HDAC1-IN-5 是一种有效的HDAC1抑制剂，对 HDAC1 和HDAC6 的IC50分别为 15 nM 和 20 nM。HDAC1-IN-5 可增强癌细胞中组蛋白 H3 和 α-微管蛋白 (α-tubulin) 的乙酰化，促进caspase 3的活化，从而诱导细胞凋亡 (apoptosis)。HDAC1-IN-5 通过与 DNA 结合诱导染色质损伤。HDAC1-IN-5 在异种移植瘤小鼠中表现出较强的肿瘤生长抑制活性。
| 生物活性 | HDAC1-IN-5 is a potentHDAC1inhibitor withIC50values of 15 nM and 20 nM forHDAC1andHDAC6, respectively. HDAC1-IN-5 can enhance the acetylation ofhistone H3andα-tubulin, as well as promote the activation ofcaspase 3incancercells, thereby inducingapoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice[1]. |
| IC50& Target[1] | HDAC1 15 nM (IC50) | HDAC6 20 nM (IC50) |
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体外研究
(In Vitro) | HDAC1-IN-5 (compound 4j) (0-50 μM; 48 h) exhibits strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL[1].
HDAC1-IN-5 (0.16-1.5 μM; 48 h) induces apoptosis in a dose-dependent manner[1].
HDAC1-IN-5 (0.17-1.5 μM; 24 h or 48 h) induces downregulation of SPT16 and SSRP-1, induces the cleavage of caspase-3, and increases the expression of Acetyl-Histone H3 and Acetyl-α-tubulin[1].
Cell Proliferation Assay[1] | Cell Line: | HCT116, HeLa, HepG2, MC38, K562 and HEL | | Concentration: | 0-50 μM | | Incubation Time: | 48 h | | Result: | Showed strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL with IC50s of 0.47 μM, 0.78 μM, 1.4 μM, 0.43 μM, 0.91 μM and 0.28 μM, respectively. |
Apoptosis Analysis[1] | Cell Line: | HCT116 | | Concentration: | 0.16 μM, 0.5 μM and 1.5 μM | | Incubation Time: | 48 h | | Result: | Induced apoptosis in a dose-dependent manner, and induced 38.5% at the concentration of 1.5 μM (both early and late apoptotic cells). |
Western Blot Analysis[1] | Cell Line: | HCT116 and MC38 | | Concentration: | 0.17 μM, 0.5 μM and 1.5 μM | | Incubation Time: | 24 h or 48 h | | Result: | Induced downregulation of SPT16 and SSRP-1 in HCT116.
Induced the cleavage of caspase-3 in HCT116 and MC38.
Increased the expression of HDAC1, 2, 6 substrate Acetyl-Histone H3 and Acetyl-α-tubulin with a dose-dependent manner. |
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体内研究
(In Vivo) | HDAC1-IN-5 (50 and 100 mg/kg; IP; every two days; for 16 days) significantly decreases the tumor volume and weight in MC38 xenograft mice[1].
| Animal Model: | C57BL/6 mice (6-10 weeks; 2×106MC38 cells were injected subcutaneously into the right flank regions)[1] | | Dosage: | 50 and 100 mg/kg | | Administration: | IP; every two days; for 16 days | | Result: | Significantly decreased the tumor volume and weight with tumor growth inhibition (TGI) of 66% at 50 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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