SB203580

SB203580

Forskolin

Forskolin

BIRB796 (Doramapimod)

$85.00
In stock
SKU
SML16B
Description

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.

Specifications
Size10 mg
Molecular NameBIRB796 (Doramapimod)
Size10 mg
FormPowder
Alternative NamesDoramapimod, p38 MAP Kinase Inhibitor X
Chemical NameUrea, N-[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4- morpholinyl)ethoxy]-1-naphthalenyl]
Chemical FormulaC31H37N5O3
Molecular Weight527.66
CAS Number285983-48-4
Purity≥98% by NMR
Physical AppearanceWhite to gray (Solid)
Targetp38 MAPK; Raf; Autophagy
ShippingRoom Temperature
StoragePowder: -20°C for 3 years and 4°C for 2 years
Quality StatementThis product is for Research Use Only and is not intended for therapeutic or diagnostic use.
Documents
References and Publications
  • 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
  • Cicenas J, et al. JNK, p38, ERK, and SGK1 Inhibitors in Cancer. Cancers (Basel). 2017 Dec 21;10(1). pii: E1.
  • Kuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem, 2005, 280(20), 19472-19479.
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