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Ralimetinib

Ralimetinib (LY2228820) is a potent and 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 p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc[1].

Product Specifications

CAS Number

862505-00-8

Product Name Alternative

LY2228820

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; p38 MAPK

Type

Reference compound

Related Pathways

Autophagy; MAPK/ERK Pathway

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

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

Purity

98.58

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

NC1=NC2=CC=C(C3=C(C4=CC=C(F)C=C4)N=C(C(C)(C)C)N3)N=C2N1CC(C)(C)C

Molecular Formula

C24H29FN6

Molecular Weight

420.53

Precautions

H302, H315, H319, H335

References & Citations

[1]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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

P38α; p38β

Citation 01

Cell Biol Int. 2020 Jan;44 (1) :89-97.|Commun Biol. 2022 Dec 20;5 (1) :1391.|Eur J Immunol. 2020 Sep;50 (9) :1350-1361.|Glia. 2020 Jan;68 (1) :27-43.|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 Cell Biol. 2025;45 (3) :99-115.|Mol Med Rep. 2019 Jul;20 (1) :735-744.|Nat Commun. 2021 Dec 3;12 (1) :6941.|Res Sq. 2025 Apr 15.|Sci Transl Med. 2018 Jul 18;10 (450) :eaaq1093.

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