T2025
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HDAC
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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。 |
T2078
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Apoptosis
PI3K
HDAC
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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。 |
T16936
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HDAC
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SS-208 是一种选择性的 HDAC6 抑制剂 (IC50 = 12 nM),具有抗肿瘤活性。 SS-208 显示出对其他 HDAC 亚型的选择性。 |
T73181
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HDAC
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HDAC-IN-51 是一种 HDAC 抑制剂。 |
T4477
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Apoptosis
HDAC
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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。 |
T79371
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Autophagy
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HDAC-IN-62(Compound 5),是一款针对HDAC6/8/11的HDAC抑制剂,IC50分别为0.78、1.0、1.2μM。该化合物通过诱导自噬(Autophagy)来抑制微胶质细胞的激活,进而抑制一氧化氮产生,显示出抗炎和抗抑郁的效果。此外,HDAC-IN-62还能抑制实验小鼠大脑中的微胶质细胞活化。 |
T16962
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HDAC
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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。 |
T6279L
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HDAC
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Givinostat hydrochloride (ITF2357 hydrochloride) 是一种 HDAC 抑制剂,对 HDAC1 和 HDAC3 的 IC50 分别为 198 和 157 nM。 Givinostat hydrochloride 具有抗炎、抗血管生成和抗肿瘤活性。 |
T78708
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JAK
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JAK/HDAC-IN-2 是一款高效的 JAK/HDAC 双靶点抑制剂,能在纳摩尔浓度范围内有效抑制 HDAC3/6 与 JAK1/2。此化合物不仅促进细胞凋亡,还能抑制组蛋白去乙酰化和 STAT3 磷酸化,对血液肿瘤和实体肿瘤细胞展现出了显著的抗增殖效果。 |
T36629
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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 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2].
Givinostat (ITF2357) at 10 mg/kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg/kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg/kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of Givinostat (ITF-2357) (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg[1].
[1]. Li S, et al. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. [2]. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. [3]. Leoni F, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol Med. 2005 Jan-Dec;11(1-12):1-15. |