histone deacetylase 9

CHDI-390576 是一种具有中枢神经系统渗透性、选择性和高效性的二苯甲酰异羟肟酸 IIa 类组蛋白脱乙酰酶(HDAC) 抑制剂，抑制 IIa 类 HDAC 4、HDAC 5、HDAC 7、HDAC 9 ，可用于研究癌症。

HDAC-IN-76 (compound 6i) 作为一种组蛋白去乙酰化酶 (HDAC) 抑制剂，对Pf3D7 (chloroquine 药敏品系) 和 PfDd2 (chloroquine 耐药品系) 的抗疟活性表现出色，IC50分别为30 nM 和 98 nM。该化合物在无性血期疟原虫中具有高效的抗疟作用，能选择性地抑制寄生虫生长。此外, HDAC-IN-76 对人类HDAC1和HDAC6的抑制作用强，IC50分别为7 nM 和 9 nM，且能同时抑制PfHDAC1。

9-hydroxy Stearic Acid 是一种羟基脂肪酸，是9-PAHSA 的活性代谢物。9-hydroxy Stearic Acid 是由9-PAHSA 通过肝脏和胰腺的羧基酯脂肪酶形成的。9-hydroxy Stearic Acid (5 μM)抑制HT-29结肠癌细胞裂解物中组蛋白去乙酰化酶1 (HDAC1)的表达。3 .当浓度为100 μM.1时，可抑制HT-29细胞的增殖，并诱导细胞周期阻滞于G0 g1期。

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

MDL-800，一种选择性SIRT6激活剂，通过将SIRT6的脱乙酰化活性提高多达22倍，有效促进了人类肝细胞癌(HCC)细胞中H3K9ac和H3K56ac水平的全面降低。SIRT6，作为一种肿瘤抑制因子，主要负责去乙酰化组蛋白H3 Nε-乙酰基赖氨酸9 (H3K9ac) 和56 (H3K56ac)，在多种癌症中常发现其表达量低下。此外，MDL-800通过SIRT6驱动的细胞周期阻滞，抑制了HCC细胞的增殖，并在肿瘤异种移植模型中显示出了效果。