A TGF-β type I receptor inhibitor
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A 83-01

Item No. 9001799

Technical Information
Formal Name
3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide
CAS Number
909910-43-6
Molecular Formula
C25H19N5S
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 25 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 14 mg/mlEthanol: 0.3 mg/ml
λmax
227, 307 nm
SMILES
S=C(N1N=C(C2=NC(C)=CC=C2)C(C3=CC=NC4=C3C=CC=C4)=C1)NC5=CC=CC=C5
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)
InChi Key
HIJMSZGHKQPPJS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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) (IC50s = 12, 45, and 7.5 nM, respectively).1 It blocks the phosphorylation of SMAD2/3 and inhibits TGF-β-induced epithelial-to-mesenchymal transition.1 It has little effect on bone morphogenic type I receptors, p38 mitogen-activated protein kinase, or ERK.1 A 83-01 has been used to reprogram fibroblasts into alternative lineages, including neural stem cells and cardiomyocytes.2,3 This product is also available as part of Cayman's Hepatocyte Differentiation Reagent Kit (Item No. 44737),

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tojo, M., Hamashima, Y., Hanyu, A., et alThe ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-β. Cancer Sci. 96(11), 791-800 (2005).

    2. Cao, N., Huang, Y., Zheng, J., et alConversion of human fibroblasts into functional cardiomyocytes by small molecules. Science 352(6290), 1216-1220 (2016).

    3. Zhang, M., Lin, Y.H., Sun, Y.J., et alPharmacological reprogramming of fibroblasts into neural stem cells by signaling-directed transcriptional activation. Cell Stem Cell 18(5), 653-667 (2016).