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

Pamapimod (Synonyms: Ro4402257; R1503)

Cat. No.: HY-10405 Purity: 99.92%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2040 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.

449811-01-2

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (83.67 mM)

*"≥" 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
10 mM 0.2461 mL 1.2304 mL 2.4608 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

PamapimodRo4402257R1503Ro 4402257Ro-4402257R 1503R-1503p38 MAPKAutophagyp38αp38βanti-inflammationRATNF-αIL-6LPSJNKIL-1βInhibitorinhibitorinhibit

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Pamapimod
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