产品
编 号:F194382
分子式:C25H27F3N6O2
分子量:500.52
产品类型
结构图
CAS No: 1620820-12-3
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产品详情
生物活性:
TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).
体外研究:
TL4 12 (0-5 μM; 4 days) shows antiproliferation activity with an IC50 value of 37 nM for MM cells, and with IC50s of 1.62, 3.7, 4.4, 5.7, 10, 32, 49, 19 μM for JJN3, MM1.S, H929, RPMI-8226, MOLP-8, SKMM2, LP-1, U266 cells, respectively..TL4-12 (0, 1, 3 μM; 24 h) dose-dependently decreases IKZF1, c-MYC, and BCL-6 protein expression and increases p53 level in K-RASG12A MM.1S cells.TL4-12 dose-dependently increases Annexin-V positive cell from 6% (dimethyl sulfoxide) to 13% (1 μM) and 22% (3 μM), respectively.TL4-12 induces apoptosis and cell-cycle arrest in the G0/G1 phase in MM.1S, RPMI-8226, RPMI-8226 cells.