Powder: -20°C for 3 years
In solvent: -80°C for 2 years
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
Description | NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM). |
Targets&IC50 | PAK1:5 nM |
In vitro | NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows 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 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases . |
In vivo | NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min). |
Molecular Weight | 479.93 |
Formula | C23H25ClF3N5O |
CAS No. | 1783816-74-9 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 125 mg/mL (260.45 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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NVS-PAK1-1 1783816-74-9 细胞骨架 PAK Inhibitor p21 activated kinases NVS PAK1 1 inhibit NVS-PAK-1-1 NVSPAK11 inhibitor