BIRB796 (Doramapimod)

BIRB796 (Doramapimod) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38 β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. BIRB796 has picomolar affinity for p38 kinase (Kd=0.1 nM) and inhibits B-Raf with an IC50 of 83 nM1,2. BIRB796 is usually associated with inflammation because of its role in T-cell proliferation and cytokine production. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97, further establishing that this is a physiological substrate of SAPK3/p38γ. The binding of Doramapimod to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4.

In research applications, BIRB796 has been shown to rescue the self-renewal ability of muscle satellite cells (Bernet et al.), increase the regenerative capacity of functional aged skeletal muscle stem cells (Cosgrove et al.), and block GADD45G-induced differentiation of long-term repopulating hematopoietic stem cells (Thalheimer et al.).

Description: High affinity and selective p38 kinase inhibitor
Alternative Names: Doramapimod, p38 MAP Kinase Inhibitor X
Chemical Name: Urea, N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4- morpholinyl)ethoxy]-1-naphthalenyl]
Purity: ≥ 98% by NMR

Features & Benefits

• High quality guaranteed
• Low price and fast delivery
• Third-party tested and validated
• High purity and consistent activity

Documents

• BIRB796 Technical Data Sheet
• Brochure: Small Molecules for Stem Cell Research
• FAQs: General Guide for Small Molecules

References and Publications

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.