。此化合物不仅具备抗肿瘤活性,能够诱导癌细胞凋亡,同时通过降低HDAC6和HDAC3水平,与H3乙酰化和α-微管蛋白的上调有关。 | |||
T79713 | JMJD3/HDAC-IN-1 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
JMJD3/HDAC-IN-1 (compound A5b) 是靶向 JMJD3 和 HDAC1(IC50=16 nM)的双重抑制剂。它能够促进 H3K27 高甲基化和 H3K9 高乙酰化,并通过裂解 caspase-7 和 PARP 导致细胞凋亡。此外,JMJD3/HDAC-IN-1 对抑制癌细胞克隆形成、迁移和侵袭也表现出有效性。 | |||
T75018 | HDAC6 degrader-3 | ||
HDAC6degrader-3 是一种有效的选择性 HDAC6降解剂,通过三元复合物形成和泛素-蛋白酶体途径,IC50值为 19.4 nM。HDAC6degrader-3 对 HDAC6和 HDAC1的 IC50值分别为 4.54 nM 和 0.647 μM。HDAC6degrader-3 引起 α-微管蛋白的强烈高度乙酰化。 | |||
T62912 |
PI3K/HDAC-IN-2
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PI3K/HDAC-IN-2 是一种有效的 PI3K/HDAC 双重抑制剂,能够作用于 PI3Kα (IC50: 226 nM)、PI3Kβ (IC50: 279 nM)、PI3Kγ (IC50: 467 nM)、PI3Kδ (IC50: 29 nM)、HDAC1 (IC50: 1.3 nM)、HDAC2 (IC50: 3.4 nM)、HDC4 (IC50: 973 nM)、HDAC6 (IC50: 17 nM)、HDAC8 (IC50: 12 nM)。PI3K/HDAC-IN-2 具有 PI3Kδ 和 I 类和 IIb 类 HDAC 选择性,并表现出显着的抗癌作用。 | |||
T79710 |
PI3Kα/HDAC6-IN-1
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HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
PI3Kα/HDAC6-IN-1(化合物21j)是一种针对PI3Kα/HDAC6的双重抑制剂,其IC50值分别为2.9 nM和26 nM。该化合物还能抑制AKT(Ser473)的磷酸化,诱导α-微管蛋白的积累,并促进其乙酰化,但对乙酰化组蛋白H3和H4无显著影响。在L-363细胞系中,PI3Kα/HDAC6-IN-1显示了高效的抑制活性(IC50=0.17 μM),表现出良好的抗癌潜力。 | |||
T2025 |
HDAC-IN-7
HBI-8000,西达本胺杂质,CS055,Chidamide impurity |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-7 (HBI-8000) 是 Chidamide 的一种杂质。Chidamide 是一种可口服的 HDAC 酶 I 类 HDAC1/2/3 和 IIb 类 HDAC10 抑制剂。 | |||
T2078 |
Fimepinostat
CUDC-907,PI3K/HDAC Inhibitor,CUDC 907 |
Apoptosis; PI3K; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Fimepinostat (CUDC 907) 是一种 I 型PI3K 及 I 和 II 型HDAC 酶抑制剂,作用于 PI3Kα/PI3Kβ/PI3Kδ 和 HDAC1/HDAC2/HDAC3/HDAC10 ,IC50分别为 19/54/39 nM 和 1.7/5.0/1.8/2.8 nM。 | |||
T9041 |
AES-350
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Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
AES-350 是一种具有口服活性HDAC6抑制剂,IC50和Ki 分别为 0.0244 μM 和 0.035 μM。它对 HDAC3、8 和 11 的 IC50值分别为 0.187、0.245和大于1μM。它通过抑制 HDAC 诱导 AML 细胞凋亡,可研究急性髓系白血病。 | |||
T6865 |
Quisinostat dihydrochloride
Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) 是一种有口服活性,高效的 pan-HDAC 抑制剂,具有广泛的抗肿瘤活性。它对 HDAC1、HDAC2、HDAC4、HDAC10和HDAC11 的IC50值分别为 0.11 nM、0.33 nM、0.64 nM、0.46 nM 和 0.37 nM。 | |||
T62545 |
HDAC-IN-43
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HDAC-IN-43 是一种强效的 HDAC 1/3/6 抑制剂,对 HDAC 1、HDAC 3 和 HDAC 6 的 IC50 值分别为 82 nM、45 nM 和 24 nM。HDAC-IN-43 是一种弱的 PI3K/mTOR 抑制剂,对 PI3K 和 mTOR 的 IC50 值分别为 3.6 μM 和 3.7 μM。HDAC-IN-43 具有广谱的抗增殖效果。 | |||
T62920 |
HDAC-IN-38
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HDAC-IN-38 是一种 HDAC 的有效抑制剂。HDAC-IN-38 对 HDAC1、2、3、5、6 和 8 具有类似的微摩尔抑制作用,也可以提高组蛋白乙酰化水平 (H3K14 或 H4K5)。HDAC-IN-38 能够提高脑血流量 (CBF),减轻认知障碍,改善海马萎缩。 | |||
T13792 | Nampt-IN-3 | Others | Others |
Nampt-IN-3 simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC (IC50s of 31 nM and 55 nM, respectively). | |||
T61209 | HDAC-IN-27 | ||
HDAC-IN-27 是一种有效的口服活性HDACI 类选择性抑制剂,对 HDAC1-3 的 IC50值范围为 0.43 至 3.01 nM。抗急性髓系白血病 (AML) 活性。 | |||
T62072 | HDAC-IN-47 | ||
HDAC-IN-47 是一种口服具有活力的组蛋白去乙酰化酶 (HDAC) 的抑制剂,对 HDAC1、HDAC2、HDAC3、HDAC6、HDAC8 的 IC50 值分别为 19.75 nM、57.8 nM、40.27 nM、5.63 nM、302.73 nM。HDAC-IN-47 可以将细胞周期阻滞在 G2/M 期,抑制细胞自噬,能够利用 Bax/Bcl-2 和 caspase-3 通路诱导凋亡,在体内具有抗癌活性。 | |||
T35765 |
SAHA-BPyne
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Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. SAHA-BPyne is a SAHA derivative with a benzophenone crosslinker and an alkyne tag intended to be used for profiling HDAC activities in proteomes and live cells. Such terminal alkyne groups can be used in linking reactions, known as click chemistry, characterized by high dependability and specificity of azi... | |||
T74783 | HDAC-IN-53 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-53是一种口服活性的选择性HDAC1-3抑制剂,其IC50分别为47 nM、125 nM和450 nM。该化合物不针对II类HDAC(HDAC4、5、6、7、9;IC50>10 μM)展现抑制作用。HDAC-IN-53能够诱导caspase依赖的细胞凋亡并在裸鼠中显著抑制人肿瘤异种移植物生长,同时抑制携带MC38结肠癌的免疫活性小鼠的肿瘤发展。 | |||
T21898 |
MI-192
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MI-192 是一种选择性 HDAC2和 HDAC3抑制剂,IC50分别为 30 nM 和 16 nM。MI-192 比其他 HDAC 异构体对 HDAC2/3 具有更高选择性。MI-192 诱导髓系白血病细胞凋亡 (apoptosis)。抗癌和神经保护活性。 | |||
T79683 |
HDAC/CD13-IN-1
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Others | Others |
HDAC/CD13-IN-1 (Compound 12) 作为HDAC/CD13抑制剂, 对hCD13的IC50为0.34 μM, 猪CD13为0.53 μM, 对HDAC1/2/3的IC50分别为0.03、0.06、0.02 μM。此化合物有效抑制MV4-11、K562、Jeko-1 和 HL60细胞增殖, IC50范围为0.25-2.04 μM,并诱导癌细胞凋亡。同时表现出抗转移和抗侵袭的特性。 | |||
T70962 | MHY219 | ||
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. M... | |||
T35822 |
CAY10722
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CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patie... | |||
T61753 |
MPT0G211 mesylate
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MPT0G211 mesylate is a powerful and selective HDAC6 inhibitor (IC50 = 0.291 nM), with high oral bioavailability. It exhibits remarkable selectivity for HDAC6 over other HDAC isoforms (>1000-fold selectivity). Additionally, MPT0G211 mesylate can effectively cross the blood-brain barrier. In preclinical studies using an Alzheimer's disease model, MPT0G211 mesylate has shown promising results in reducing tau phosphorylation and cognitive deficits. Furthermore, this compound exhibits anti-metastatic... | |||
T36629 | Givinostat | ||
Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1... |