Doramapimod Inhibitor CAS No. 285983-48-4

Cat. No.	Name	Size	Price
KI1395	Doramapimod	10 mg	$234
	Doramapimod	50 mg	$752
	Doramapimod	100 mg	$1004
	Doramapimod	250 mg	$2352

Chemical Characteristic

Product Name	Doramapimod
Synonyms	BIRB 796
CAS No.	285983-48-4
Molecular Weight	527.66
Formula	C₃₁H₃₇N₅O₃
Chemical Name	1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea
Smiles	N(C(=O)Nc1ccc(c2ccccc12)OCCN1CCOCC1)c1n(nc(c1)C(C)(C)C)c1ccc(cc1)C
Chemical Structure

Biological activities

Doramapimod is a picomolar inhibitor of human p38 MAP kinase with K_{γ of 0.1 nM. Doramapimod inhibits TNFα in THP.1 with an IC50 of 18 nM. ^[1] Doramapimod inhibits the stress-activated protein kinases p38α and p38β. Doramapimod blocks the stress-induced phosphorylation of the scaffold protein SAP97. ^[2] Doramapimod inhibits Hsp27 phosphorylation induced by 17-AAG plus bortezomib, thereby enhancing cytotoxicity. In bone marrow stromal cells (BMSC), doramapimod inhibits phosphorylation of p38 MAPK and secretion of interleukin-6 (IL-6) and vascular endothelial growth factor triggered by either tumour necrosis factor-α or tumour growth factor-β1. ^[3] In vivo, doramapimod inhibits c-Jun N-terminal kinase (JNK) activation. ^[2]}

Protocols

In vitro: Doramapimod is dissolved in DMSO, and stored at -80 °C until use. ^[2]

References

[1] Pargellis C, et al. Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat Struct Biol. 2002, 9(4): 268-272. [2] Kuma Y, et al. BIRB796 inhibits all p38 MAPK isoforms in vitro and in vivo. J Biol Chem. 2005, 280(20): 19472-19479. [3] Yasui H, et al. BIRB 796 enhances cytotoxicity triggered by bortezomib, heat shock protein (Hsp) 90 inhibitor, and dexamethasone via inhibition of p38 mitogen-activated protein kinase/Hsp27 pathway in multiple myeloma cell lines and inhibits paracrine tumour growth. Br J Haematol. 2007, 136(3): 414-423.

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