2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy
  4. Pamapimod

Pamapimod  (Synonyms: Ro4402257; R1503)

Cat. No.: HY-10405 Purity: 99.92%
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Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.

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

Pamapimod Chemical Structure

Pamapimod Chemical Structure

CAS No. : 449811-01-2

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10 mM * 1 mL in DMSO
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10 mg USD 240 In-stock
25 mg USD 480 In-stock
50 mg USD 768 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Pamapimod:

Pamapimod 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

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1].

IC50 & Target[1]

p38α

14 nM (IC50)

p38α

1.3 nM (Ki)

p38β

480 (IC50)

p38β

120 nM (Ki)

In Vitro

Pamapimod binds to JNK kinases with Ki values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively[1].
After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC50 of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC50 values of 0.40 and 0.10 μM, respectively[1].

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

Pamapimod Related Antibodies
In Vivo

Pamapimod (0-150 mg/kg; oral gavage; once daily; DBA/1J female mice) treatment reduces inflammation and bone loss in murine collagen-induced arthritis[1].

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

Animal Model: DBA/1J female mice (8-10 weeks of age) induced murine collagen[1]
Dosage: 0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 90 mg/kg, 150 mg/kg
Administration: Oral gavage; once daily
Result: Reduced inflammation and bone loss.
Molecular Weight

406.38

Formula

C19H20F2N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C
Shipping

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

DMSO : ≥ 34 mg/mL (83.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4608 mL 12.3038 mL 24.6075 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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

Purity: 99.92%

COA (247 KB) LCMS (123 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4608 mL 12.3038 mL 24.6075 mL 61.5188 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL 12.3038 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 mL 6.1519 mL
15 mM 0.1641 mL 0.8203 mL 1.6405 mL 4.1013 mL
20 mM 0.1230 mL 0.6152 mL 1.2304 mL 3.0759 mL
25 mM 0.0984 mL 0.4922 mL 0.9843 mL 2.4608 mL
30 mM 0.0820 mL 0.4101 mL 0.8203 mL 2.0506 mL
40 mM 0.0615 mL 0.3076 mL 0.6152 mL 1.5380 mL
50 mM 0.0492 mL 0.2461 mL 0.4922 mL 1.2304 mL
60 mM 0.0410 mL 0.2051 mL 0.4101 mL 1.0253 mL
80 mM 0.0308 mL 0.1538 mL 0.3076 mL 0.7690 mL
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Pamapimod 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:

Pamapimod449811-01-2Ro4402257 R1503Ro 4402257Ro-4402257R1503R 1503R-1503p38 MAPKAutophagyp38αp38βanti-inflammationRATNF-αIL-6LPSJNKIL-1βInhibitorinhibitorinhibit

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