1. MAPK/ERK Pathway
  2. MAPKAPK2 (MK2)
  3. Zunsemetinib

Zunsemetinib  (Synonyms: ATI-450; CDD-450)

Cat. No.: HY-139553 Purity: 99.37% ee.: 100.00%
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Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.

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

Zunsemetinib Chemical Structure

Zunsemetinib Chemical Structure

CAS No. : 1640282-42-3

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1 mg USD 340 In-stock
5 mg USD 850 In-stock
10 mg USD 1450 In-stock
25 mg USD 2800 In-stock
50 mg USD 4200 In-stock
100 mg USD 6280 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1].

IC50 & Target

MK2[1]

In Vitro

Zunsemetinib (1 and 10 μM; 1 hour; WT and NOM ID BMMs) has no effect on NLRP3 expression, but decreases IL-1β expression by promoting IL-1β mRNA degradation[1].
Zunsemetinib (0.4 nM~1 μM; 16 hours; PBMC) reduces IL-1β secretion and promotes IL-1β mRNA instability[1].
Zunsemetinib selectively blocks p38α MAPK activation of the proinflammatory kinase MK2 while sparing p38α activation of other effectors such as PRAK and ATF2. Zunsemetinib inhibits in vitro osteoclast formation induced by RANKL[1].

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

RT-PCR[1]

Cell Line: WT and NOM ID BMMs
Concentration: 1 and 10 μM
Incubation Time: 1 hour
Result: Had no effect on NLRP3 expression, but decreased IL-1β expression by promoting IL-1β mRNA degradation.
In Vivo

Zunsemetinib (1,000 ppm; p.o.) blocks LPS-induced TNF-α expression persisted for up to 4 weeks after dosing[1].
Zunsemetinib (10 and 20 mg/kg; p.o.) increases bone density[1].
Zunsemetinib prevents osteopenia in NOM IDc mice through inhibition of osteoclastogenesis[1].

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

Animal Model: 8-week-old WT female mice[1]
Dosage: 1,000 ppm
Administration: P.o.
Result: Blocked LPS-induced TNF-α expression persisted for up to 4 weeks after dosing.
Animal Model: Rats[1]
Dosage: 10 and 20 mg/kg
Administration: P.o.
Result: Increased bone density.
Molecular Weight

513.92

Formula

C25H22ClF2N5O3

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

FC1=CC(F)=CN=C1COC2=C(Cl)C(N(C3=CC(C4=NC(C(C)(C)O)=NC=C4)=NC=C3C)C(C)=C2)=O

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 : 100 mg/mL (194.58 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 1.9458 mL 9.7291 mL 19.4583 mL
5 mM 0.3892 mL 1.9458 mL 3.8917 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:

Dosage

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 1.9458 mL 9.7291 mL 19.4583 mL 48.6457 mL
5 mM 0.3892 mL 1.9458 mL 3.8917 mL 9.7291 mL
10 mM 0.1946 mL 0.9729 mL 1.9458 mL 4.8646 mL
15 mM 0.1297 mL 0.6486 mL 1.2972 mL 3.2430 mL
20 mM 0.0973 mL 0.4865 mL 0.9729 mL 2.4323 mL
25 mM 0.0778 mL 0.3892 mL 0.7783 mL 1.9458 mL
30 mM 0.0649 mL 0.3243 mL 0.6486 mL 1.6215 mL
40 mM 0.0486 mL 0.2432 mL 0.4865 mL 1.2161 mL
50 mM 0.0389 mL 0.1946 mL 0.3892 mL 0.9729 mL
60 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8108 mL
80 mM 0.0243 mL 0.1216 mL 0.2432 mL 0.6081 mL
100 mM 0.0195 mL 0.0973 mL 0.1946 mL 0.4865 mL
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Zunsemetinib 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.

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