Darizmetinib

Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4) . Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts[1][2][3].

Product Specifications

CAS Number

[2369583-33-3]

Product Name Alternative

HRX-0215

UNSPSC

12352005

Target

JNK; MDM-2/p53; NF-κB; p38 MAPK

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway; NF-κB

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/darizmetinib.html

Purity

99.94

Solubility

DMSO : 175 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(C(NS(=O)(CCC)=O)=C1F)F)C2=NNC3=NC=C(C4=CC=NC=C4)C=C32

Molecular Formula

C21H17F2N5O3S

Molecular Weight

457.45

References & Citations

[1]Praefke B, et al. Preparation of pyrazolopyridines as protein kinase MKK4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death: World Intellectual Property Organization, WO2019149738. 2019-08-08.|[2]WHO Drug Information-World Health Organization (WHO) .|[3]Zwirner S, et al. First-in-class MKK4 inhibitors enhance liver regeneration and prevent liver failure. Cell. 2024 Mar 28;187 (7) :1666-1684.e26.