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
- GC36690 Nampt-IN-3 Nampt-IN-3 (Compound 35) 同时抑制烟酰胺磷酸核糖转移酶 (NAMPT) 和 HDAC,IC50 分别为 31 nM 和 55 nM。Nampt-IN-3 有效诱导细胞凋亡 (apoptosis) 和自噬 (autophagy),最终导致细胞死亡。
- GC35893 Domatinostat Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
- GC35668 CG-200745 CG-200745 (CG-200745) 是一种具有口服活性的强效 pan-HDAC 抑制剂,其异羟肟酸部分可与催化袋底部的锌结合。 CG-200745 抑制组蛋白 H3 和微管蛋白的去乙酰化。 CG-200745 诱导 p53 的积累,促进 p53 依赖性反式激活,并增强 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。 CG-200745 增强了吉西他滨耐药细胞对吉西他滨和 5-氟尿嘧啶 (5-FU;) 的敏感性。 CG-200745 诱导细胞凋亡并具有抗肿瘤作用。
- GC35551 BRD 4354 ditrifluoroacetate BRD 4354 (ditrifluoroacetate) 是 HDAC5 和 HDAC9 抑制剂,其 IC50 值分别为 0.85,1.88 μM。
- GC41085 HDAC6 Inhibitor An inhibitor of HDAC6
- GC34629 J22352 J22352是一种具有类似靶向嵌合体蛋白水解(PROTAC)特性、高度选择性HDAC6抑制剂,其IC50值为4.7nM,J22352通过抑制胶质母细胞瘤自噬、诱发抗肿瘤免疫反应来促进HDAC6降解和诱导抗癌效果,并通过降低PD-L1的免疫抑制活性,使宿主抗肿瘤活性恢复。
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GC34458
ACY-1083
ACY-1083是一种可渗透脑的选择性HDAC6抑制剂,IC50为3nM,ACY-1083对HDAC6的选择性比其他类别的HDAC亚型高260倍。ACY-1083可有效逆转化疗引起的周围神经病变。
- GC34165 Corin Corin是组氨酸赖氨酸特异性去甲基化酶(LSD1)和组氨酸脱乙酰化酶(HDAC)的双重抑制剂,其对LSD1的Ki(inact)值为110nM,对HDAC1的IC50值为147nM。
- GC33395 HDAC-IN-5 HDAC-IN-5是组蛋白去乙酰化酶(HDAC)的一个抑制剂。
- GC33331 BRD 4354 BRD4354是HDAC5和HDAC9适度抑制剂,其IC50值分别为0.85,1.88μM。
- GC33317 HDAC6-IN-1 SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.
- GC33290 Remetinostat (SHP-141) Remetinostat (SHP-141) (SHP-141) 是一种基于异羟肟酸的组蛋白脱乙酰酶 (HDAC) 抑制剂,正在开发用于治疗皮肤 T 细胞淋巴瘤。
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GC33159
Givinostat hydrochloride (ITF-2357 hydrochloride)
HDAC inhibitor with anti-
inflammatory and antineoplastic activities -
GC33115
Pomiferin (NSC 5113)
Pomiferin (NSC 5113) (NSC 5113) 作为 HDAC 的潜在抑制剂,其 IC50 为 1.05 μM,并且还有效抑制 mTOR (IC50, 6.2 μM)。
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GC33050
Givinostat (ITF-2357)
HDAC inhibitor with anti-
inflammatory and antineoplastic activities - GC32964 NKL 22 A selective HDAC1/3 inhibitor
- GC32565 CRA-026440 CRA-026440 是一种有效的广谱 HDAC 抑制剂。
- GC31511 Sinapinic acid (Sinapic acid) A phenylpropanoid hydroxycinnamic acid with diverse biological activities
- GC30782 ACY-775 An HDAC6 inhibitor
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GC30763
Benzenebutyric acid (4-Phenylbutyric acid)
4-Phenylbutyric acid (4-PBA, Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and a key epigenetic inducer of anti-HCV hepatic hepcidin. 4-Phenylbutyric acid inhibits LPS-induced inflammation through regulating endoplasmic-reticulum (ER) stress and autophagy in acute lung injury models.
- GC30526 ACY-957 ACY-957是一种选择性的HDAC1和HDAC2抑制剂,对HDAC1/2/3的IC50值分别为7nM,18nM和1300nM,对HDAC4/5/6/7/8/9无作用。
- GC19406 TH34 TH34 是一种 HDAC6/8/10 抑制剂,IC50 分别为 4.6 μM、1.9 μM 和 7.7 μM,对 HDAC1/2/3 具有高选择性。
- GC19360 TMP195 A class IIa HDAC inhibitor
- GC19337 SR-4370 An HDAC3 inhibitor
- GC19190 HDAC-IN-4 An HDAC inhibitor
- GC19189 HDAC8-IN-1 An HDAC8 inhibitor
- GC19129 EDO-S101 An HDAC inhibitor and DNA alkylating agent
- GC19020 ACY-738 An HDAC6 inhibitor
- GC18402 GSK3117391 An HDAC inhibitor
- GC18206 WT161 A potent inhibitor of HDAC6
- GC11949 MI-192 A selective HDAC2/3 Inhibitor
- GC14016 Sulforaphane A class I and II HDAC inhibitor with anticancer activity
- GC14058 CBHA Inhibitor of histone deacetylases
- GC12334 HNHA HDAC inhibitor
- GC13925 Nullscript A negative control for scriptaid
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GC14597
ITSA-1 (ITSA1)
ITSA-1 是一种组蛋白去乙酰化酶(HDAC)激活剂,能够抑制HDAC抑制剂TSA对HDAC的抑制,但不抑制其他HDAC抑制剂。
- GC17472 Oxamflatin Inhibitor of histone deacetylases
- GC12822 BML-210(CAY10433) A potent, synthetic HDAC inhibitor
- GC14367 UF 010 A class I HDAC inhibitor
- GC12074 BG45 A selective HDAC3 inhibitor
- GC10417 ACY-241 An HDAC6 inhibitor
- GC16042 Chidamide An HDAC inhibitor
- GC11360 ORY-1001 An LSD1 inhibitor
- GC12484 BRD73954 A dual inhibitor of HDAC6 and HDAC8
- GC11574 HPOB A potent and selective inhibitor of HDAC6
- GC12971 CAY10603 An exceptionally potent inhibitor of HDAC6
- GC14439 Santacruzamate A (CAY10683) A histone deacetylase inhibitor
- GC12667 4SC-202 An HDAC1-3 and KDM1A inhibitor
- GC13764 Nexturastat A A potent, cell-permeable HDAC6 inhibitor
- GC15857 Sodium butyrate A short-chain fatty acid and HDAC inhibitor