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产品价格:电议      采购度:1630      原产地:美洲
发布时间:2021/6/23 8:44:26 所属地区:国外 国外
简要描述:
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。
标签:iBET-BD1
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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 Cmax (85 ng/mL), Tmax (1.48 h) and AUC∞ (132 ng.h/mL) following oral administration (10 mg/kg) in mice.
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更新时间:2024/7/4 13:12:35
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