PIN1 inhibitor API-1

SKU: orb1217737

Description

PIN1 inhibitor API-1 is a specific Pin1 inhibitor (IC50: 72.3 nM). PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from the nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase domain and effectively inhibits Pin1 cis-trans isomerizing activity.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 680622-70-2
• MW: 366.3
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₃F₃N₆O₂
• SMILES: C1=CC(=CC=C1CNC(=O)C(F)(F)F)COC2=NC(=NC3=C2NC=N3)N
• Target: Pin1
• Solubility: DMSO:250 mg/mL (682.50 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis.
• In Vitro:
  PIN1 inhibitor API-1 obviously inhibits SK-Hep-1, SNU-423, and Hep3B cell proliferation with low IC50 values (IC50 = 0.683-4.16 μM).

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

Pin1