Ralimetinib (LY2228820)

Catalog No.S1494

Ralimetinib (LY2228820) Chemical Structure

Molecular Weight(MW): 612.74

Ralimetinib (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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6 Customer Reviews

  • CD34 expression after 14 days of culture of CB CB CD34+ cells treated with the P38α inhibitor Ly2228820 or vehicle (DMSO; n=3). Error bars represent SEM.

    Blood 2012 119, 6255-8. Ralimetinib (LY2228820) purchased from Selleck.

    Cell cycle phase distributions were determined on U87EV and U87PTEN cell treated with B, +/- rapamycin and +/- LY2228820 as shown. Percent apoptotic cells as determined via annexin V staining is also shown below each graph. D were identical to B, except LN229MER-AKT and LN229EV cells induced with 4OHT were used.

    Mol Cancer Ther 2011 10, 2244-56. Ralimetinib (LY2228820) purchased from Selleck.

  • Cells were treated with 100-mU/mL bTSH with or without 1μM LY2228820. After 5 days, OPN expression (C) was determined by RT-qPCR. OPN secretion was determined by ELISA in cell culture medium. The bars represent the mean ± SEM of 3 experiments with at least 2 biological replicates.

    Endocrinology, 2016, 157(5):2173-81. Ralimetinib (LY2228820) purchased from Selleck.

    Relationship of JNK, p38 MAPK, and PI3K activation in TNF-α-induced signaling. Western blot analysis of the effect of another p38 MAPK inhibitor, LY2228820, on TNF-α signaling. HUVECs were pretreated with LY2228820 (10 umol/L) or wortmannin (1 umol/L) for 1 h, followed by stimulation with TNF-α (5 ng/mL) for 15 min (n=2).

    Acta Pharmacol Sin 2014 35, 339-50. Ralimetinib (LY2228820) purchased from Selleck.

  • Neuroscience, 2018, 374:61-69. Ralimetinib (LY2228820) purchased from Selleck.

    For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of LY2228820 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. Ralimetinib (LY2228820) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Ralimetinib (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.
p38α [1]
(Cell-free assay)
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 Ml\WT4lv[XOnIHHzd4F6 NUXiO49DhjhyMDDuUS=> MoPBSG1UVw>? MVLpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MmXYNVg{QTd|NEW=
U266 NHnzTZlMcW6jc3WgZZN{[Xl? Mk\5glgxOCCwTR?= NV;R[JI2TE2VTx?= MV\pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MXuxPFM6PzN2NR?=
MM.1S MUPLbY5ie2ViYYPzZZk> NF7ldpF,QDByIH7N MVjEUXNQ MnHwbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M{jQN|E5Ozl5M{S1
RPMI-Dox40 NGjLdVdMcW6jc3WgZZN{[Xl? NYPtZYU{hjhyMDDuUS=> MkewSG1UVw>? M3f1N4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= M1q2UVE5Ozl5M{S1
RPMI-LR5 Mn;iT4lv[XOnIHHzd4F6 M2nrZZ45ODBibl2= MoLlSG1UVw>? MUPpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NHrIcFkyQDN7N{O0OS=>
INA-6 M{[zSGtqdmG|ZTDhd5NigQ>? NWLsV4RmhjhyMDDuUS=> NF73WWdFVVOR MYHpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NXLjXZhoOTh|OUezOFU>
RPMI-8226 MVfDfZRwgGmlaYT5JIF{e2G7 Ml7oglExODBibl2= M3ywZmROW09? NWjmTW1Zdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NFfHU2QyQDN7N{O0OS=>
U266 Mlu5R5l1d3irY3n0fUBie3OjeR?= MofFglExODBibl2= NUHuSppDTE2VTx?= M3jWd45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M2nCbFE5Ozl5M{S1
MM.1S NIizS|BEgXSxeHnjbZR6KGG|c3H5 M3zwep4yODByIH7N NIfFcFFFVVOR M3W0XI5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NI\2TVUyQDN7N{O0OS=>
RPMI-Dox40 M13YbGN6fG:6aXPpeJkh[XO|YYm= Ml7GglExODBibl2= MlXrSG1UVw>? MYTuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NH\ySlIyQDN7N{O0OS=>
RPMI-LR5 NWHZUFE1S3m2b4jpZ4l1gSCjc4PhfS=> NFW5[YN,OTByMDDuUS=> MniwSG1UVw>? MVzuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MXyxPFM6PzN2NR?=
INA-6 MlPnR5l1d3irY3n0fUBie3OjeR?= M2j5cp4yODByIH7N NF3tWZRFVVOR M{jVPI5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NITTTmsyQDN7N{O0OS=>
CD14+ MmHjSpVv[3Srb36gZZN{[Xl? M2nzOZ45ODBibl2= NEjPRmJFVVOR M2K3N4lvcGmkaYTzJI9{fGWxY3zhd5Rw\2WwZYPpd{Bnem:vIFPENVQheG:|aYTpeoUh[2WubIO= NWH2eIpKOTh|OUezOFU>
U-87-MG NFfKUFlHfW6ldHnvckBie3OjeR?= M33jWVEh|ryP MkP1SG1UVw>? M{XjS5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NY\VSXhlOjN|M{W1NFY>
MDA-MB-231 MWrGeY5kfGmxbjDhd5NigQ>? MkS5NUDPxE1? MnjmSG1UVw>? Ml3TdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NHvzWmgzOzN|NUWwOi=>
A-2780 M1z2UWZ2dmO2aX;uJIF{e2G7 M{XPNFEh|ryP NYX1cWZoTE2VTx?= NYDodJdQemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MoTBNlM{OzV3ME[=
SK-OV-3 MWrGeY5kfGmxbjDhd5NigQ>? MVyxJO69VQ>? NG\ORmtFVVOR NFq0RlRz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MmTaNlM{OzV3ME[=
LXFA-629 MYHGeY5kfGmxbjDhd5NigQ>? NGrVZYgyKM7:TR?= Mlz6SG1UVw>? Mn\MdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NHnaOWEzOzN|NUWwOi=>
NCI-H1650 MUHGeY5kfGmxbjDhd5NigQ>? MUWxJO69VQ>? M1z0fWROW09? MoHPdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MXGyN|M{PTVyNh?=
PC-3 MmH3SpVv[3Srb36gZZN{[Xl? MVmxJO69VQ>? MVPEUXNQ MnLMdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NIfVOG8zOzN|NUWwOi=>
RAW264.7 M3\id2Z2dmO2aX;uJIF{e2G7 NX\tdY54hjJyIN88US=> MYjEUXNQ NVvUeG56cW6qaXLpeJMhSW6rc3;tfYNqdi2|dHnteYxifGWmIF3LNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDN3LkOgcm0> Mk\vNlQ{PTZ6MUS=
mouse peritoneal macrophages Mk\1SpVv[3Srb36gZZN{[Xl? MWf+NlAh|ryP M{PwVGROW09? NH75SnRNWFNxSV\OMe6{6oDVc4TpcZVt[XSnZDDUUmYu|rFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhPi5|IH7N MXOyOFM2PjhzNB?=
A549 MYnGeY5kfGmxbjDhd5NigQ>? Ml[wglIxKM7:TR?= NHPyS3RFVVOR MYTpcohq[mm2czDMVHMucW6mdXPl[EBEYEOOODDwdo9lfWO2aX;uJJdqfGhiSVO1NEBw\iBzNESuPUBvVQ>? NU\JNnYzOjR|NU[4NVQ>
MDA-231 NFv6[otHfW6ldHnvckBie3OjeR?= MX;+NVAh|ryP Ml3Od5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u NGe1eFEzPjRyN{i0Ny=>
MCF-7 Mk\2SpVv[3Srb36gZZN{[Xl? NHjz[IZ,OTBizszN M4fafJN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> M{jrZVI3PDB5OESz
MDA-435 MWjGeY5kfGmxbjDhd5NigQ>? NYqw[JRLhjFyIN88US=> MWfzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MnfVNlY1ODd6NEO=

... 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]


Kinase Assay:[1]
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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 Research:[2, 3]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL warmed (163.2 mM)
DMSO 4 mg/mL warmed (6.52 mM)
Ethanol 3 mg/mL (4.89 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
30 mg/mL

* 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 Information

Molecular Weight 612.74


CAS No. 862507-23-1
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02364206 Active not recruiting Adult Glioblastoma Centre Jean Perrin|National Cancer Institute France|ARC Foundation for Cancer Research June 8 2015 Phase 1|Phase 2
NCT02322853 Terminated Postmenopausal|Metastatic Breast Cancer Centre Francois Baclesse|National Cancer Institute France|ARC Foundation for Cancer Research January 2015 Phase 2
NCT01663857 Completed 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID