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About This Item
Empirical Formula (Hill Notation):
C17H12N4
CAS Number:
Molecular Weight:
272.30
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
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
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.
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 Code
11 - Combustible Solids
WGK
WGK 3
Certificates of Analysis (COA)
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