2. MAPK/ERK Pathway NF-κB Apoptosis
  3. p38 MAPK JNK NF-κB MDM-2/p53
  4. Darizmetinib

Darizmetinib  (Synonyms: HRX-0215)

Cat. No.: HY-152860 Purity: 99.94%
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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.

For research use only. We do not sell to patients.

Darizmetinib Chemical Structure

Darizmetinib Chemical Structure

CAS No. : 2369583-33-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 471 In-stock
Solution
10 mM * 1 mL in DMSO USD 471 In-stock
Solid
5 mg USD 468 In-stock
10 mg USD 750 In-stock
25 mg USD 1560 In-stock
50 mg USD 2500 In-stock
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Based on 1 publication(s) in Google Scholar

Darizmetinib Related Antibodies

Top Publications Citing Use of Products

View All p38 MAPK Isoform Specific Products:

View All Isoforms
p38 MAPK p38α p38β MAPK13 p38δ p38γ

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JNK1 JNK2 JNK3 JNK

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

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].

In Vitro

Darizmetinib (0.3, 1,3 μM, 2 h) reduces lipopolysaccharide (LPS) (HY-D1056)-induced pMKK4 levels in peripheral blood mononuclear cells (PBMCs)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Darizmetinib Related Antibodies

Western Blot Analysis[3]

Cell Line: PBMCs
Concentration: 0.3, 1,3 μM
Incubation Time: 2 h
Result: Reduced pMKK4 levels in a potent and dose-dependent manner in PBMCs, confirming cell membrane permeability.
In Vivo

Darizmetinib (30 mg/kg, p.o., a single dose for 15 min-24 h) increases the number of proliferating hepatocytes upon partial hepatectomy in fibrotic mouse livers [3].
Darizmetinib (10 mg/kg, p.o., a single dose for 2 h and 9 h) activates pro-regenerative program by increaseing MKK7 and JNK1 signaling with a downstream activation of the transcription factors ATF2 and ELK1, reduces p38- and p53 activation, activates nuclear factor κB (NF-κB) signaling, and upregulates the anti-apoptotic protein Bcl-XL in hepatectomized mice[3].
Darizmetinib (5 mg/kg, i.v., every 12 h, starting 24 h before surgery)--mediated suppression of MKK4 increases hepatocyte regeneration in a pig hepatectomy model[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: partial hepatectomy in fibrotic mouse livers[2]
Dosage: 30 mg/kg
Administration: p.o., a single dose for 15 min-24 h
Result: Enhanced hepatocyte proliferation in partial hepatectomy in fibrotic mouse livers, suggesting that the presence of fibrosis per se does not interfere with the Darizmetinib-mediated pro-regenerative mechanism.
Molecular Weight

457.45

Formula

C21H17F2N5O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 175 mg/mL (382.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1860 mL 10.9302 mL 21.8603 mL
5 mM 0.4372 mL 2.1860 mL 4.3721 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.94%

SDS (252 KB)

COA (250 KB) HNMR (290 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1860 mL 10.9302 mL 21.8603 mL 54.6508 mL
5 mM 0.4372 mL 2.1860 mL 4.3721 mL 10.9302 mL
10 mM 0.2186 mL 1.0930 mL 2.1860 mL 5.4651 mL
15 mM 0.1457 mL 0.7287 mL 1.4574 mL 3.6434 mL
20 mM 0.1093 mL 0.5465 mL 1.0930 mL 2.7325 mL
25 mM 0.0874 mL 0.4372 mL 0.8744 mL 2.1860 mL
30 mM 0.0729 mL 0.3643 mL 0.7287 mL 1.8217 mL
40 mM 0.0547 mL 0.2733 mL 0.5465 mL 1.3663 mL
50 mM 0.0437 mL 0.2186 mL 0.4372 mL 1.0930 mL
60 mM 0.0364 mL 0.1822 mL 0.3643 mL 0.9108 mL
80 mM 0.0273 mL 0.1366 mL 0.2733 mL 0.6831 mL
100 mM 0.0219 mL 0.1093 mL 0.2186 mL 0.5465 mL
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Darizmetinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Darizmetinib2369583-33-3HRX-0215HRX0215HRX 0215p38 MAPKJNKNF-κBMDM-2/p53c-Jun N-terminal kinaseNuclear factor-κBNuclear factor-kappaBorally activeMKK4MKK7JNK1ATF2ELK1liver failureInhibitorinhibitorinhibit

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