JNJ-16241199,604769-01-9

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JNJ-16241199

CAS No. : 604769-01-9

MCE 国际站：JNJ-16241199

产品活性：JNJ-16241199 是一种具有口服活性的选择性 hydroxamate-based histone deacetylase (HDAC) 抑制剂，对 HDAC 1 和 HDAC8 的IC₅₀ 分别为 3.3 nM 和 23 nM。JNJ-16241199 诱导组蛋白 3 乙酰化，并显著上调 A2780 卵巢癌细胞中 p21^waf1, ^cip1 的表达。JNJ-16241199 诱导细胞凋亡 (cell apoptosis)，并在多种人类恶性肿瘤中显示抗癌活性。JNJ-16241199 可用于癌症研究。

研究领域：Apoptosis  |  Epigenetics  |  Cell Cycle/DNA Damage

作用靶点：Apoptosis  |  HDAC

In Vitro: JNJ-16241199 inhibits proliferation with comparable potency in acute lymphoblastic leukaemia (ALL), AML, chronic lymphoblastic leukaemia (CLL), chronic myeloid leukaemia (CML), lymphoma and myelomatumour cells (IC₅₀ values = 15–486 nM) .
JNJ-16241199 inhibits the Primary human mammary epithelial cell (HMEC) proliferation with the IC₅₀ of 32 nM, and is insensitive to quiescent, non-proliferative HMEC cells (IC₅₀ = 7815 nM) .
JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) induces apoptosis and inhibits angiogenesis in A2780 cell line.

In Vivo: JNJ-16241199 (10-40 mpk/day for 28 days, p.o.) inhibits the growth of A2780 ovarian, H460 lung and HCT116 colon carcinomas orthotopic xenograft tumor models .

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