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MRIA9 是 ATP 竞争性的、pan-SIK 和PAK2/3抑制剂,其对 SIK1、SIK2 和SIK3的IC50值分别为 516 nM, 180 nM 和 127 nM。
MRIA9 是 ATP 竞争性的、pan-SIK 和PAK2/3抑制剂,其对 SIK1、SIK2 和SIK3的IC50值分别为 516 nM, 180 nM 和 127 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 5,798 | 期货 | |
10 mg | ¥ 9,282 | 期货 |
产品描述 | MRIA9, an ATP-competitive inhibitor targeting pan Salt-Inducible Kinases (SIK) and PAK2/3, demonstrates IC50 values of 516 nM, 180 nM, and 127 nM for SIK1, SIK2, and SIK3, respectively [1]. |
体外活性 | MRIA9 (5 μM) MRIA9 sensitizes SKOV3 cells to paclitaxel treatment through inducing pronounced apoptosis[1].MRIA9 (5 μM) with paclitaxel (2 nM) significantly enhances cell death in HeLa cells[1].MRIA9 strongly impedes centrosome function, causes mitotic spindle mispositioning in ovarian cancer cell lines, prevents the centrosome disjunction during the late G2 phase, and sensitized ovarian cancer cells and patient derived 3D-spheroids to paclitaxel treatment[2]. |
体内活性 | MRIA9 shows high oral bioavailability (F = 75-80%)[1]. |
分子量 | 496.92 |
分子式 | C24H22ClFN6O3 |
CAS No. | 2750707-05-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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