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Doramapimod

$41$363

Products Details

Product Description

– 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].

Web ID

– HY-10320

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– COVID-19-immunoregulation

Molecular Formula

– C31H37N5O3

References

– [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]Park JK, et al. p38 mitogen-activated protein kinase inhibition ameliorates angiotensin II-induced target organ damage. Hypertension. 2007 Mar;49(3):481-9.|[5]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.

CAS Number

– 285983-48-4

Molecular Weight

– 527.66

Compound Purity

– 99.98

SMILES

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

Clinical Information

– Phase 2

Research Area

– Inflammation/Immunology; Cancer

Solubility

– DMSO : 125 mg/mL (ultrasonic)|Ethanol : 33.33 mg/mL (ultrasonic)

Target

– Autophagy;p38 MAPK;Raf

Isoform

– BRaf;p38 MAPK;p38α;p38β;p38γ;p38δ

Pathway

– Autophagy;MAPK/ERK Pathway

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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