供货周期: | 一周 |
品牌: | 爱必信 |
规格: | 98% |
货号: | abs821186 |
CAS号: | 1783816-74-9 |
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抑制剂描述: 产品名称:NVS-PAK1-1 产品别名:见爱必信官网 英文别名:NVS-PAK1-1 靶点:PAK CAS:1783816-74-9 纯度:98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder) 描述: NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM. 溶解性:DMSO : ≥ 125 mg/mL (260.45 mM) 体外研究: NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved. 体内研究:NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved.
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