616453

TGF-β RI Kinase Inhibitor III

The TGF-β RI Kinase Inhibitor III, also referenced under CAS 356559-13-2, controls the biological activity of TGF-β RI Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): TGF-β RI Kinase Inhibitor III, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor III, 2-(5-Benzo[1,3]dioxol-4-yl-2-tert-butyl-1H-imidazol-4-yl)-6-methylpyridine, HCl, ALK5 Inhibitor III, SB-505124, HCl
• Empirical Formula (Hill Notation): C₂₀H₂₁N₃O₂ · xHCl
• CAS Number: 356559-13-2
• Molecular Weight: 335.40 (free base basis)
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: light yellow
• solubility: DMSO: 20 mg/mL; water: 3 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C20H21N3O2.ClH/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15;/h5-10H,11H2,1-4H3,(H,22,23);1H
• InChI key: BTUOOXPZOVNPMF-UHFFFAOYSA-N

Description

General description

A cell-permeable imidazolyl-pyridine compound that acts as a potent, ATP-competitive, reversible, and selective inhibitor of activin receptor-like kinase 4 (IC₅₀ = 129 nM), 5 ( IC₅₀ = 47 nM), and 7. It inhibits p38 MAPKα only at much higher concentrations (IC₅₀ = 10.6 µM) and has little effect against ALK1/2/3/6 as well as a panel of 26 other kinases.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Activin receptor-like kinase 4, 5, 7

Product competes with ATP.

Reversible: yes

Target IC₅₀: 129 nM, 47 nM, against activin receptor-like kinase 4, 5, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

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

Other Notes

Hu, T., et al. 2005. Am. J. Physiol. Renal Physiol.289, F816.
DaCosta Byfield, S., et al. 2004. Mol. Pharmacol.65, 744.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable