Home MAPK p38 MAPK inhibitor BMS-582949 For research use only.

BMS-582949

Synonyms: PS540446

BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.

BMS-582949 Chemical Structure

BMS-582949 Chemical Structure

CAS No. 623152-17-0

Purity & Quality Control

Batch: S812401 DMSO]81 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.05%
99.05

BMS-582949 Related Products

Signaling Pathway

p38 MAPK Signaling Pathways

p38 MAPK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Caco2 Function assay 2 hrs Drug level in apical and basal side of human Caco2 cells assessed as BMS-582949 level incubated at 37 degC for 2 hrs 17292610
Click to View More Cell Line Experimental Data

Biological Activity

Description BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
Targets
p38 MAPK [1]
(Cell-free assay)
13 nM
In vitro
In vitro BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop[2].
In Vivo
In vivo The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00162292 Completed
Rheumatoid Arthritis
Bristol-Myers Squibb
 November 2005 Phase 1

Chemical Information & Solubility

Molecular Weight 406.48 Formula

C22H26N6O2
CAS No. 623152-17-0 SDF Download BMS-582949 SDF
Smiles CCCNC(=O)C1=CN2C(=C1C)C(=NC=N2)NC3=C(C=CC(=C3)C(=O)NC4CC4)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (199.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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