Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 79.00 | |
2 mg | In stock | $ 123.00 | |
5 mg | In stock | $ 222.00 | |
10 mg | In stock | $ 315.00 | |
25 mg | In stock | $ 529.00 | |
50 mg | In stock | $ 768.00 | |
100 mg | In stock | $ 1,080.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 222.00 |
Description | BMS-582949 is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13 nM, inhibiting both p38 kinase activity and activation of p38. |
Targets&IC50 | p38 MAPK(Cell-free assay):13 nM |
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 | 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]. |
Kinase Assay | Autophosphorylation activity is measured by adding of 32P-γ ATP. Endonuclease activity is measured by the adding of radiolabeled HAC1 508-nt RNA substrate synthesized in vitro using α32P-UTP. Mix STF083010 with recombinant hIRE1 protein, radiolabeled HAC1 508 nt RNA, and appropriate buffers to incubate. Kinase activity is quantitated by polyacrylamide gel electrophoresis. RNAsecleavage products are quantitated by 32P-γATP or 32P-UTP autoradiography. |
Synonyms | BMS 582949, PS540446, BMS-582949 |
Molecular Weight | 406.48 |
Formula | C22H26N6O2 |
CAS No. | 623152-17-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 75 mg/mL (184.5 mM)
You can also refer to dose conversion for different animals. More
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BMS582949 623152-17-0 MAPK p38 MAPK PS-540446 BMS 582949 PS 540446 PS540446 BMS-582949 inhibitor inhibit