An MKK4 inhibitor
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HRX215

Item No. 41238

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,6-difluoro-3-[[5-(4-pyridinyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]carbonyl]phenyl]-1-propanesulfonamide
CAS Number
2369583-33-3
Synonyms
  • Darizmetinib
  • LN3348
Molecular Formula
C21H17F2N5O3S
Formula Weight
457.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/ml
SMILES
FC(C(NS(=O)(CCC)=O)=C1F)=CC=C1C(C(C2=C3)=NNC2=NC=C3C4=CC=NC=C4)=O
InChi Code
InChI=1S/C21H17F2N5O3S/c1-2-9-32(30,31)28-19-16(22)4-3-14(17(19)23)20(29)18-15-10-13(11-25-21(15)27-26-18)12-5-7-24-8-6-12/h3-8,10-11,28H,2,9H2,1H3,(H,25,26,27)
InChi Key
WBNMARNYIFMNEP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $138

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    5 mg

    $471

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    10 mg

    $825

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    25 mg

    $1,375

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    Product Description

    HRX215 is an inhibitor of MAP kinase kinase 4 (MKK4; IC50 = 0.02 µM).1 It is selective for MKK4 over JNK1, B-RAF, and MKK7 (IC50s = 7.07, 11.46, and 14.97 µM, respectively). HRX215 (10 mg/kg) decreases hepatocyte apoptosis in a mouse model of liver damage induced by carbon tetrachloride (CCl4). It increases survival and hepatic size and regeneration, decreases intracranial pressure (ICP), and reduces blood ammonia, total bilirubin, and aspartate aminotransferase (AST) levels in a porcine model of partial hepatectomy-induced liver failure when administered at 5 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zwirner, S., Rmilah, A.A.A., Klotz, S., et al. First-in-class MKK4 inhibitors enhance liver regeneration and prevent liver failure. Cell 187(7), 1666-1684 (2024).