A 83-01 An inhibitor of TGFβ-RI, ACTR-IB and ACTR-IC

A 83-01 (CAS 909910-43-6)

A 83-01 | CAS 909910-43-6 is rated 5.0 out of 5 by 1.
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Synonym: 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
Application: An inhibitor of TGFβ-RI, ACTR-IB and ACTR-IC
CAS Number: 909910-43-6
Purity: ≥97%
Molecular Weight: 421.52
Molecular Formula: C25H19N5S
* Refer to Certificate of Analysis for lot specific data (including water content).
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A 83-01 is a selective an inhibitor of TGFβ-RI, ACTR-IB and ACTR-IC (IC50 values are 12, 45 and 7.5 nM respectively). This compound blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. A 83-01 only weakly inhibits ALK-1, -2, -3, -6 and MAPK activity and is more potent than SB 431542 (sc-204265).


References

1. Tojo, M. et al. 2005. Cancer Sci. 96(11): 791-800. PMID: 16271073
2. Hoberg, M. et al. 2007. Ann. Rheum. Dis. 66(4): 446-451. PMID: 17124250

Physical State :
Solid
Solubility :
Soluble in DMSO (50 mM).
Storage :
Store at -20° C
Melting Point :
272.95° C (Predicted)
Boiling Point :
590.01° C at 760 mmHg (Predicted)
Density :
1.28 g/cm3 (Predicted)
Refractive Index :
n20D 1.71 (Predicted)
IC50 :
TGF-β type I receptor ALK5 kinase: IC50 = 12 nM; TGF-β type I activin/nodal receptor ALK4: IC50 = 45 nM; TGF-β type I nodal receptor ALK7: IC50 = 7.5 nM
pK Values :
pKa: 8.77 (Predicted), pKb: 3.16 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
16218924
MDL Number :
MFCD08705403
SMILES :
CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5

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Certificate of Analysis

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A 83-01  Product Citations

See how others have used A 83-01. Click on the entry to view the PubMed entry .

Citations 1 to 5 of 5 total

PMID: # 25088330  Prasanphanich, AF. et al. 2014. Free Radic. Biol. Med. 76: 1-13.

PMID: # 25351330  2014. Bioscience, biotechnology, and biochemistry. 78: 1805-12.

PMID: # 22425773  2012. Biochemical and biophysical research communications. 420: 380-4.

PMID: # 20427282  Galvin, KE. et al. 2010. J Biol Chem. -.

PMID: # 16271073  Tojo, M. et al. 2005. Cancer Sci. 96: 791-800.

Citations 1 to 5 of 5 total
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Rated 5 out of 5 by from Galvin et al Galvin et al. (PubMed ID 20427282) used A 83-01 to prevent phosphorylation of Smad2 by selectively inhibiting ALK4/5/7 receptors in mouse embryonic stem cells. -SCBT Publication Review
Date published: 2015-03-06
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