5.08158

TGF-β

InSolution, ≥99%, 50 mM in DMSO, RI Kinase Inhibitor II, RepSox

• Synonym(s): InSolution TGF-β RI Kinase Inhibitor II, RepSox, RepSox InSolution, E-616452 InSolution, ALK5 Inhibitor II, Transforming Growth Factor-β, Type I Receptor Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
• Empirical Formula (Hill Notation): C₁₇H₁₃N₅
• CAS Number: 446859-33-2
• Molecular Weight: 287.32
• MDL number: MFCD09037561
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥99% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• storage temp.: −70°C
• SMILES string: [nH]1ncc(c1c4nc(ccc4)C)c2nc3c(nccc3)cc2
• InChI: 1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
• InChI key: LBPKYPYHDKKRFS-UHFFFAOYSA-N

Description

General description

A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of TGF-β type I receptor (ALK5; IC₅₀ = 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation, and TGF-β cellular assay in HepG2 cells, respectively). Minimally affects a panel of 9 closely related kinases including p38 MAPK (IC₅₀ >16 µM).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ALK5

Reversible: yes

Target IC₅₀: 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation, and TGF-&beta

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

A 50 mM (5 mg/348 µl) sterile-filtered solution of TGF-β RI Kinase Inhibitor II, RepSox (Cat. No. 616452) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C. Use only fresh DMSO for further dilution.

Other Notes

Ichida, J. K., et al. 2009. Cell Stem Cell5, 491.
Gellibert, F., et al. 2004. J. Med. Chem.47, 4494.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 10 - Combustible liquids
• wgk_germany: WGK 2
• flash_point_f: 188.6 °F - (refers to pure substance)
• flash_point_c: 87 °C - (refers to pure substance)