HDAC-IN-57

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HDAC-IN-57 是一种具有口服活性的组蛋白脱乙酰酶 (HDAC) 泛抑制剂，对 HDAC1, HDAC2, HDAC6, HDAC8 的 IC50 值分别为 2.07 nM, 4.71 nM, 2.4 nM 和 107 nM。HDAC-IN-57 可抑制 LSD1，对 LSD1 的 IC50 值为 1.34 μΜ。HDAC-IN-57 诱导凋亡 (apoptosis)，具有抗肿瘤活性。

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ.HDAC-IN-57 induces apoptosis, and has anti-tumor activity.

Western Blot Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.5 μM Incubation Time:48 hours Result:Inhibited cellular LSD1 and HDACs. Upregulated the expression of apoptotic markers, including cytochrome C, Bax, cleaved caspase-3/7/9, and cleaved PARP, while downregulating the expression of anti-apoptotic protein Bcl-2. Apoptosis Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.5 μM, 5.0 μM Incubation Time:48 hours Result:Triggered MGC-803 and HCT116 cells apoptosis in a dose-dependent manner.Induced about 55.4% and 51.5% MGC-803 cell apoptosis at a concentration of 5 μM.Cell Migration Assay Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.0 μM, 4 μM Incubation Time:48 hours Result:Reduced the number of migrated of MGC-803 and HCT-116 cells. Inhibited the migration and invasion of cancer cells.Cell Cycle Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.5 μM, 5.0 μM Incubation Time:48 hours Result:Induced G2/M cycle arrest in MGC-803 and HCT-116 cells.

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Cell Cycle/DNA Damage

HDAC

HDAC | Apoptosis

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2716217-79-5

377.39

C21H19N3O4

>98% (HPLC)

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C(NCC1=CC=C(C(NO)=O)C=C1)(=O)C=2C=C(N=CC2)C3=CC=C(OC)C=C3

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(-20℃)

With Ice Pack

≥ 2 years