1. MAPK/ERK Pathway
  2. p38 MAPK

Pamapimod (Synonyms: Ro4402257; R1503)

Cat. No.: HY-10405 Purity: 99.86%
Handling Instructions

Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor.

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 418 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 144 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 468 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 1680 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pamapimod is a novel p38 mitogen-activated protein kinase inhibitor. Pamapimod inhibited p38α and p38β enzymatic activity, with IC50 values of 0.014 ± 0.002 and 0.48 ± 0.04 μM, respectively. Pamapimod is p38 inhibitor with IC50 of 0.06μM in THP-1 cell. IC50: 0.014 ± 0.002 and 0.48 ± 0.04 μM(p38α and p38β enzymatic activity,respectively.) IC50:0.06μM (THP-1 cell)[1] In vitro: Pamapimod inhibited p38α and p38β enzymatic activity, with IC50 values of 0.014 ± 0.002 and 0.48 ± 0.04 μM, respectively. There was no activity against p38δ or p38γ isoforms. When profiled across 350 kinases, pamapimod bound only to four kinases in addition to p38. Cellular potency was assessed using phosphorylation of heat shock protein-27 and c-Jun as selective readouts for p38 and c-Jun NH2-terminal kinase (JNK), respectively. Pamapimod inhibited p38 (IC50, 0.06 μM), but inhibition of JNK was not detected.Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod. [1] In vivo: In murine collagen-induced arthritis, pamapimod reduced clinical signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation. Finally, an analog of pamapimod that has equivalent potency and selectivity inhibited renal disease in lupus-prone MRL/lpr mice. [1]

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
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Pamapimod
Cat. No.:
HY-10405
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Pamapimod

Cat. No.: HY-10405