Darizmetinib (HRX215, HRX0215) | MKK4 inhibitor

Chemical Structure : HRX215

CAS No.: 2369583-33-3

HRX215 (Darizmetinib, HRX-215, LN3348, HRX0215)

Catalog No.: PC-20026Not For Human Use, Lab Use Only.

Darizmetinib (HRX215, HRX0215) is a first-in-class, potent, selective inhibitor of MKK4 (mitogen-activated protein kinase kinase 4, MEK4, MAP2K4) with IC50 of 20 nM, >100-fold selectivity against JNK1, BRAF, and MKK7.

Packing	Price	Stock
5 mg	$198	In stock
10 mg	$298	In stock
25 mg	$488	In stock
50 mg	$758	In stock
100 mg		Get quote

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Biological Activity

Darizmetinib (HRX215, HRX0215) is a first-in-class, potent, selective inhibitor of MKK4 (mitogen-activated protein kinase kinase 4, MEK4, MAP2K4) with IC50 of 20 nM, >100-fold selectivity against JNK1, BRAF, and MKK7.

Darizmetinib (HRX215) (0.3-3 uM) potently reduces p-MKK4 (S257) of LPS-induces SAPK signaling via TLR4 in peripheral blood mononuclear cells (PBMCs).

Darizmetinib (HRX215) (0.4, 2, 10 mg/kg, p.o.) increases hepatocyte proliferation upon partial hepatectomy and attenuates apoptosis in a CCl4 liver damage model.

Darizmetinib (HRX215) (0.4, 2, and 10 mg/kg) reduce steatosis and inhibit fibrosis development in alcoholic steatohepatitis (ASH) model.

Darizmetinib (HRX215) shows antisteatotic efficacy in a long-term NASH-HCC model.

Darizmetinib (HRX215) (10 uM) induces growth inhibition of murine NrasG12V; Cdkn2aARF−/- and NrasG12V; Trp53−/- liver cancer cells.

Darizmetinib (HRX215) (5 mg/kg, i.v.) increases liver regeneration after 80% hepatectomy in pigs, prevents liver failure.

Physicochemical Properties

M.Wt	457.46
Formula	C21H17F2N5O3S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(2,6-difluoro-3-(5-(pyridin-4-yl)-1H-pyrazolo[3,4-b]pyridine-3-carbonyl)phenyl)propane-1-sulfonamide

References

1. Patent WO2019149738 A1.
2. Stefan Zwirner, et al. Cell. 2024 Mar 8:S0092-8674(24)00225-3.

HRX215 (Darizmetinib, HRX-215, LN3348, HRX0215)

Biological Activity

Physicochemical Properties

References

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