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ROCK/HDAC-IN-1(Compound 10h)作为一种抑制剂,通过口服展现出对ROCK/HDAC的有效抑制。该化合物针对ROCK1/2和HDAC1/2/3/6/8表现出卓越的抑制效率,其IC50值分别为254.9 nM、58.18 nM和9.09、8.03、6.26、0.41、7.69 nM。此外,ROCK/HDAC-IN-1能激活DAMP,尤其增强了钙网蛋白(CRT)的外露和HMGB1的释放,显示其作为免疫性细胞死亡(ICD)诱导剂的潜力。对于乳腺癌细胞,特别是MDA-MB-231细胞,此抑制剂具有抗增殖活性,IC50值为0.37 μM,且能在不产生明显毒性的情况下,抑制肿瘤生长并激活T细胞。
ROCK/HDAC-IN-1(Compound 10h)作为一种抑制剂,通过口服展现出对ROCK/HDAC的有效抑制。该化合物针对ROCK1/2和HDAC1/2/3/6/8表现出卓越的抑制效率,其IC50值分别为254.9 nM、58.18 nM和9.09、8.03、6.26、0.41、7.69 nM。此外,ROCK/HDAC-IN-1能激活DAMP,尤其增强了钙网蛋白(CRT)的外露和HMGB1的释放,显示其作为免疫性细胞死亡(ICD)诱导剂的潜力。对于乳腺癌细胞,特别是MDA-MB-231细胞,此抑制剂具有抗增殖活性,IC50值为0.37 μM,且能在不产生明显毒性的情况下,抑制肿瘤生长并激活T细胞。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity. |
靶点活性 | HDAC3:6.26nM(IC50), HDAC2:8.03nM(IC50), HDAC8:7.69nM(IC50), HDAC6:0.41nM(IC50), ROCK2:58.18nM(IC50), ROCK1:254.9nM(IC50), HDAC1:9.09nM(IC50) |
分子量 | 386.47 |
分子式 | C19H22N4O3S |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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