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GW843682X

CAS No. : 660868-91-7

MCE 站：GW843682X

产品活性：GW843682X 是一种选择性的，ATP-竞争性的 PLK1 and PLK3 抑制剂，IC₅₀ 值分别为 2.2 nM and 9.1 nM，选择性是其他 30 种激酶的 100 多倍。

研究领域：Cell Cycle/DNA Damage

作用靶点：Polo-like Kinase (PLK)

In Vitro: GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC₅₀s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC₅₀ of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells. GW843682X inhibits proliferation of U937 cells with an EC₅₀ of 120 nM. GW843682X (500 nM) in combination with 5 ?M VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X (0.06-1?μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1?μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1?μM) dephosphorylates Bcl-xl in leukemia cells.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Anti-Blood Cancer Compound Library  |  Wortmannin  |  LFM-A13  |  Poloxin  |  HMN-214  |  SBE13 Hydrochloride  |  TC-S 7005  |  Poloxime  |  Cyclapolin 9

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