Ralimetinib dimesylate

Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

Product Specifications

CAS Number

[862507-23-1]

Product Name Alternative

LY2228820 dimesylate

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; p38 MAPK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/LY2228820.html

Purity

99.94

Solubility

DMSO : 61 mg/mL (ultrasonic; warming) |H2O : ≥ 33.33 mg/mL

Smiles

FC1=CC=C(C=C1)C2=C(NC(C(C)(C)C)=N2)C3=NC4=C(C=C3)N=C(N)N4CC(C)(C)C.OS(C)(=O)=O.OS(C)(=O)=O

Molecular Formula

C26H37FN6O6S2

Molecular Weight

612.74

Precautions

H302, H315, H319, H335

References & Citations

[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]Campbell RM, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity. Mol Cancer Ther. 2014 Feb;13 (2) :364-74.