NVS-PAK1-1|PAK1 inhibitor|cas 1783816-74-9

Cas No.:	1783816-74-9
Chemical Name:	NVS-PAK1-1，NVS-PAK11，NVS-PAK1 1
Synonyms:	NVS-PAK1-1，NVS-PAK11，NVS-PAK1 1
SMILES:	CC(C)NC(=O)N1CC[C@@H](C1)NC2=NC3=C(C=CC(=C3)F)N(C4=C2C=C(C=C4)Cl)CC(F)F
Formula:	C₂₃H₂₅ClF₃N₅O
M.Wt:	479.93
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
In Vivo:	NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)[1].
In Vitro:	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[1].

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