PIN1 inhibitor API-1


Catalog No. Size PriceQuantity
M33011-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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

Product information

CAS Number: 680622-70-2

Molecular Weight: 366.30

Formula: C15H13F3N6O2

Chemical Name: N-[(4-{[(2-amino-7H-purin-6-yl)oxy]methyl}phenyl)methyl]-2,2,2-trifluoroacetamide

Smiles: NC1=NC(OCC2=CC=C(CNC(=O)C(F)(F)F)C=C2)=C2NC=NC2=N1

InChiKey: AQFWAWXGBQPBIA-UHFFFAOYSA-N

InChi: InChI=1S/C15H13F3N6O2/c16-15(17,18)13(25)20-5-8-1-3-9(4-2-8)6-26-12-10-11(22-7-21-10)23-14(19)24-12/h1-4,7H,5-6H2,(H,20,25)(H3,19,21,22,23,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (682.50 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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).

In Vivo:

PIN1 inhibitor API-1 suppresses tumor growth in mice by up-regulating mature miRNA biogenesis.

Products are for research use only. Not for human use.

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