Ralimetinib dimesylate

SKU: orb1301121

Description

Ralimetinib dimesylate (LY2228820 dimesylate) is an orally bioavailable, tri-substituted imidazole inhibitor of p38 MAPK. It has demonstrated potential anti-inflammatory and anti-cancer activity in preclinical in vitro and in vivo models, supporting research in oncology and inflammatory disease.

Research Area

Cell Biology, Signal Transduction

Images & Validation

−

Key Properties

−

CAS Number	862507-23-1
MW	612.74
Purity	99.38%
Formula	C₂₄H₂₉FN₆·2CH₄O₃S
SMILES	CS(O)(=O)=O.CS(O)(=O)=O.CC(C)(C)Cn1c(N)nc2ccc(nc12)-c1[nH]c(nc1-c1ccc(F)cc1)C(C)(C)C
Target	Autophagy,p38 MAPK,Apoptosis
Solubility	DMSO:27.5 mg/mL (44.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.26 mM)

Bioactivity

−

Target IC50	p38β MAPK:3.2 nM\|p38α:7 nM
In Vivo	In LPS-induced mice, Ralimetinib effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED50) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), Ralimetinib displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED50)of 1.5 mg/kg. Read more...
In Vitro	Ralimetinib inhibits p38α, as well as the level of phosphoMAPKAPK-2 (pMK2) in RAW 264.7 cells, with IC50 values of 7 nM and 34.3 nM, respectively. Furthermore, Ralimetinib inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC50 of 5.2 nM. In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, Ralimetinib (200 nM–800 nM) significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. Ralimetinib (200 nM–400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but Ralimetinib alone doesn't inhibit the growth of MM.1S cells. Ralimetinib (200 nM–800 nM) also inhibits secretion of IL-6 and MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138+, CD138 or PB CD14+ cells. Ralimetinib (400 nM–800 nM) also blocks osteoclastogenesis from CD14+ cells. Read more...
Cell Research	MTT assays and APO 2.7 staining are performed to assess cellular proliferation and induction of apoptosis, respectively. Viability is expressed as percent viable cells. Apoptosis in cells is evaluated by APO 2.7 staining. For detection of mitochondrial membrane protein 7A6 expressed in apoptotic cells, cells are incubated with APO 2.7 reagent for 20 min. Expression of APO 2.7 is determined using an EPICS XL flow cytometer.(Only for Reference) Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

Autophagy, Apoptosis, LY 2228820, LY 2228820 Dimesylate, LY-2228820, LY2228820 dimesylate, LY-2228820 Dimesylate, p38α, p38MAPK, p38 MAPK

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID

11570805 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols