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Ralimetinib dimesylate
$99 – $1,045
Products Details
Product Description
– 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.
Web ID
– HY-13241
Storage Temperature
– 4°C (Powder, sealed storage, away from moisture)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C26H37FN6O6S2
Citations
– bioRxiv. 2023 Feb 8.|Cell Death Dis. 2021 Oct 23;12(11):994.|Cell Rep. 2023 Mar 20;42(3):112275.|EBioMedicine. 2015 Nov 19;2(12):1944-56. |Harvard Medical School LINCS LIBRARY|Mol Med Rep 2019 Jul;20(1):735-744.|Nat Commun. 2021 Dec 3;12(1):6941.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Cell Biol Int. 2019 Jul 19.|Commun Biol. 2022 Dec 20;5(1):1391.|Eur J Immunol. 2020 Sep;50(9):1350-1361.|Glia. 2020 Jan;68(1):27-43.
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]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.|[3]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.
CAS Number
– 862507-23-1
Molecular Weight
– 612.74
Compound Purity
– 99.91
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
Clinical Information
– Phase 2
Research Area
– Cancer; Inflammation/Immunology
Solubility
– DMSO : 61 mg/mL (ultrasonic;warming)|H2O : ≥ 33.33 mg/mL
Target
– Apoptosis;Autophagy;p38 MAPK
Isoform
– p38α;p38β
Pathway
– Apoptosis;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. Agdia Products are available for delivery only in Canada.
