For research use only. Not for therapeutic Use.
NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM)[1].
NVS-PAK1-1 potently inhibits autophosphorylation of PAK1 (S144) at 0.25 µM in the Su86.86 cell line and MEK S289 phosphorylation with an IC50=0.21 µM in Su86.86 cells in which PAK2 is downregulated[1].
Catalog Number | I014966 |
CAS Number | 2250019-95-3 |
Synonyms | (3S)-3-[[8-chloro-11-(2,2-difluoroethyl)-3-fluoro-5H-benzo[b][1,4]benzodiazepin-6-ylidene]amino]-N,N-dimethylpyrrolidine-1-carboxamide |
Molecular Formula | C22H23ClF3N5O |
Purity | ≥95% |
InChI | InChI=1S/C22H23ClF3N5O/c1-29(2)22(32)30-8-7-15(11-30)27-21-16-9-13(23)3-5-18(16)31(12-20(25)26)19-6-4-14(24)10-17(19)28-21/h3-6,9-10,15,20H,7-8,11-12H2,1-2H3,(H,27,28)/t15-/m0/s1 |
InChIKey | RVHZFZVJXGIAJF-HNNXBMFYSA-N |
SMILES | CN(C)C(=O)N1CCC(C1)N=C2C3=C(C=CC(=C3)Cl)N(C4=C(N2)C=C(C=C4)F)CC(F)F |
Reference | [1]. NVS-PAK1-1 A Chemical Probe For PAK1 |