NVS-PAK1-1

SKU: orb1307937

Description

NVS-PAK1-1 is a potent and selective allosteric inhibitor of PAK1 with an IC50 of 5 nM. It is a valuable research tool for studying PAK1 signaling in cancer cell proliferation and migration, applicable in both in vitro and in vivo experimental models.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1783816-74-9
• MW: 479.93
• Purity: 99.35% (May vary between batches)
• Formula: C₂₃H₂₅ClF₃N₅O
• SMILES: CC(C)NC(=O)N1CC[C@@H](C1)NC1=Nc2cc(F)ccc2N(CC(F)F)c2ccc(Cl)cc12
• Target: PAK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.33 mM);DMSO:145 mg/mL (302.13 mM)

Bioactivity

• Target IC50:
  PAK1:5 nM
• 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).
• 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 .

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NVS PAK1 1, NVSPAK11, NVS-PAK-1-1, NVS-PAK1-1, p21 activated kinases, Inhibitor, PAK1, PAK, inhibit

Compound Identifiers

PubChem CID

137125241