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TGF-β RI Kinase Inhibitor IV

TGF-β RI Kinase Inhibitor IV, CAS 909910-43-6, is a cell-permeable, selective inhibitor of ALK-4/5/7-mediated signaling (IC₅₀ = 45, 12, and 7.5 nM, respectively).

Synonym(s):

TGF-β RI Kinase Inhibitor IV, Transforming Growth Factor-β Type I Receptor Kinase Inhibitor IV, 3-(6-Methylpyridin-2-yl)-4-(4-quinolyl)-1-phenylthiocarbamoyl-1H-pyrazole, A-83-01, ALK5 Inhibitor IV

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About This Item

Empirical Formula (Hill Notation):
C25H19N5S
CAS Number:
909910-43-6
Molecular Weight:
421.52
UNSPSC Code:
12352200

Quality Level

200

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

pale yellow

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)

InChI key

HIJMSZGHKQPPJS-UHFFFAOYSA-N

General description

A cell-permeable trisubstituted pyrazole compound that has been shown to selectively inhibit ALK-4/5/7-mediated (IC50 = 45, 12, and 7.5 nM, respectively, in luciferase transcription activity assays), but not ALK-1/2/3/6-mediated cellular signaling in Mv1Lu R4-2 transfectants expressing the individual Type I TGF-β receptors. Inhibits TGF-β-induced Smad2-phosphorylation in HaCaT cells and epithelial-to-mesenchymal transition in NMuMG cells at a concentration of 1 µM.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
ALK-4/5/7
Product does not compete with ATP.
Reversible: no
Target IC50: 45, 12, and 7.5 nM, respectively, in inhibit ALK-4/5/7-mediated luciferase transcription activity assays

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

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

Other Notes

Tojo, M., et al. 2005. Cancer Sci.96, 791.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

Certificates of Analysis (COA)

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