Catalog No.S1494

LY2228820 is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.

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LY2228820 Chemical Structure

LY2228820 Chemical Structure
Molecular Weight: 612.74

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Related Compound Libraries

LY2228820 is available in the following compound libraries:

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Product Information

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  • Research Area
  • Inhibition Profile

Product Description

Biological Activity

Description LY2228820 is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
Targets p38α [1]
(Cell-free assay)
IC50 7 nM
In vitro LY2228820 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, LY2228820 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, 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. LY2228820 (200 nM–400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but LY2228820 alone doesn't inhibit the growth of MM.1S cells. LY2228820 (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. LY2228820 (400 nM–800 nM) also blocks osteoclastogenesis from CD14+ cells. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
mouse peritoneal macrophagesMXTGeY5kfGmxbjDhd5NigQ>?M4r3UJ4zOCEQvF2=NEf3dY5FVVORNWjV[WNjVFCVL1nGUk3Pu+LCk4P0bY12dGG2ZXSgWG5HNc7zIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDZwMzDuUS=>Mnv3NlQ{PTZ6MUS=

... Click to View More Cell Line Experimental Data

In vivo In LPS-induced mice, LY2228820 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), LY2228820 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]

Protocol(Only for Reference)

Kinase Assay: [1]

Inhibition of p38α 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 LY2228820. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with LY2228820 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.

Cell Assay: [2, 3]

Cell lines MM cells, including INA6, RPMI-8226, U266, and RPMI-Dox40
Concentrations 200 nM–800 nM
Incubation Time 48 hours
Method 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.

Animal Study: [1]

Animal Models Lipopolysaccharide (LPS)-induced Balb/c mice
Formulation Dissolved in 1% CMC/0.25% Tween 80 in water
Dosages 0–20 mg/kg
Administration Oral bid dosing for 14 days

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Mader M, et al. Bioorg Med Chem Lett, 2008, 18(1), 179-183.

[2] Ishitsuka K, et al. Br J Haematol, 2008, 141(5), 598-606.

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Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02364206 Recruiting Adult Glioblastoma Centre Jean Perrin|National Cancer Institute, France|ARC  ...more Centre Jean Perrin|National Cancer Institute, France|ARC Foundation for Cancer Research June 2015 Phase 1|Phase 2
NCT02322853 Recruiting Postmenopausal|Metastatic Breast Cancer Centre Francois Baclesse|National Cancer Institute, Franc  ...more Centre Francois Baclesse|National Cancer Institute, France|ARC Foundation for Cancer Research January 2015 Phase 2
NCT01663857 Recruiting Epithelial Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Cancer Eli Lilly and Company July 2012 Phase 1|Phase 2
NCT01393990 Completed Advanced Cancer Eli Lilly and Company August 2008 Phase 1

Chemical Information

Download LY2228820 SDF
Molecular Weight (MW) 612.74


CAS No. 862507-23-1
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 4 mg/mL warming (6.52 mM)
Water 100 mg/mL warming (163.2 mM)
Ethanol 3 mg/mL (4.89 mM)
In vivo Saline 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 5-(2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-neopentyl-3H-imidazo[4,5-b]pyridin-2-amine dimethanesulfonate

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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