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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

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About This Item

Empirical Formula (Hill Notation):
C17H12N4
CAS Number:
396129-53-6
Molecular Weight:
272.30
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00800758
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

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

SMILES string

[nH]1ncc(c1c4ncccc4)c2c3c(ncc2)cccc3

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

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

Preparation Note

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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