LY2228820 Inhibitor CAS No. 862507-23-1

Cat. No.	Name	Size	Price	Add Cart
KI0260	LY2228820	25 mg	$1336.5

Chemical Characteristic

Product Name	LY2228820
CAS No.	862507-23-1
Molecular Weight	612.74
Formula	C₂₆H₃₇FN₆O₆S₂
Chemical Name	5-(2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-neopentyl-3H-imidazo[4,5-b]pyridin-2-amine dimethanesulfonate
Smiles	c12c(ccc(n1)c1nc([nH]c1c1ccc(cc1)F)C(C)(C)C)nc(n2CC(C)(C)C)N CS(=O)(=O)O CS(=O)(=O)O
Chemical Structure

Biological activities

LY2228820 is a novel p38 mitogen-activated protein kinase (p38MAPK) inhibitor. LY2228820 inhibits p38a , Macrophage TNFa , cELISA pMK2 with IC50s of 7.0, 5.2 and 34.3 nM, respectively.^[1] LY2228820 inhibits p38aMAPK and p38βMAPK with IC50s of 7 and 3 nM, respectively, while for p38δMAPK, p38gMAPK and a panel of 172 additional kinases, the IC50s of LY2228820 are more than 20 µM. LY2228820 significantly enhances the toxicity of bortezomib by down-regulating bortezomib-induced heat shock protein 27 phosphorylation. LY2228820 inhibits interleukin-6 secretion from long term cultured-BM stromal cells and BM mononuclear cells. LY2228820 also inhibits macrophage inflammatory protein-1a secretion, as well as normal CD14⁺ positive osteoclast precursor cells. LY2228820 represents a promising novel targeted approach to improve multiple myeloma outcome both by enhancing the effect of bortezomib and by reducing osteoskeletal events.^[2] At the same time, LY2228820 is very permeable at the blood-brain barrier (BBB), and LY2228820 decreases at least 4-fold in Bcrp-expressing cells because of active efflux. In vitro, LY2228820 significantly inhibits osteoclastogenesis from CD14+ positive cells induced by macrophage-colony stimulating factor and soluble receptor activator of nuclear factor-κB ligand. In vivo, LY2228820 also inhibits osteoclatogenesis in a severe combined immunodeficiency mouse model of human MM.^[2] Brain uptake of LY2228820 is almost perfusion flow rate-limited in mdr1a (-/-) mice. In mdr1a (+/+) mice, LY2228820 brain uptake decreases nearly 60%, as LY2228820 brain uptake is not limited by Bcrp.^[3] In the SCID-hu murine model of human MM, LY2228820 significantly inhibits osteoclastogenesis.^[2]

References

[1] Mader M, et al. Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38alpha MAP kinase inhibitors with excellent in vivo antiinflammatory properties. Bioorg Med Chem Lett. 2008, 18(1): 179-183. [2] Ishitsuka K, et al. p38 mitogen-activated protein kinase inhibitor LY2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications. Br J Haematol. 2008, 141(5): 598-606. [3] Zhao R, et al. Breast cancer resistance protein interacts with various compounds in vitro, but plays a minor role in substrate efflux at the blood-brain barrier. Drug Metab Dispos. 2009, 37(6): 1251-1258.

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