P-gp inhibitor 1

SKU: orb1309288

Description

P-gp inhibitor 1 is a potent small molecule that reverses P-glycoprotein-mediated multidrug resistance, demonstrating an EC50 of 57.9 nM in K562/A02 cell assays. This compound is a valuable research tool for studying drug efflux mechanisms and overcoming chemoresistance in both in vitro and in vivo cancer models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2050747-49-2
• MW: 517.62
• Purity: 98.65% (May vary between batches)
• Formula: C₃₂H₃₁N₅O₂
• SMILES: COc1cc2CCN(CCc3ccc(Nc4nc(nc5ccccc45)-c4ccncc4)cc3)Cc2cc1OC
• Target: P-gp
• Solubility: DMSO:45 mg/mL (86.94 mM)

Bioactivity

• In Vitro:
  In K562/A02 MDR cells, P-gp inhibitor 1 (0.1, 1, 5 μM, 1 h) boosts the potency of other MDR-related cytotoxic agents with different structures, increases the accumulation of DOX, blocks Pgp-mediated Rh123 efflux, and suppresses P-gp ATPase activity.
  Read more...

Storage & Handling

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

Alternative Names

ABCB1, Cluster of differentiation 243, CD243, Multidrug resistance protein 1, inhibit, Inhibitor, MDR1, P gp inhibitor 1, Pgp inhibitor 1, P-gp inhibitor 1, P-gp, Pgp, P-glycoprotein

Compound Identifiers

PubChem CID

132822387