Doramapimod (Standard)

Doramapimod (Standard) is the analytical standard of Doramapimod. This product is intended for research and analytical applications. Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM) . Doramapimod also inhibits B-Raf with an IC50 of 83 nM[1][2].

Product Specifications

CAS Number

[285983-48-4]

Product Name Alternative

BIRB 796 (Standard)

UNSPSC

12352005

Target

Autophagy; p38 MAPK; Raf; Reference Standards

Related Pathways

Autophagy; MAPK/ERK Pathway; Others

Field of Research

Inflammation/Immunology; Cancer

Smiles

O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3

Molecular Formula

C31H37N5O3

Molecular Weight

527.66

References & Citations

[1]Dietrich J, et al. The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors. Bioorg Med Chem. 2010 Aug 1;18 (15) :5738-48|[2]Cicenas J, et al. JNK, p38, ERK, and SGK1 Inhibitors in Cancer. Cancers (Basel) . 2017 Dec 21;10 (1) . pii: E1.|[3]Kuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem, 2005, 280 (20), 19472-19479.|[4]He D, et al. BIRB796, the inhibitor of p38 mitogen-activated protein kinase, enhances the efficacy of chemotherapeutic agents in ABCB1 overexpression cells. PLoS One. 2013;8 (1) :e54181.|[5]Park JK, et al. p38 mitogen-activated protein kinase inhibition ameliorates angiotensin II-induced target organ damage. Hypertension. 2007 Mar;49 (3) :481-9.