TGF-β RI Kinase Inhibitor II-CAS 446859-33-2-Calbiochem

C₁₇H₁₃N₅

287.32

MFCD09037561

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).
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).

Cell permeable: yes
Secondary Target
ALK 5 auto phosphorylation (IC₅₀ = 4 nM)
Product competes with ATP.
Primary Target
ALKS binding

Toxicity: Standard Handling (A)

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

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

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

100

≥95% (HPLC)

solid

23 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

yellow

DMSO: 5 mg/mL
methanol: 5 mg/mL

ambient

2-8℃

2 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3