Doramapimod, Free Base (1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea) (BIRB 796, DB03044, D03736)

Doramapimod is a protein kinase inhibitor with a >330-fold selectivity for p38 MAPK compared with 12 other protein kinases. In contrast to other p38 MAPK inhibitors (e.g., SB203580), doramapimod prevents both the kinetic activity and phosphorylation of p38 MAPK by binding to the ATP pocket as well as to a novel allosteric binding site on p38 MAPK.\n\nSolubility:\nSoluble in DMSO at 50mg/ml. Soluble in ethanol at 33mg/ml. Very poorly soluble in water. Maximum solubility in plain water is estimated to be about 5-20uM.\n\nMelting Point:\n114-142C\n\nElemental Anaylsis:\nC = 70.56%\nH = 7.07%\nN = 13.27%\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

D9023

Size

5mg

Form

Supplied as a white to off-white powder.

Purity

~90%

References

1. Branger, J., et al. \"Anti-Inflammatory Effects of a p38 Mitogen-Activated Protein Kinase Inhibitor During Human Endotoxemia.\" J. Immunol. 168:4070-4077 (2002). 2. Carter, T.A., et al. \"Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.\" Proc. Natl. Acad. Sci. USA 102:11011-11016 (2005). 3. Fabian, M.A., et al. \"A small molecule-kinase interaction map for clinical kinase inhibitors.\" Nat. Biotechnol. 23:329-336 (2005). 4. Pargellis, C., et al. \"Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site.\" Nat. Struct. Biol. 9:268-272 (2002). 5. Branger, J., et al. \"Inhibition of coagulation, fibrinolysis, and endothelial cell activation by a p38 mitogen-activated protein kinase inhibitor during human endotoxemia.\" Blood 101:4446-4448 (2003).