Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Find Your Distributors

Select Your Country or Region

 $ USD

Product Inquiry: sales@probechem.com
Order/PO receiving: order@probechem.com

You are here:Home-Chemical Inhibitors & Agonists-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-HRX215
HRX215

Chemical Structure : HRX215

CAS No.: 2369583-33-3

Add to Favorites

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 Quantity
5 mg $248 In stock
10 mg $398 In stock
25 mg $588 In stock
50 mg Get quote
100 mg Get quote
Get Quotation Now
* Please select Quantity before adding items.
 or Bulk Inquiry

Bulk size, bulk discount!

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

Purity & Documentation Purity: >98% (HPLC) Select Batch:

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.

Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

Contact Us sales@probechem.com

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • *Additional Information:

Get Quote

* Indicates a Required FieldYour information is safe with us.

  • *Product name:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Requested quantity:
  • *Country:
  • Additional Information: