A selective inhibitor of ALK5
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ALK5 Inhibitor II (hydrochloride)

Item No. 15526

Technical Information
Formal Name
2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-1,5-naphthyridine, monohydrochloride
CAS Number
2319939-07-4
Synonyms
  • E 616452
  • RepSox
  • SJN 2511
Molecular Formula
C17H13N5 • HCl
Formula Weight
Purity
≥98%
A crystalline solid
Ethanol: 0.5 mg/mlPBS (pH 7.2): 0.2 mg/ml
λmax
332 nm
SMILES
CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1.Cl
InChi Code
InChI=1S/C17H13N5.ClH/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14;/h2-10H,1H3,(H,19,22);1H
InChi Key
ZKLHJSQURWMEIX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    ALK5 inhibitor II is a cell permeable, selective inhibitor of the TGF-β type 1 activin like kinase receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively).1 This inhibitor demonstrated less potent activity (IC50s > 16 μM) when tested against a panel of 9 related kinases, including p38 MAPK and GSK3.1 At 25 μM, this compound has been used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2 via inhibition of the TGF-β signaling pathway and induction of Nanog transcription.2 This product is a hydrochloride form of the compound. A non-hydrochloride version of ALK5 inhibitor II (Item No. 14794) is also available.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gellibert, F., Wollven, J., Fouchet, M.H., et alIdentification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-β type I receptor inhibitors. J. Med. Chem. 47(18), 4494-4506 (2004).

    2. Ichida, J.K., Blanchard, J., Lam, K., et alA small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog. Cell Stem Cell 5(5), 491-503 (2009).