40
2
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。 | |||
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。 | |||
T36575 |
HDAC3 Inhibitor
|
||
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). | |||
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。 | |||
T24132 |
HDAC3-IN-T326
HDAC3 inhibitor-T326,T326,HDAC3 IN T326,HDAC3 inhibitor T326,HDAC3INT326 |
||
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. | |||
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。 | |||
T3193 |
Pimelic diphenylamide 106
Histone Deacetylase Inhibitor VII,TC-H 106,RGFA-8 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Pimelic diphenylamide 106 (RGFA-8) 是一种缓慢和紧密结合的I 类HDAC 抑制剂,对HDAC1、 2和3的IC50值分别150、760和370 nM。 | |||
T2512 |
Mocetinostat
MGCD0103,MG0103 |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Mocetinostat (MG0103) 是一种可口服和同种型选择性的HDAC 抑制剂,抑制HDAC1,HDAC2,HDAC3和HDAC11的IC50分别为0.15,0.29,1.66 和 0.59 μM。 | |||
T73515 |
MC2590
|
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
MC2590 是一种具有有效性和选择性的组蛋白脱乙酰酶 (HDAC) 抑制剂 ,抑制 HDAC1-3、-6、-8 和 -10 的活性,诱导细胞周期停滞,促进细胞凋亡。 | |||
T1888 |
Tacedinaline
Acetyldinaline,N-acetyldinaline,PD-123654,CI994,Goe-5549 |
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Tacedinaline (CI994) 是一种组蛋白脱乙酰酶抑制剂,抑制重组 HDAC 1, 2 和 3 的IC50值分别为 0.9,0.9,1.2 μM。 | |||
T10245 |
ACY-957
HDAC Inhibitor C001 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
ACY-957 (HDAC Inhibitor C001) 是一种具有口服活性,选择性的 HDAC1 和 HDAC2 抑制剂,对 HDAC1/2/3 的 IC50 值分别为 7 nM,18 nM 和 1300 nM,对 HDAC4/5/6/7/8/9 无作用。 | |||
T0431 |
Abexinostat
CRA 24781,阿贝司他,PCI24781,PCI-24781,PCI 24781,CRA 024781 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Abexinostat (PCI24781) 是一种新型的泛HDAC 抑制剂,对HDAC1的Ki 值为7 nM。 | |||
T4481 |
Tucidinostat
HBI-8000,Chidamide,西达本胺,CS 055 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Tucidinostat (Chidamide) 是一种可口服的 HDAC I 类 HDAC1/2/3和第 IIb 类 HDAC10的抑制剂,IC50值分别为 95、160、67 和 78 nM。 | |||
T4477 |
Domatinostat tosylate
4SC-202 tosylate,4SC-202 |
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Domatinostat tosylate (4SC-202) 是一种 I 型 HDAC 抑制剂,能够抑制 HDAC1、HDAC2和 HDAC3 的活性,IC50值分别为 1.20 μM、1.12 μM 和 0.57 μM。它也抑制组蛋白赖氨酸特异性脱甲基酶1 的活性。 | |||
T1583 |
Vorinostat
MK0683,伏立诺他,suberoylanilide hydroxamic acid,SAHA |
Apoptosis; Mitophagy; Virus Protease; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology |
Vorinostat (SAHA) 是一种泛的组蛋白脱乙酰酶 (HDAC) 抑制剂 (IC50=10 nM),对 HDAC1/2/3/6/7/11 均有抑制活性。 Vorinostat 具有抗肿瘤活性,可以诱导细胞分化,阻滞细胞周期,诱导细胞凋亡。 | |||
T9041 |
AES-350
|
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。 | |||
T6055 |
Quisinostat
奎诺司他,JNJ-26481585 |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Quisinostat (JNJ-26481585) 是一种高效的,具有口服活性的 pan-HDAC 抑制剂,对 HDAC1、HDAC2、HDAC4、HDAC10、HDAC11 作用的 IC50值范围为 0.11-0.64 nM。它在成神经细胞瘤中能诱导自噬,具有广泛的抗肿瘤活性。 | |||
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。 | |||
T3205 |
UF010
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
UF010 是一种有效的选择性 HADC 抑制剂,对 HDAC 1、2、3 和 8 的 IC50 分别为 0.5 μM、0.1 μM、0.06 μM 和 1.5 μM。它比作用于其他HDACs 选择性高6倍多。 | |||
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
|
||
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。 | |||
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。 | |||
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。 | |||
T62123 | FNDR-20123 | ||
FNDR-20123 是一个安全的、有效的抗疟疾 HDAC 抑制剂,能够作用于疟原虫 HDAC (IC50: 31 nM) 和人类 HDAC (IC50: 3 nM)。FNDR-20123 对恶性疟原虫 (Plasmodium falciparum) 无性期和性血期 (雄性配子体) 都显示出抗疟疾效果,其 IC50 值分别为 41 nM 和 190 nM。FNDR-20123 能够抑制 HDAC1 (IC50: 25 nM)、HDAC2 (IC50: 29 nM)、HDAC3 (IC50: 2 nM)、HDAC6 (IC50: 11 nM)、HDAC8 (IC50: 282 nM),而且在纳摩尔浓度下可以抑制 III 类 HDAC 亚型。 | |||
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... | |||
T61572 |
FNDR-20123 free base
|
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FNDR-20123 free base 是一种有效、安全、首创的抗疟疾HDAC 抑制剂,对疟原虫和人类 HDAC 的IC50分别为 31 nM 和 3 nM。FNDR-20123 free base 对恶性疟原虫 (Plasmodium falciparum) 无性期 (IC50=41 nM) 和性血期 (雄性配子体 IC50=190 nM) 具有抗疟疾活性。FNDR-20123 free base 抑制 HDAC1,HDAC2,HDAC3,HDAC6,HDAC8 的 IC50分别为 25,29,2,11,282 nM,并在纳摩尔浓度下抑制 III 类 HDAC 亚型。 | |||
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。 | |||
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。 | |||
T35821 |
CAY10721
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CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM). Upregulation of SIRT3 transcription is associated with oral squamous cell carcinoma (OSCC) and breast cancer with lymph node involvement, while SIRT3 down-regulation inhibits the growth of OSCC cells and sensitizes them to radiation and chemotherapy. | |||
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。 | |||
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。 | |||
T70962 |
MHY219
|
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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... | |||
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。 | |||
T79683 |
HDAC/CD13-IN-1
|
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。 | |||
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... | |||
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... | |||
T60511 |
Theophylline sodium glycinate
|
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Theophylline (1,3-Dimethylxanthine) sodium glycinate 是一种有效的磷酸二酯酶 (PDE) 抑制剂,可抑制 PDE3 活性以松弛气道平滑肌。Theophylline sodium glycinate 可用于研究哮喘和慢性阻塞性肺疾病 (COPD) 。Theophylline sodium glycinate 也是一种腺苷受体拮抗剂和组蛋白脱乙酰酶 (HDAC) 激活剂。 Theophylline sodium glycinate 通过增加 IL-10 和抑制 NF-κB 的核输入而具有抗炎活性。Theophyllin sodium glycinate 可诱导细胞凋亡。 | |||
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... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T6S0033 |
Crotonoside
巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE |
Others; FLT; HDAC | Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors |
Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。 它抑制 FLT3 和 HDAC3/6,有治疗急性髓性白血病 (AML)的研究潜力。 | |||
TN4220 |
Homobutein
3-O-Methylbutein,2',4,4'-Trihydroxy-3-methoxychalcone |
Antioxidant; NF-κB; HDAC; Parasite; Immunology/Inflammation related | Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; Microbiology/Virology; NF-κB; oxidation-reduction |
Homobutein (3-O-Methylbutein) 是 HDAC 和 NF-κB 的双重抑制剂,IC50 分别为 190 和 38 μM。 Homobutein 是一种铁螯合剂,具有抗癌、抗炎、抗寄生虫和抗氧化活性。 |