化合物ISA-2011B T15597

Product Introduction
Bioactivity


英文名: ISA-2011B

描述: ISA-2011B 是有效的PIP5K1α抑制剂， 显示出抗癌活性。

体外活性: ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B shows the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells[1]. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR[2]. The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is obviously reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively.

体内活性: Overexpression of AR-V7 increases PIP5K1α, promotes rapid growth of PCa in xenograft mice, whereas inhibition of PIP5K1α by its inhibitor ISA-2011B suppresses the growth and invasiveness of xenograft tumors overexpressing AR-V7. ISA-2011B obviously suppresses the growth of tumor cells in xenograft mice and is mediated by targeting PIP5K1α-associated PI3K/AKT and the downstream survival, proliferation, and invasion pathways[1]. ISA-2011B disrupts protein stabilization of AR-V7 which is dependent on PIP5K1α, leading to suppression of invasive growth of AR-V7-high tumors in xenograft mice[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (235.93 mM)


关键字: Inhibitor | ISA-2011B | inhibit | ISA 2011B | ISA2011B

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途