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Pamapimod

Catalog No. T6927   CAS 449811-01-2
Synonyms: R1503, Ro4402257

Pamapimod (R1503) (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38 gamma isoforms.

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Pamapimod Chemical Structure
Pamapimod, CAS 449811-01-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 51.00
5 mg In stock $ 122.00
10 mg In stock $ 197.00
25 mg In stock $ 397.00
50 mg In stock $ 637.00
100 mg In stock $ 897.00
500 mg In stock $ 1,790.00
1 mL * 10 mM (in DMSO) In stock $ 133.00
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Purity: 99.99%
Purity: 99.94%
Purity: 97.63%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Pamapimod (R1503) (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38 gamma isoforms.
Targets&IC50 p38β:0.48±0.04 μM, p38α:0.014 ±0.002μM
In vitro Pamapimod inhibited p38, 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[1].
In vivo In murine collagen-induced arthritis, pamapimod reduced Clinicalal 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. Pamapimod suppresses spontaneous production of TNFα by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod[1].
Synonyms R1503, Ro4402257
Molecular Weight 406.38
Formula C19H20F2N4O4
CAS No. 449811-01-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 27 mg/mL (66.4 mM)

DMSO: 75 mg/mL (184.6 mM)

TargetMolReferences and Literature

1. Hill RJ, et al. J Pharmacol Exp Ther. 2008, 327(3):610-9.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Inhibitor Library Human Metabolite Library Anti-Ovarian Cancer Compound Library Cancer Cell Differentiation Compound Library Neural Regeneration Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Fluorochemical Library Reprogramming Compound Library

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Keywords

Pamapimod 449811-01-2 Autophagy MAPK p38 MAPK Ro-4402257 Inhibitor R1503 IL-6 TNF-α inhibit IL-1β JNK R-1503 p38β Ro 4402257 Ro4402257 p38α anti-inflammation LPS R 1503 inhibitor

 

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