HDAC6-IN-4 (C10) 是一种有效的、具有口服活性的、高选择性的HDAC6抑制剂， IC50值为23 nM。HDAC6-IN-4 诱导肿瘤细胞凋亡 (apoptosis)，具有显著的抗肿瘤作用，且无明显毒性。
| 生物活性 | HDAC6-IN-4 (C10) is a potent, orally active and highly selectiveHDAC6inhibitor with anIC50value of 23 nM. HDAC6-IN-4 inducescancercellsapoptosisand shows significant antitumor efficacy, without obvious toxicity[1]. |
| IC50& Target | HDAC6 23 nM (IC50) | HDAC3 46 nM (IC50) | HDAC2 172 nM (IC50) | HDAC8 2175 nM (IC50) | HDAC1 3604 nM (IC50) |
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体外研究
(In Vitro) | HDAC6-IN-4 (C10) (0-50 μM, 72 h) shows strong antiproliferative activity against different cancer cells with low cytotoxicity[1].
HDAC6-IN-4 (0-6 μM, 24 h) exhibits significant selectivity for HDAC6 over HDAC1[1].
HDAC6-IN-4 inhibits migration activity in a time-dependent and dose-dependent way in B16 and CT26 cells[1].
HDAC6-IN-4 (0-8 μM, 24 h) induces B16 cell apoptosis in a dose-dependent manner[1].
HDAC6-IN-4 exhibits significant plasma stability in humans (97% retention after 6 h), and exhibits significant metabolic stability in human (half-life of 101.91 min) and mouse liver (half-life of 67.94 min) microsomes[1].
Cell Proliferation Assay[1] | Cell Line: | B16, HepG2, A549, and CT26 cells | | Concentration: | 0-50 μM | | Incubation Time: | 72 h | | Result: | Showed antiproliferative activity with IC50values of 1.52, 2.36, 5.77, and 2.09 μM against B16, HepG2, A549, and CT26 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | B16 and CT26 cancer cells | | Concentration: | 2, 4, and 6 μM | | Incubation Time: | 2, 4, 8, 12, and 24 h | | Result: | Dramatically increased the level of Ac-Tub (acetyl-α-tubulin) in a dose-dependent and time-dependent manner. Had almost no effect on the content of Ac-H3 (acetyl-H3). |
Apoptosis Analysis[1] | Cell Line: | B16 cells | | Concentration: | 4, 6, and 8 μM | | Incubation Time: | 24 h | | Result: | Caused moderate to potent induction of apoptosis in the B16 cell line in a dose-dependent manner. Upregulated the expression of apoptotic protein cleaved PARP. |
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体内研究
(In Vivo) | HDAC6-IN-4 (C10) (0-100 mg/kg; i.g.; once daily for 21 days) shows excellent antitumor activity and significantly promoted T cell response in a dose-dependent manner, with no obvious toxicity[1].
| Animal Model: | Five-week-old C57BL/6 mice (immune-related CT26 xenograft model)[1]. | | Dosage: | 50 and 100 mg/kg | | Administration: | Oral gavage, once daily for 21 days | | Result: | Resulted in a substantial tumor growth and tumor tissue size inhibition in a dose-dependent way. Showed significantly high antitumor activity (TGI = 75%) at 100 mg/kg. Raised the plasma IFN-g level and the numbers of CD+and CD3+CD+(activated cytotoxic T) cells. Decreased CD4+CD25+CD127low/-T regulatory cells. Showed no obvious toxicity. |
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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. |
