製品番号: HY-13241

Ralimetinib dimesylate

(別名: LY2228820 dimesylate)

17 Cited Publications

カスタマーレビュー

Based on 17 publication(s) in Google Scholar

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.

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純度: 99.97%
CAS 番号: 862507-23-1
分子式: C₂₆H₃₇FN₆O₆S₂
分子量:612.74

保管条件:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Ralimetinib dimesylate 構造式

CAS 番号: 862507-23-1

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Amount: USD 0.00

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (17)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[3]

p38β MAPK

3.2 nM (IC₅₀)

p38α MAPK

5.3 nM (IC₅₀)

p38 MAPK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	56.2 μM Compound: LY2228820	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	0.87 μM Compound: LY2228820	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1

体外実験

Ralimetinib dimesylate 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 dimesylate inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC₅₀ of 5.2 nM^[1]. In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, Ralimetinib dimesylate (LY2228820) (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 dimesylate (200 nM-400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but Ralimetinib dimesylate alone doesn't inhibit the growth of MM.1S cells. Ralimetinib dimesylate (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 dimesylate (400 nM-800 nM) also blocks osteoclastogenesis from CD14⁺ cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

In LPS-induced mice, Ralimetinib dimesylate 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 dimesylate displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED₅₀)of 1.5 mg/kg^[1]. Ralimetinib dimesylate inhibits tumor phospho-MK2 in a dose-dependent manner (TED₅₀=1.95 mg/kg, TED₇₀=11.17 mg/kg) in mice implanted with B16-F10 melanoma. Ralimetinib dimesylate inhibits MK2 phosphorylation: mouse in vivo TED₅₀=1.01 mg/kg (compound exposure approximately 100 nM) and human ex vivo IC₅₀=0.12 μM with either mouse or human PBMC^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 862507-23-1
性状 Solid
分子量 612.74
分子式 C₂₆H₃₇FN₆O₆S₂
Color White to yellow
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
別名

LY2228820 dimesylate
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Publications (17)

All Cell Proliferation/Viability AssayELISAWB

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Journal Impact Factor

Nat Commun

Inhibition of cytoplasmic EZH2 induces antitumor activity through stabilization of the DLC1 tumor suppressor protein. [Abstract]

2021 Dec 3;12(1):6941. PMID: 34862367
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Death Dis

Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]

2021 Oct 23;12(11):994. PMID: 34689152

Ralimetinib dimesylate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Oct 23;12(11):994. [Abstract]

HT-29 cells were transfected with an expression vector of flag-tagged MLKL fused with two AP20187 (10 μM)-binding (FKBPv) domains. The cells were pretreated with indicated compounds (Ralimetinib dimesylate (LY2228820, 10 μM), et al.) for 4 h followed by treatment with AP20187 to induce MLKL oligomerization. Cell viability was determined by CellTiter-Glo after treatment with AP20187 for 2 h (Left). Cell lysates were separated by non-reducing SDS/PAGE and analyzed by western blotting using MLKL antibody (Right).
EBioMedicine

PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. [Abstract]

2015 Nov 19;2(12):1944-56. PMID: 26844273

Ralimetinib dimesylate purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2015 Nov 19;2(12):1944-56. [Abstract]

CRC cells were treated with 4 μM Ralimetinib dimesylate (LY2228820), 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.
Oncogene

ULK1 promotes metastatic progression in experimental models of epithelial ovarian cancer. [Abstract]

2026 Mar 5. PMID: 41786876

Ralimetinib dimesylate purchased from MedChemExpress. Usage Cited in: Oncogene. 2026 Mar 5. [Abstract]

Spheroids were cultured for 24 h before treating with either AKTi-1/2 (5 µM) or Ralimetinib dimesylate (15 µM) for 72 h before performing Trypan Blue Exclusion Assay. Treatment with AKTi-1/2 (AKT inhibitor) and Ralimetinib dimesylate (p38 inhibitor) resulted in significantly increased cell viability in OVCAR8-ULK1KO spheroids, while no differences were observed in HEYA8-ULK1KO spheroids.
Cell Rep

VEGFR2 inhibition potentiates STING-mediated antitumor immunity. [Abstract]

2026 Jun 18;45(7):117576. PMID: 42313565
Cell Rep

Pharmacological boosting of cGAS activation sensitizes chemotherapy by enhancing antitumor immunity. [Abstract]

2023 Mar 20;42(3):112275. PMID: 36943864
Commun Biol

Dickkopf1 fuels inflammatory cytokine responses. [Abstract]

2022 Dec 20;5(1):1391. PMID: 36539532
Glia

Activation of G protein-coupled receptor 30 protects neurons by regulating autophagy in astrocytes. [Abstract]

2020 Jan;68(1):27-43. PMID: 31429156
Mol Med Rep

MicroRNA‑22 alleviates inflammation in ischemic stroke via p38 MAPK pathways. [Abstract]

2019 Jul;20(1):735-744. PMID: 31115561

Ralimetinib dimesylate purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jul;20(1):735-744. [Abstract]

p38 inhibitor Ralimetinib dimesylate (p38 i, 3 nM; 24 h) reduced the proinflammatory effects of Anti-22 in model in vitro. p-p38, NF-κB, COX-2 and iNOS protein expression was determined by western blotting and statistically analyzed.

Ralimetinib dimesylate purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jul;20(1):735-744. [Abstract]

p38 inhibitor Ralimetinib dimesylate (p38 i, 3 nM; 24 h) reduced the proinflammatory effects of Anti-22 in the in vitro stroke model. TNF-α, IL-1β, IL-6, IL-18, MIP-2 and PGE2 expression was determined by ELISA.
Toxics

Co-Exposure of Microplastics and Avermectin at Environmental-Related Concentrations Caused Severe Heart Damage Through ROS-Mediated MAPK Signaling in Larval and Adult Zebrafish. [Abstract]

2025 Dec 25;14(1):24. PMID: 41600573
Med Oncol

P38MAPK targeting in pancreatic ductal adenocarcinoma: Promising interventional approach for breaking drug resistance and tumor control. [Abstract]

2026 Jun 3;43(7):191. PMID: 42234045
Eur J Immunol

Neutralization of IL-10 produced by B cells promotes protective immunity during persistent HCV infection in humanized mice. [Abstract]

2020 Sep;50(9):1350-1361. PMID: 32339264
Cell Biol Int

Lipopolysaccharide inhibits GPR120 expression in macrophages via Toll-like receptor 4 and p38 MAPK activation. [Abstract]

2020 Jan;44(1):89-97. PMID: 31322778
Mol Cell Biol

Kinase Inhibitor-Induced Cell-Type Specific Vacuole Formation in the Absence of Canonical ATG5-Dependent Autophagy Initiation Pathway. [Abstract]

2025;45(3):99-115. PMID: 39895059
Res Sq

2025 Apr 15.
bioRxiv

2023 Feb 8.

溶剤 & 溶解度

体外:

DMSO : 61 mg/mL (99.55 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 33.33 mg/mL (54.40 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6320 mL

8.1601 mL

16.3201 mL

5 mM

0.3264 mL

1.6320 mL

3.2640 mL

10 mM

0.1632 mL

0.8160 mL

1.6320 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

プロトコル

Kinase Assay^[1]

Inhibition of p38α is determined using recombinant human p38α in a standard filter binding protocol using ATP[γ-³³P] and EGFR 21-mer peptide as substrate. Functional inhibition of TNFα in murine peritoneal macrophages is determined using LPS stimulation in the presence of Ralimetinib. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with Ralimetinib and then stimulated with anisomycin. The level of p38α activity is detected using a phosphoMAPKAPK-2 (pMK2) (Thr 334) antibody which reacts with a residue specifically phosphorylated by p38α.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Murine B16-F10 melanoma cells are cultured in Dulbecco's Modified Eagle Medium supplemented with l-glutamine, high glucose and 10% FBS (GIBCO 11965-092). C57/bl6 mice are implanted in the rear flank with B16-F10 cells (2×10⁶), and when tumors reach approximately 200 mm³ in size, are dosed orally with Ralimetinib dimesylate in 1% carboxymethylcellulose/0.25% Tween 80. Two hours postdose, tumors are excised, homogenized, and lysed for Western blot analysis. MK2 phosphorylation (p-Thr334), normalized to total glyceraldehyde-3-phosphate dehydrogenase, is quantified by chemiluminescent detection. The 50% or 70% threshold effective dose (TED₅₀ and TED₇₀, respectively) is calculated to approximate effective dose ranges for testing of Ralimetinib dimesylate in xenograft models, that is, where significant target inhibition is observed. The TED₅₀ or TED₇₀ is defined as the dose where a statistically significant effect is achieved, and there is at least 50% or 70% inhibition, respectively, compared with vehicle control.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.6320 mL	8.1601 mL	16.3201 mL	40.8003 mL
	5 mM	0.3264 mL	1.6320 mL	3.2640 mL	8.1601 mL
	10 mM	0.1632 mL	0.8160 mL	1.6320 mL	4.0800 mL
	15 mM	0.1088 mL	0.5440 mL	1.0880 mL	2.7200 mL
	20 mM	0.0816 mL	0.4080 mL	0.8160 mL	2.0400 mL
	25 mM	0.0653 mL	0.3264 mL	0.6528 mL	1.6320 mL
	30 mM	0.0544 mL	0.2720 mL	0.5440 mL	1.3600 mL
	40 mM	0.0408 mL	0.2040 mL	0.4080 mL	1.0200 mL
	50 mM	0.0326 mL	0.1632 mL	0.3264 mL	0.8160 mL
DMSO	60 mM	0.0272 mL	0.1360 mL	0.2720 mL	0.6800 mL
DMSO	80 mM	0.0204 mL	0.1020 mL	0.2040 mL	0.5100 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Ralimetinib dimesylate

17 Cited Publications

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Ralimetinib dimesylate

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MedChemExpress（MCE）の使用を引用している文献 Ralimetinib dimesylate

p38 MAPK アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (17)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Ralimetinib dimesylate 関連分類

HY-13241 関連分類