SB203580

SB203580

Forskolin

Forskolin

BIRB796 (Doramapimod)

BIRB796 is a highly potent inhibitor of p38 MAPK that enhances stem cell activity of cultured umbilical cord blood-derived hematopoietic cells (Baudet et al.). Powder, 10 mg
$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.

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

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
  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.
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