Doramapimod

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

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; p38 MAPK; Raf

Type

Reference compound

Related Pathways

Autophagy; MAPK/ERK Pathway

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/Doramapimod.html

Purity

99.98

Solubility

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 33.33 mg/mL (ultrasonic)

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

Precautions

H302, H315, H319, H335

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.