A 83-01 CAS: 909910-43-6
MF: C25H19N5S
MW: 421.52

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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Alternate Names: A 83-01 is known as an ALK5, ALK4, and ALK7 inhibitor.
Application: A 83-01 is an inhibitor of TGF-β type I receptor kinase (ALK5), activin type IB receptor (ALK4), and nodal type I receptor (ALK7).
CAS Number: 909910-43-6
Purity: ≥97%
Molecular Weight: 421.52
Molecular Formula: C25H19N5S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
* Refer to Certificate of Analysis for lot specific data (including water content).
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A 83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. A 83-01 lonly weakly inhibits ALK-1, -2, -3, -6 and MAPK activity. A 83-01 is more potent than SB 431542. Fibroblasts can be reprogrammed by A 83-01 into alternative lineages.


References

1. Tojo et al (2005) The ALK5 inhibitor A-83-01 inhibits smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-b. Cancer.Sci. 96 791.
2. Hoberg et al (2008) Attachment to laminin-111 facilitates transforming growth factor b-induced expression of matrix metalloproteinase-2 in synovial fibroblasts. Ann.Rheum.Dis. 66 446.

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.
Available in US only.
WGK Germany :
3
PubChem CID :
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 (CAS 909910-43-6)  Product Citations

See how others have used A 83-01 (CAS 909910-43-6). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 35926589  Vedoya, GM.|Galarza, TE.|Mohamad, NA.|Cricco, GP.|Martín, GA.| et al. 2022. Life Sci. 307: 120853.

PMID: # 34088009  Yoshimatsu, S.|Qian, E.|Sato, T.|Yamamoto, M.|Ishikawa, M.|Okano, H.| et al. 2021. Stem Cell Res. 53: 102380.

PMID: # 34088013  Yoshimatsu, S.|Murakami, R.|Nakajima, M.|Sato, T.|Kawasaki, H.|Okano, H.| et al. 2021. Stem Cell Res. 53: 102385.

PMID: # 33375083  Nemoto, A.|Kobayashi, R.|Yoshimatsu, S.|Sato, Y.|Kondo, T.|Yoo, AS.|Shiozawa, S.|Okano, H.| et al. 2020. Cells. 10:

PMID: # 31178141  Nakajima, M.|Yoshimatsu, S.|Sato, T.|Nakamura, M.|Okahara, J.|Sasaki, E.|Shiozawa, S.|Okano, H.| et al. 2019. Biochem Biophys Res Commun. 515: 593-599.

PMID: # 25985394  Costa-Silva, B. et al. 2015. Nat. Cell Biol. 17: 816-26.

PMID: # 25877931  González-Domínguez, É.|Samaniego, R.|Flores-Sevilla, JL.|Campos-Campos, SF.|Gómez-Campos, G.|Salas, A.|Campos-Peña, V.|Corbí, ÁL.|Sánchez-Mateos, P.|Sánchez-Torres, C.| et al. 2015. J Leukoc Biol. 98: 453-66.

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

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

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

Citations 1 to 10 of 14 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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