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In the lyophilized form, this product is stored refrigerated at 2 - 8°C. This item is assigned a retest date, which is reported on the lot-specific Certificate of Analysis. Upon reconstitution at 20 mg/mL in DMSO, aliquot and store the solution at -20°C, protected from light, for up to 3 months.
616454
A 83-01
≥97% (HPLC), solid, TGF-β RI kinase inhibitor, Calbiochem
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:
Molecular Weight:
421.52
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
Pricing and availability is not currently available.
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Product Name
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).
Quality Level
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
SMILES string
S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1
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
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 Code
11 - Combustible Solids
WGK
WGK 3
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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