HDAC(组蛋白去乙酰化酶)

Histone deacetylases (HDACs), known for their ability to target histones as well as more than 50 non-histone proteins, are classified into three major classes according to their homology to yeast proteins, including class I (HDAC1, HDAC2, HDAC3 and HDAC8), class II (HDAC4, HDAC5, HDAC7 and HDAC9) and class IV (HDAC11). HDAC inhibitors, a large group of compounds that is able to induce the accumulation of acetylated histones as well as non-histone proteins, are divided into several structural classes including hydroxamates, cyclic peptides, aliphatic acids and benzamides. HDAC inhibitors have been investigated for their efficacy as anticancer agents in the treatment of a wild range of cancers.

Products for HDAC

Cat.No. 产品名称 Information
GC15114 LAQ824 (NVP-LAQ824,Dacinostat)
达诺司他,LAQ-824, NVP-LAQ 824
A hydroxamate-based HDAC inhibitor
GC13408 CI994 (Tacedinaline)
4-乙酰氨基-N-(2'-氨基苯基)-苯甲酰胺,N-acetyldinaline; CI-994; Goe-5549
An inhibitor of HDAC1, -2, and -3
GC10839 Tubastatin A Tubastatin A 是一种有效的选择性 HDAC6 抑制剂，IC₅₀ 值为 15 nM。并且Tubastatin A也是一种新型GPX4抑制剂，Tubastatin A 直接与 GPX4 结合，诱导乳腺癌细胞铁死亡。
GC13706 Droxinostat
4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺,NS 41080
An inhibitor of HDAC3, HDAC6, and HDAC8
GC15794 Valproic acid sodium salt (Sodium valproate)
丙戊酸钠; Sodium Valproate sodium
Valproic acid sodium salt (Sodium valproate)（VPA）是一种具有口服活性的组蛋白脱乙酰酶（HDAC）抑制剂，IC₅₀值为1.5mM，抑制HDAC1的IC₅₀值为400μM，同时可诱导HDAC2的降解。
GC14682 PCI-24781 (CRA-024781)
阿贝司他; 艾贝司他; CRA 024781; PCI-24781
An HDAC inhibitor
GC12115 CUDC-907
CUDC-907
CUDC 是一种口服生物可利用的小分子 PI3K 和 HDAC 双重抑制剂，作用于 PI3K α 和 HDAC1 / 2 / 3 / 10，IC50 分别为 19 nm 和 1.7 nm / 5 nm / 1.8 nm / 2.8 nm .在 WSU DLCL2 细胞中评估了双功能 HDAC 和 PI3K 抑制剂 CUDC-907 的抗肿瘤活性。
GC15962 Belinostat (PXD101)
贝利司他(PXD101),PXD-101, PXD 101, PX105684, PX-105684
Belinostat (PXD101) 是 HeLa 细胞提取物中组蛋白脱乙酰酶 (HDAC) 活性的新型异羟肟酸型抑制剂，IC50 为 27 nM 。
GC16734 Pracinostat (SB939)
(2E)-3-[2-丁基-1-[2-(二乙基氨基)乙基]-1H-苯并咪唑-5-基]-N-羟基丙烯酰胺,SB-939, SB 939

A pan-HDAC inhibitor
GC15965 MC1568
MC 1568, MC-1568
A selective class IIa HDAC inhibitor
GC15879 Resminostat (RAS2410)
RAS2410; 4SC-201
Resminostat (RAS2410) (RAS2410; 4SC-201) 是一种有效的 HDAC1、HDAC3 和 HDAC6 抑制剂，平均 IC50 值分别为 42.5、50.1、71.8 nM，对 HDAC8 的活性较低，IC50 为 877 nM .
GC15002 Sodium Phenylbutyrate
苯丁酸钠; 4-PBA sodium; 4-Phenylbutyric acid sodium; Benzenebutyric acid sodium
A chemical chaperone
GC15315 Scriptaid
Scriptide; GCK1026
HDAC inhibitor
GC17836 ITF2357 (Givinostat)
N-[4-[(羟基氨基)羰基]苯基]氨基甲酸[6-[(二乙基氨基)甲基]-2-萘基]甲酯盐酸盐水合物,ITF-2357, Givinostat (hydrochloride monohydrate)

HDAC inhibitor with anti-inflammatory and antineoplastic activities
GC16008 CUDC-101
7-[[4-(3-乙炔基苯基氨基)-7-甲氧基喹唑啉-6-基]氧基]-N-羟基庚酰胺,CUDC101, CUDC 101
A multi-target inhibitor of HDACs, EGFR, and HER2
GC18008 PCI-34051
N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺,PCI34051, PCI 34051
A potent, selective HDAC8 inhibitor
GC15476 JNJ-26481585
JNJ26481585
A pan-HDAC inhibitor
GC13055 Mocetinostat (MGCD0103, MG0103)
N-(2-氨基苯基)-4-([[4-(吡啶-3-基)嘧啶-2-基]氨基]甲基)苯甲酰胺,MGCD-0103
An orally available HDAC inhibitor
GC17390 Vorinostat (SAHA, MK0683)
伏立诺他; SAHA; Suberoylanilide hydroxamic acid

An HDAC inhibitor
GC14998 Rocilinostat (ACY-1215)
Ricolinostat
A selective inhibitor of HDAC6
GN10357 Parthenolide
小白菊内酯; (-)-Parthenolide
Parthenolide是一种NF-κB抑制剂，对Eca109、KYSE-510、SiHa和MCF-7细胞48h的IC₅₀值分别约为10.3、13.3、8.42和9.54µM。
GC12961 Apicidin
OSI 2040

A cell-permeable HDAC inhibitor
GC11334 Romidepsin (FK228, depsipeptide)
罗米地辛; FK 228; FR 901228; NSC 630176
A class I HDAC inhibitor
GC15526 Trichostatin A (TSA)
曲古抑菌素A; TSA
Trichostatin A (TSA) 是一种有效的组蛋白脱乙酰酶 (HDAC) 抑制剂和抗真菌抗生素，对 HDAC 的 IC50 值为 1.8 nM，具有抑制细胞生长和诱导细胞分化。
GC12257 Panobinostat (LBH589)
帕比司他; LBH589; NVP-LBH589
A pan-HDAC inhibitor
GC11625 Entinostat (MS-275,SNDX-275)
恩替诺特; MS-275; SNDX-275
A histone deacetylase inhibitor