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TGF-beta&Smad

A83-01 (909910-43-6)

A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.

Not Intended for Therapeutic Use. For research use only.

CAS: 909910-43-6 Category

A83-01 (909910-43-6) Description:

A-83-01 is an ALK inhibibitor. It was found that A-83-01 inhibited the transcriptional activity induced by TGF-beta type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 was found to be more potent in the inhibition of ALK5 than a previously described ALK-5 inhibitor, SB-431542, and also to prevent phosphorylation of Smad2/3 and the growth inhibition induced by TGF-beta. A-83-01 inhibited the epithelial-to-mesenchymal transition induced by TGF-beta, suggesting that A-83-01 and related molecules may be useful for preventing the progression of advanced cancers.

A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.

It has little effect on bone morphogenic type I receptors, p38 mitogen-activated protein kinase, or ERK. A 83-01 has been used to reprogram fibroblasts into alternative lineages, including neural stem cells and cardiomyocytes.

A83-01 (909910-43-6) Specifications:

Product Name A83-01
Synonyms A8301; A 8301; A-8301
Chemical Name 3-(6-methylpyridin-2-yl)-~{N}-phenyl-4-quinolin-4-ylpyrazole-1-carbothioamide
Purity >98%
CAS Number 909910-43-6
Molecular Formula C25H19N5S
Molecular Weight 421.522 g/mol
Monoisotopic Mass 421.136 g/mol
MDL number MFCD08705403
InChIKey HIJMSZGHKQPPJS-UHFFFAOYSA-N
InChi Code 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)
SMILES CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5
Form powder
Color white to beige
Solubility  Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor; TGF-β/ALK5 inhibitor

 


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RIDADR NONH for all modes of transport

References:

1.The Transcriptome of Human Endometrial Mesenchymal Stem Cells Under TGFβR Inhibition Reveals Improved Potential for Cell-Based Therapies. Gurung S, Williams S, Deane JA, Werkmeister JA, Gargett CE. Front Cell Dev Biol. 2018 Dec 4;6:164. doi: 10.3389/fcell.2018.00164. eCollection 2018.

2.Inhibitors of the VEGF Receptor Suppress HeLa S3 Cell Proliferation via Misalignment of Chromosomes and Rotation of the Mitotic Spindle, Causing a Delay in M-Phase Progression. Okumura D, Hagino M, Yamagishi A, Kaibori Y, Munira S, Saito Y, Nakayama Y. Int J Mol Sci. 2018 Dec 12;19(12). pii: E4014. doi: 10.3390/ijms19124014.

3.Leucine-rich repeat-containing G-protein coupled receptor 5 enriched organoids under chemically-defined growth conditions. Hahn S, Kim MS, Choi SY, Jeong S, Jee J, Kim HK, Jeong SY, Shin H, Kim HS, Park JS, Yoo J. Biochem Biophys Res Commun. 2019 Jan 8;508(2):430-439. doi: 10.1016/j.bbrc.2018.11.003. Epub 2018 Nov 28.

4.Small molecule-mediated reprogramming of human hepatocytes into bipotent progenitor cells. Kim Y, Kang K, Lee SB, Seo D, Yoon S, Kim SJ, Jang K, Jung YK, Lee KG, Factor VM, Jeong J, Choi D. J Hepatol. 2019 Jan;70(1):97-107. doi: 10.1016/j.jhep.2018.09.007. Epub 2018 Sep 19.

1 review for A83-01 (909910-43-6)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The A83-01 (909910-43-6) is high purity,also customer service is pretty nice !gotta try!!

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