PTP1B-IN-2


Catalog No. Size PriceQuantity
M17902-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.

Product information

CAS Number: 1919853-46-5

Molecular Weight: 680.79

Formula: C34H36N2O9S2

Chemical Name: methyl 5-[N-({4-[N-(2-methoxy-2-oxoethyl)methanesulfonamido]phenyl}methyl)phenylmethanesulfonamido]-2-[(4-methylphenyl)methoxy]benzoate

Smiles: CS(=O)(=O)N(CC(=O)OC)C1C=CC(CN(C2=CC(=C(C=C2)OCC2C=CC(C)=CC=2)C(=O)OC)S(=O)(=O)CC2C=CC=CC=2)=CC=1

InChiKey: IPNJQCVHNPGYOX-UHFFFAOYSA-N

InChi: InChI=1S/C34H36N2O9S2/c1-25-10-12-27(13-11-25)23-45-32-19-18-30(20-31(32)34(38)44-3)36(47(41,42)24-28-8-6-5-7-9-28)21-26-14-16-29(17-15-26)35(46(4,39)40)22-33(37)43-2/h5-20H,21-24H2,1-4H3

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : ≥ 100 mg/mL (146.89 mM).

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:

PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several hydrogen bonds and hydrophobic interactions with key residues of the catalytic site. The binding characteristics between PTP1B domain and ligand shows that PTP1B-IN-2 is an ABC type inhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 µM and 30 µM. Insulin-stimulated glucose uptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%, 19.0% and 38.1% at 5, 10 and 20 µM, respectively .

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

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