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≥95% (HPLC), solid, TGF-β RI kinase inhibitor, Calbiochem

Synonym(s):

TGF-β RI Kinase Inhibitor II, ALK5 Inhibitor II, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor II, 2-(3-(6-Methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine

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About This Item

Empirical Formula (Hill Notation):
C17H13N5
CAS Number:
446859-33-2
Molecular Weight:
287.32
MDL number:
MFCD09037561
UNSPSC Code:
51111800
NACRES:
NA.77

product name

TGF-β RI Kinase Inhibitor II, TGF-β RI Kinase Inhibitor II, CAS 446859-33-2, is a cell-permeable, potent, reversible, ATP-competitive inhibitor of TGF-β R1 kinase (IC₅₀ = 23 nM and 4 nM for ALK5 binding & auto-phosphorylation).

Quality Level

100

Assay

≥95% (HPLC)

form

solid

potency

23 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 5 mg/mL
methanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)

InChI key

LBPKYPYHDKKRFS-UHFFFAOYSA-N

General description

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).
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).

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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