FRAX1036

SKU: orb1300419

Description

FRAX-1036 is a potent and selective small molecule inhibitor of PAK1. It is a valuable research tool for studying PAK1 signaling in cancer biology and neuroscience, with utility in both cellular assays and in vivo models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1432908-05-8
• MW: 518.05
• Purity: 99.95%
• Formula: C₂₈H₃₂ClN₇O
• SMILES: CCn1c2nc(NCCC3CCN(C)CC3)ncc2cc(-c2ccc(cc2Cl)-c2cncc(C)n2)c1=O
• Target: PAK
• Solubility: DMSO:insoluble

Bioactivity

• Target IC50:
  PAK1:23.3 nM(Ki)|PAK2:72.4 nM(Ki)|PAK4:2.4 μM(Ki)
• In Vivo:
  KT21 are treated with Frax1036 showing slower tumor growth, while Frax1036 is unlikely to have significant blood-brain barrier permeability in mice.
• In Vitro:
  MDA-MB-175 cells,which are PAK1-amplified (MEK1-S298 and CRAF-S338) ,was observed Potent cellular inhibition at 2.5 to 5 μM concentrations of FRAX1036. PAK1-amplified breast cancer cells are treated with FRAX1036 leading to apoptosis. OVCAR-3 cells are treated with FRAX-1036 resulting in upregulation of p53 and p21, while down-regulating cyclin B1.
• Cell Research:
  MDA-MB175 cells are treated with increasing concentrations (0, 0.5, 1, 2.5, 5 μM) of FRAX1036 for 24 hours.
• Animal Research:
  Pak2-deficient mice were treated by oral gavage of 30 mg/kg Frax1036.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, PAK1, PAK, PAK2, PAK4, FRAX 1036, FRAX1036, FRAX-1036, p21 activated kinases

Compound Identifiers

PubChem CID

71557891