Product Description
BIRB796 (Doramapimod) is a pyrazole-based allosteric inhibitor of p38 MAP Kinase with a Kd of 0.1 nM. BIRB796 has slow binding kinetics, as evidenced by an marked increase in apparent IC50 after preincubation periods up to 2h, as well as dissociation rates of up to six orders of magnitude greater when compared to other MAPK inhibitors. (1) BIRB796 possesses an excellent selectivity profile over a panel of relevant kinases, with the most active being inhibition of JNK2a2 at 100 nM (330-fold selectivity). (2)Related studies have shown that BIRB796 also inhibits activity and activation of SAPK3/p38g (3% remaining activity at 10 uM). At these concentrations, BIRB796 blocks stress-induced phosphorylation of scaffold protein SAP97. (3)
Technical information:
| Chemical Formula: | C31H37N5O3 | |
| CAS #: | 285983-48-4 | |
| Molecular Weight: | 527.66 | |
| Purity: | > 98% | |
| Appearance: | White | |
| Chemical Name: | 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(2-morpholinoethoxy)naphthalen-1-yl)urea - See more at: http://www.selleckchem.com/products/BIRB-796-(Doramapimod).html#sthash.FpSrDH3J.dpuf | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | BIRB796, BIRB 796, Doramapimod |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Pargellis et al., Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol. 2002, 9(4), 268-272. Pubmed ID: 11896401 |
| 2. | Regan et al., Pyrazole Urea-Based Inhibitors of p38 MAP Kinase: From Lead Compound to Clinical Candidate. J. Med. Chem. 2002, 45, 2994-3008. Pubmed ID: 12086485 |
| 3. | Kuma et al., BIRB796 Inhibits All p38 MAPK Isoforms in Vitro and in Vivo. J. Biol. Chem. 2005, 280(20), 19472-19479. Pubmed ID: 15755732 |
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