NVS-PAK1-1

SKU: orb1218618

Description

NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1783816-74-9
• MW: 479.93
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₅ClF₃N₅O
• SMILES: FC1=CC2=C(C=C1)N(CC(F)F)C3=C(C=C(Cl)C=C3)C(N[C@H]4CCN(C(NC(C)C)=O)C4)=N2
• Target: PAK
• Solubility: DMSO:125 mg/mL (260.45 mM)

Bioactivity

• 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).
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

PAK