616451-M

TGF-β RI Kinase Inhibitor

The TGF-β RI Kinase Inhibitor, also referenced under CAS 396129-53-6, 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, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, LY-364947, HTS-466284, [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole, TβR-I Inhibitor, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor, ALK5 Inhibitor I, LY-364947, HTS-466284
• Empirical Formula (Hill Notation): C₁₇H₁₂N₄
• CAS Number: 396129-53-6
• Molecular Weight: 272.30
• MDL number: MFCD00800758
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 200
• Assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: brown
• solubility: DMSO: 5 mg/mL
• storage temp.: 2-8°C
• InChI: 1S/C17H12N4/c1-2-6-15-13(5-1)12(8-10-19-15)14-11-20-21-17(14)16-7-3-4-9-18-16/h1-11H,(H,20,21)
• InChI key: IBCXZJCWDGCXQT-UHFFFAOYSA-N

Description

General description

A cell-permeable diheteroaryl-substituted pyrazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of TGF-β Receptor I kinase (IC₅₀ = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC₅₀ = 740 nM). Shown to inhibit TGF-β-dependent cellular growth (IC₅₀ = 89 nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC₅₀ = 47 nM in mink lung cells).

A cell-permeable, a potent, selective, reversible, and ATP-competitive inhibitor of TGF-b RI serine/threonine kinase (IC₅₀ = 51 nM). Displays ~15-fold greater selectivity over p38α MAP kinase (IC₅₀ = 740 nM). Reported to inhibit TGF-b-dependent cellular growth (IC₅₀ = 89 nM in mouse NIH3T3 fibroblasts) and transcription activation (IC₅₀ = 47 nM in mink lung cells).

Biochem/physiol Actions

Primary Target
TGF-β receptor I kinase

Target IC₅₀: 51 nM against TGF-β Receptor I kinase; 89 nM against TGF-β-dependent cellular growth in NIH 3T3 mouse fibroblasts; 47 nM against TGF-β-dependent transcription activation in mink lung cells

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sawyer, J.S., et al. 2003. J. Med. Chem.46, 3953.
Singh, J., et al. 2003. Bioorg. Med. Chem. Lett.13, 4355.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3