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GSK778

CAS No. : 2451862-42-1

MCE 站：GSK778

产品活性：GSK778 (iBET-BD1) 是一种有效和选择性的 BET 蛋白 BD1 溴结构域的抑制剂，IC₅₀ 值为 75 nM (BRD2 BD1)，41 nM (BRD3 BD1)，41 nM (BRD4 BD1) 和143 nM (BRDT BD1)。GSK778 表型化了 pan-BET 抑制剂在癌症模型中的作用。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Epigenetic Reader Domain  |  Apoptosis

In Vitro: GSK778 inhibits BRD BD2 with the IC₅₀s of 3950 nM (BRD2 BD2), 1210 nM (BRD3 BD2), 5843 nM (BRD4 BD2), ａnd 17451 nM (BRDT BD2), respectively.
GSK778 (0.01-10 μM; 72 hours) inhibits the proliferative activity of human primary CD4⁺ T cells ａnd the production of effector cytokines including IFNγ, IL-17A ａnd IL-22.
GSK778 (0.001-10 μM; 5 days) has a more pronounced effect on the growth ａnd viability of MDA-453, MOLM-13, K562, MV4-11, THP-1, ａnd MDA-MB-231 cells.
GSK778 (1000 nM; 72 hours) inhibits proliferation, induces a cell cycle arrest ａnd apoptosis in MV4-11, MOLM13, MDA-MB-231 ａnd MB453 cells.
GSK778 (1000 nM; 12 days) reduces the clonogenic capacity of primary human AML cells.

In Vivo: GSK778 (15 mg/kg/BID; i.p. for 30 days) offers a superior survival advantage to iBET-BD2 in the aggressive MLL-AF9 AML model.
GSK778 (15 mg/kg/BID; s.c. for 14 days) reduces the production of anti-keyhole limpet hemocyanin (KLH) IgM ａnd is well tolerated.
GSK778 exhibits C_max (85 ng/mL), T_max (1.48 h) ａnd AUC_∞ (132 ng.h/mL) following oral administration (10 mg/kg) in mice.

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