An ALK4 and ALK5 inhibitor
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TP-008

Item No. 41367

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-(5-chloro-2-fluorophenyl)-5-methyl-4-pyridinyl]-1,2-dihydro-2-oxo-3H-imidazo[4,5-c]pyridine-3-acetamide
CAS Number
1976038-41-1
Molecular Formula
C20H15ClFN5O2
Formula Weight
411.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
O=C1N(C(C=C(C(C=C2Cl)=C(C=C2)F)N=C3)=C3C)C4=CC=NC=C4N1CC(N)=O
InChi Code
InChI=1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28)
InChi Key
LVEUPFUJRKZPEN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    TP-008 is an inhibitor of activin receptor-like kinase 4 (ALK4) and ALK5, also known as TGF-β receptor type 1 (TGF-βRI; IC50s = 113 and 343 nM, respectively).1 It is selective for ALK4 and ALK5 over a panel of 467 kinases at 1 µM. TP-008 inhibits ALK4 or ALK5 signaling in a reporter assay using HEK293 cells expressing ALK4 or ALK5 (IC50s = 526 and 245 nM, respectively). It inhibits TGF-β1-induced increases in the levels of phosphorylated Smad2 in C2C12 mouse skeletal muscle myoblasts when used at concentrations of 1 or 10 µM. In vivo, TP-008 (150 or 500 mg/kg per day) induces valvular interstitial cell proliferation, neutrophil infiltration, hemorrhage, and fibrin deposition in rat heart valves.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hanke, T., Wong, J.F., Berger, B.-T., et al. A highly selective chemical probe for activin receptor-like kinases ALK4 and ALK5. ACS Chem. Biol. 15(4), 862-870 (2020).

    2. Wang, H., Lawson, J.D., Scorah, N., et al. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors. Bioorg. Med. Chem. Lett. 26(17), 4334-4339 (2016).