An AKS1 inhibitor
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GS-444217

Item No. 40757

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-cyclopropyl-1H-imidazol-1-yl)-N-[3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl]-2-pyridinecarboxamide
CAS Number
1262041-49-5
Synonyms
  • Apoptosis Signal-regulating Kinase 1-IN-1
  • Apoptosis Signal-regulating Kinase 1 Inhibitor 1
  • ASK1-IN-1
  • ASK1 Inhibitor 1
Molecular Formula
C23H21N7O
Formula Weight
411.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C(C1=CC(N2C=NC(C3CC3)=C2)=CC=N1)NC4=CC=CC(C5=NN=CN5C6CC6)=C4
InChi Code
InChI=1S/C23H21N7O/c31-23(20-11-19(8-9-24-20)29-12-21(25-13-29)15-4-5-15)27-17-3-1-2-16(10-17)22-28-26-14-30(22)18-6-7-18/h1-3,8-15,18H,4-7H2,(H,27,31)
InChi Key
ZGCMQKWOUIMBEP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $87

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    10 mg

    $139

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    25 mg

    $261

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    50 mg

    $476

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    Product Description

    GS-444217 is an inhibitor of apoptosis signal-regulating kinase 1 (ASK1; IC50 = 2.87 nM).1 It is selective for ASK1 over 442 additional kinases at 1 µM. GS-444217 (0.001-10 µM) inhibits phosphorylation of the ASK1 substrates MAP kinase kinase 3 (MKK3), MKK6, and MKK4, as well as their downstream substrates p38 MAPK and JNK in HEK293T cells expressing human ASK1. Dietary administration of GS-444217 (0.3% w/w) reduces renal fibrosis and proteinuria in a db/db eNOS-/- mouse model of diabetic kidney disease (DKD).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liles, J.T., Corkey, B.K., Notte, G.T., et al. ASK1 contributes to fibrosis and dysfunction in models of kidney disease. J. Clin. Invest. 128(10), 4485-4500 (2018).