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Home >> Signaling Pathways >> Chromatin/Epigenetics >> HDAC

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

  1. Cat.No. 产品名称 Information
  2. GC45717 Chlamydocin An HDAC inhibitor
  3. GC38412 Crotonoside A guanosine analog with diverse biological activities
  4. GA20605 Ac-Lys-AMC Ac-Lys-AMC（己酰胺），也称为 MAL，是组蛋白去乙酰化酶 HDAC 的荧光底物。
  5. GA20481 Ac-Arg-Gly-Lys(Ac)-AMC Ac-Arg-Gly-Lys(Ac)-AMC 是 HDAC 的底物。
  6. GC37845 Tucidinostat An HDAC inhibitor
  7. GC37753 Tefinostat Tefinostat (CHR-2845) 是一种单核细胞/巨噬细胞靶向的 HDAC 广谱抑制剂，通过细胞内酯酶人羧酸酯酶-1 (hCE-1) 切割成活性酸 CHR-2847。具有抗抗单核细胞系白血病活性。
  8. GC37643 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11)-specific inhibitor with IC50 of 0.83 μM. SIS17 inhibits the demyristoylation of HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
  9. GC36905 PI3K/HDAC-IN-1 PI3K/HDAC-IN-1 是一种有效的 (PI3K/HDAC) 双重抑制剂，高效抑制 PI3Kδ 和 HDAC1 的 IC50 值分别为 8.1 nM 和 1.4 nM。
  10. GC36691 Nanatinostat Nanatinostat (CHR-3996) 是一种有效的，有口服活性、I 类选择性的组蛋白去乙酰化酶 (HDAC) 抑制剂，IC50 值为 8 nM。
  11. 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。
  12. 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.
  13. 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。
  14. 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。
  15. GC45095 Tubastatin A (trifluoroacetate salt) A potent HDAC6 inhibitor
  16. GC44866 SAHA-d5 An internal standard for the quantification of SAHA
  17. GC44865 SAHA-BPyne A probe for HDAC activity
  18. GC43318 coumarin-SAHA A fluorescent probe for HDAC
  19. GC43201 CAY10722 A SIRT3 inhibitor
  20. GC43200 CAY10721 An inhibitor of SIRT3
  21. GC43147 CAY10398 A potent, cost-effective histone deacetylase inhibitor
  22. GC41495 HDAC3 Inhibitor An allosteric HDAC3 inhibitor
  23. GC41085 HDAC6 Inhibitor An inhibitor of HDAC6
  24. GC40923 BRD4884 A kinetically selective HDAC2 inhibitor
  25. GC40674 APHA Compound 8 A class I and II HDAC inhibitor
  26. 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。
  27. 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。
  28. 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。
  29. GC33395 HDAC-IN-5 HDAC-IN-5是组蛋白去乙酰化酶(HDAC)的一个抑制剂。
  30. GC33331 BRD 4354 BRD4354是HDAC5和HDAC9适度抑制剂，其IC50值分别为0.85，1.88μM。
  31. 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.
  32. 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。
  33. GC33159 Givinostat hydrochloride (ITF-2357 hydrochloride) HDAC inhibitor with anti-inflammatory and antineoplastic activities
  34. 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)。
  35. GC33050 Givinostat (ITF-2357) HDAC inhibitor with anti-inflammatory and antineoplastic activities
  36. GC32964 NKL 22 A selective HDAC1/3 inhibitor
  37. GC32565 CRA-026440 CRA-026440 是一种有效的广谱 HDAC 抑制剂。
  38. GC31511 Sinapinic acid (Sinapic acid) A phenylpropanoid hydroxycinnamic acid with diverse biological activities
  39. GC30782 ACY-775 An HDAC6 inhibitor
  40. 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.
  41. 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。
  42. 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。
  43. GC19360 TMP195 A class IIa HDAC inhibitor
  44. GC19337 SR-4370 An HDAC3 inhibitor
  45. GC19190 HDAC-IN-4 An HDAC inhibitor
  46. GC19189 HDAC8-IN-1 An HDAC8 inhibitor
  47. GC19129 EDO-S101 An HDAC inhibitor and DNA alkylating agent
  48. GC19020 ACY-738 An HDAC6 inhibitor
  49. GC18915 Trapoxin A Trapoxin A is a cyclotetrapeptide histone deacetylase (HDAC) inhibitor.
  50. GC18402 GSK3117391 An HDAC inhibitor
  51. GC18206 WT161 A potent inhibitor of HDAC6

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