| Bioactivity | HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer[1]. |
| Invitro | HDAC-IN-53 (化合物 19h) 对一组癌细胞系具有良好的抗增殖活性，例如 MC38 (IC50=0.66 μM)、HCT116 细胞 (IC50=0.56 μM)[1]。 HDAC-IN-53 (0.1-1 μM; 24 小时) 在 MC38 细胞中引起 G0/G1 细胞周期停滞，在 HCT116 细胞中诱导 G2/M 细胞周期停滞[1]。 HDAC-IN-53 (0.1-1 μM; 24 小时) 以剂量依赖的方式上调 cleaved caspase-3 和 cleaved PARP 的表达[1]。 Cell Cycle Analysis[1] Cell Line: |
| In Vivo | HDAC-IN-53 (60 或 120 mg/kg; 灌胃给药; 每日一次; 持续 15 天) 通过直接肿瘤生长抑制和间接免疫细胞介导的抗肿瘤作用发挥抗肿瘤活性[1]。 Pharmacokinetic Parameters of HDAC-IN-53 in Mice[1]. |
| Name | HDAC-IN-53 |
| Formula | C23H20ClN7O2 |
| Molar Mass | 461.90 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Nan Sun, et al. Design and Synthesis of Triazole-Containing HDAC Inhibitors That Induce Antitumor Effects and Immune Response. J Med Chem. 2023 Apr 13;66(7):4802-4826. |