59
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3206 |
NKL 22
Histone Deacetylase Inhibitor IV,PAOA |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
NKL 22 (Histone Deacetylase Inhibitor IV) 是一种有效的选择性组蛋白脱乙酰基酶(HDAC) 抑制剂,对 HDAC2/4/5/7/8 具有选择性,抑制HDAC1和HDAC3的IC50值分别为 199 和 69 nM。它可改善亨廷顿氏病转基因小鼠的疾病表型和转录异常。 | |||
T2157 |
M344
MS 344,Histone Deacetylase Inhibitor III |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
M344 (Histone Deacetylase Inhibitor III) 是一种组蛋白去乙酰化酶抑制剂,IC50为 100 nM。 | |||
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。 | |||
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。 | |||
T6481 |
Droxinostat
NS 41080,4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺 |
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Droxinostat (NS 41080) 是HDAC3、HDAC6和HDAC8抑制剂,IC50分别为16.9、2.47和1.46 μM。 | |||
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。 | |||
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。 | |||
T3358 |
ITSA-1
ITSA1 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
ITSA-1 是一种具有膜渗透性的HDAC 激活剂,抵消曲古抑菌素 A (TSA) 诱导的细胞周期停滞,组蛋白乙酰化和转录水平。 | |||
T3983 |
TMP195
TFMO 2,TMP 195 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
TMP195 (TFMO 2) 是一种选择性 IIa 类组蛋白脱乙酰酶 (HDAC) 抑制剂。对 HDAC4、HDAC5、HDAC7,HDAC9的 Ki 值分别为59、60、26,5 nM。 | |||
T8517 |
Belinostat
PX105684,PXD101,贝利司他,PXD-101 |
HDAC; Autophagy | Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Belinostat (PXD101) 是一种异羟肟酸型组蛋白脱乙酰酶抑制剂,具有抗肿瘤活性,在 HeLa 细胞提取物中的IC50为 27 nM。 | |||
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。 | |||
T21505 |
Suberoyl bis-hydroxamic acid
SBHA,软木肟酸,Suberohydroxamic acid |
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Suberoyl bis-hydroxamic acid (SBHA) 是一种竞争性且可透过细胞的HDAC1和HDAC3抑制剂,ID50值分别为 0.25 μM 和 0.30 μM。它使肿瘤细胞易于凋亡并促进线粒体凋亡途径,可研究甲状腺髓样癌。 | |||
T17028 |
Tefinostat
CHR-2845 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Tefinostat (CHR-2845) 是一种有效的单核细胞/巨噬细胞靶向组蛋白脱乙酰酶 (HDAC) 抑制剂。 Tefinostat 可被胞内酯酶人羧酸酯酶-1 (hCE-1) 裂解成活性酸 CHR-2847。Tefinostat 具有抗肿瘤活性,可用于研究白血病和晚期血液系统恶性肿瘤。 | |||
T6678 |
Splitomicin
1-Naphthalenepropanoic Acid,斯普利特麻一辛 |
Sirtuin; HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Splitomicin (1-Naphthalenepropanoic Acid) 是 NAD(+) 依赖性组蛋白去乙酰化酶 Sir2p 的特异性抑制剂,可抑制酵母提取物中 HDAC,IC50为 60 μM。 | |||
T16962 |
SW-100
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
SW-100 是一种选择性组蛋白去乙酰化酶 6 抑制剂,IC50为2.3 nM。它有提高的穿过血脑屏障的能力,相对于其他 HDAC 同工酶,还显示出对 HDAC6 的至少高 1000 倍的选择性。 | |||
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。 | |||
T77334 |
HDAC-IN-57
|
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-57 是一种具有口服活性的组蛋白脱乙酰酶 (HDAC) 泛抑制剂,对 HDAC1, HDAC2, HDAC6, HDAC8 具有抑制作用, IC50 值分别为 2.07 nM, 4.71 nM, 2.4 nM 和 107 nM。HDAC-IN-57 对 LSD1具有抑制作用, IC50 值为 1.34 μΜ。HDAC-IN-57 具有抗肿瘤活性,可诱导凋亡 (apoptosis)。 | |||
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。 | |||
T1852 |
Rac-Belinostat
NSC726630,PXD101,PX-105684 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rac-Belinostat (PX-105684) 是一种具有抗肿瘤活性的新型异羟肟酸型组蛋白脱乙酰酶 (HDAC) 抑制剂。 Belinostat 靶向 HDAC 酶,从而抑制肿瘤细胞增殖、诱导细胞凋亡、促进细胞分化和抑制血管生成。这种药物可以使耐药肿瘤细胞对其他抗肿瘤药物敏感,可能是通过一种涉及胸苷酸合酶下调的机制。 | |||
T27083 |
Crebinostat
|
Epigenetic Reader Domain; Histone Acetyltransferase; HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂,对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用, IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性,增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化,并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。 | |||
T3661 |
Citarinostat
ACY241,HDAC-IN-2 |
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂,具有抗肿瘤活性,对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。 | |||
T11543 | HDAC-IN-5 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor. | |||
T25630 | Largazole | ||
Largazole is a potent and selective histone deacetylase (HDAC) inhibitor and antiproliferative agent from Symploca. | |||
T34635 |
SHP-141
SHP141,SHP 141 |
||
SHP-141 is a topical preparation containing histone deacetylase (HDAC) inhibitor, with potential anti-tumor activity. | |||
T63747 | MC4355 | ||
MC4355 是 EZH2 和组蛋白脱乙酰酶 (HDAC) 的双重抑制剂。 | |||
T26731 | Azumamide E | ||
Azumamide E, a cyclotetrapeptide isolated from the sponge Mycale izuensis, is a carboxylic acid containing natural histone deacetylase (HDAC) inhibitor. | |||
T36686 |
Ac-Arg-Gly-Lys(Ac)-AMC
|
||
Ac-RGK(Ac)-AMC, fluorogenic substrate for assaying histone deacetylase (HDAC) activity in a two-step enzymatic reaction. The assay consists of the initial lysine deacetylation by HDAC followed by the release of the fluorescent group by trypsin. | |||
T62500 | WW437 | ||
WW437 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂,在体内外都表现出有效的抗乳腺癌活性。 | |||
T79543 |
J27644
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
J27644为一高效HDAC抑制剂,能缓解TGF-β所引发的肺纤维化现象。 | |||
T36110 |
L-Pyrohomoglutamic Acid
|
||
L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitors... | |||
T61630 | HDAC-IN-42 | ||
HDAC-IN-42 (compound 14f) is a highly potent and selective inhibitor of histone deacetylase (HDAC) enzymes, with IC50 values of 0.19 μM for HDAC1 and 4.98 μM for HDAC6. It exhibits remarkable anticancer properties and inhibits cell proliferation. Additionally, HDAC-IN-42 induces apoptosis and causes cell cycle arrest specifically at the G2/M phase [1]. | |||
T79541 |
HDAC-IN-61
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-61(compound 12k)为口服生效的HDAC抑制剂,表现出针对Bel-7402细胞线的明显抗癌活性,其IC50值仅为30 nM,适用于癌症研究领域。 | |||
TP1836 |
BMf-BH3
|
||
BMf-BH3 belongs to the Bcl-2 apoptosis mediator family. This peptide belongs to the Bcl-2 apoptosis mediator family. Bmf is a key player in histone deacetylase (HDAC) inhibition, which alters the balance between deacetylation and acetylation. | |||
T36102 |
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline
|
||
4-Chloro-6,7-bis(2-methoxyethoxy)quinazoline is a building block and synthetic intermediate.1,2,3,4,5It has been used as a precursor in the synthesis of receptor tyrosine kinase (RTK) inhibitors, dual RTK and histone deacetylase (HDAC) inhibitors, and anticancer compounds.1,2,3It is also a synthetic intermediate in the synthesis of EGFR inhibitors, including erlotinib , with antiproliferative activity.4,5 | |||
T78767 | HDAC-IN-60 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-60 (化合物21a) 作为一种高效HDAC抑制剂,能增强细胞内ROS生成,导致DNA损伤,阻碍G2/M期细胞周期,且触发线粒体相关凋亡途径促进细胞死亡。 | |||
T21749 |
4-iodo-SAHA
|
||
4-Iodo-SAHA (1k) 是一种具有口服活性的I 类和II 类histone deacetylase (HDAC)抑制剂,对 Skbr3、 HT29、 U937、 JA16 和 HL60细胞的EC50值分别为1.1、0.95、0.12、0.24、0.85和1.3 μM。4-Iodo-SAHA (1k) 可用于癌症的研究。 | |||
T71110 |
Nanatinostat TFA
|
||
Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor... | |||
T78766 | HDAC-IN-59 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
HDAC-IN-59(compound 13a)为一种高效HDAC抑制剂。该化合物能增强细胞内ROS生成,导致DNA损伤,阻止G2/M期细胞周期进程,并激活线粒体途径引发细胞凋亡。 | |||
T63791 |
HDAC-IN-36
|
||
HDAC-IN-36 是口服具有活力的 HDAC (组蛋白去乙酰化酶) 抑制剂,对 HDAC6 的 IC50 值为 11.68 nM)。HDAC-IN-36 能够诱导细胞凋亡 (apoptosis),自噬 (autophagy) 和抑制迁移。HDAC-IN-36 表现出抗肿瘤和抗转移效果,能够用于研究乳腺癌。 | |||
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。 | |||
T36105 |
coumarin-SAHA
coumarin-Suberoylanilide Hydroxamic Acid,coumarin-SAHA |
||
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. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino cap" group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm | |||
T74368 |
OKI-006
|
||
OKI-006 是一种有效的、具有口服活性的组蛋白脱乙酰酶 (HDAC) 抑制剂。OKI-006 是天然产物HDAC 抑制剂 largazole 的独特同系物。组蛋白去乙酰化酶 (HDAC) 在表观基因组调控中起关键作用,并且组蛋白乙酰化在许多人类癌症中失调。OKI-006 具有研究癌症疾病的潜力。 | |||
T74454 | JPS016 | ||
JPS016 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS016 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS016 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 | |||
T74453 | JPS014 | ||
JPS014, 基于苯甲酰胺的Von Hippel-Lindau (VHL) E3-连接酶蛋白水解靶向嵌合体 (PROTAC),有效降解I 类组蛋白脱乙酰酶 (HDAC)。它作为HDAC1/2的强效降解剂,与HCT116细胞中的总差异表达基因更大和增强的细胞凋亡 (apoptosis) 密切相关。 | |||
T77937 |
JPS014 TFA
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
JPS014 TFA是一种VHL E3连接酶蛋白水解靶向嵌合体(PROTAC),以苯甲酰胺为基础,专门降解I类组蛋白脱乙酰酶(HDAC)。作为一种高效的HDAC1/2降解剂,JPS014 TFA与HCT116细胞中广泛的基因表达差异及促进细胞凋亡(apoptosis)密切相关。 | |||
T74456 | JPS036 | ||
JPS036 是一种基于苯甲酰胺的Von Hippel-Lindau (VHL)E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。JPS036 降解 I 类组蛋白脱乙酰酶 (HDAC)。JPS036 是一种有效的 HDAC1/2 降解剂,与 HCT116 细胞中更大的总差异表达基因和增强的细胞凋亡 (apoptosis) 相关。 | |||
T77938 |
JPS016 TFA
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
JPS016 TFA是一种苯甲酰胺基Von Hippel-Lindau (VHL) E3连接酶蛋白水解靶向嵌合体(PROTAC)。该化合物能够降解I类组蛋白脱乙酰酶(HDAC),特别是有效地降解HDAC1/2。在HCT116细胞中,JPS016 TFA与大量差异基因表达增加及细胞凋亡(apoptosis)激活相关。 | |||
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
|
||
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... | |||
T70195 | NL-103 | ||
NL-103 is a novel dual-targeted inhibitor of histone deacetylases and hedgehog pathway, effectively overcomes vismodegib resistance conferred by Smo mutations. NL-103 comprises structural elements of Hh pathway inhibitor vismodegib, and histone deacetylase (HDAC) inhibitor vorinostat. NL-103 simultaneously and significantly inhibited both HDACs and Hh pathway. Importantly, NL-103 effectively overcame vismodegib resistance induced by Smoothened point mutations. Moreover, NL-103 significantly dow... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T14305 |
Apicidin
OSI 2040 |
Apoptosis; HDAC; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Apicidin (OSI 2040) 是组蛋白去乙酰化酶(HDAC)抑制剂,具有抗寄生虫活性和抗增殖活性。Apicidin 通过减少 APP/PS1 小鼠中的 Abeta 负荷来减轻记忆缺陷,抑制细胞生长增殖,诱导细胞凋亡和自噬,可用于研究白血病。 | |||
T70778 | Depudecin | ||
Depudecin is a polyketide obtained from the fungus Alternaria brassicicola and having a highly unusual structure of an 11-carbon chain containing two epoxides and six stereogenic centres. It is an inhibitor of histone deacetylase (HDAC) both in vivo and in vitro and also exhibits anti-angiogenic activity. |