616452

TGF-β RI Kinase Inhibitor II

TGF-β RI Kinase Inhibitor II, CAS 446859-33-2, is a cell-permeable, potent, reversible, ATP-competitive inhibitor of TGF-β R1 kinase (IC₅₀ = 23 nM and 4 nM for ALK5 binding & auto-phosphorylation).

• Synonym(s): TGF-β RI Kinase Inhibitor II, 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: 12352200

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: solid
• potency: 23 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 5 mg/mL; methanol: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• 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 naphthyridinyl pyrazolo compound that acts as a 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 at IC₅₀ >16 µM. Also available as a 50 mM solution in DMSO (Cat. No. 508158).

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
ALKS binding

Product competes with ATP.

Secondary Target
ALK 5 auto phosphorylation (IC₅₀ = 4 nM)

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Gellibert, F., et al. 2004. J. Med. Chem.47, 4494.
Ichida, J. K., et al. 2009. Cell Stem Cell 5, 491.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable