Ralimetinib (LY2228820)

For research use only.

Catalog No.S1494

44 publications

Ralimetinib (LY2228820) Chemical Structure

CAS No. 862507-23-1

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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Selleck's Ralimetinib (LY2228820) has been cited by 44 publications

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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 Ml7qT4lv[XOnIHHzd4F6 NEDN[JJ,QDByIH7N MV;EUXNQ MkTJbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 Ml74NVg{QTd|NEW=
U266 MkLST4lv[XOnIHHzd4F6 M{HTR545ODBibl2= NWDsWVNVTE2VTx?= NFj6TJJqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MkexNVg{QTd|NEW=
MM.1S Ml;TT4lv[XOnIHHzd4F6 NIjGeFR,QDByIH7N MWnEUXNQ MVzpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MnfTNVg{QTd|NEW=
RPMI-Dox40 NGfJSY9McW6jc3WgZZN{[Xl? NGT0S4J,QDByIH7N M2fubWROW09? NV\sNmx3cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 MXuxPFM6PzN2NR?=
RPMI-LR5 MV7LbY5ie2ViYYPzZZk> M{\Lb545ODBibl2= M2TsWGROW09? MoHybY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M3e3NVE5Ozl5M{S1
INA-6 MnrYT4lv[XOnIHHzd4F6 MorvglgxOCCwTR?= M{nhS2ROW09? NITzWYxqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NETKWpEyQDN7N{O0OS=>
RPMI-8226 Mlr2R5l1d3irY3n0fUBie3OjeR?= MWL+NVAxOCCwTR?= MWHEUXNQ MYXuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M3XNclE5Ozl5M{S1
U266 NXSxc4dwS3m2b4jpZ4l1gSCjc4PhfS=> M1rHRZ4yODByIH7N MmT2SG1UVw>? MmLmco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 NXnS[3pSOTh|OUezOFU>
MM.1S MX3DfZRwgGmlaYT5JIF{e2G7 NW\xcJJshjFyMECgcm0> NGr6RVVFVVOR M{HsTo5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NHrLZXIyQDN7N{O0OS=>
RPMI-Dox40 M1LQfWN6fG:6aXPpeJkh[XO|YYm= MmS1glExODBibl2= NYHpXoNETE2VTx?= NGrnToFvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NE[2fI8yQDN7N{O0OS=>
RPMI-LR5 NVLVNYw6S3m2b4jpZ4l1gSCjc4PhfS=> MV7+NVAxOCCwTR?= MkLNSG1UVw>? Mmjmco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 MV:xPFM6PzN2NR?=
CD14+ MUfGeY5kfGmxbjDhd5NigQ>? NY\LOGNYhjhyMDDuUS=> NYD0TlFLTE2VTx?= NWmyWlNMcW6qaXLpeJMhd3O2ZX;jcIF{fG:pZX7ld4l{KG[{b32gR2QyPCCyb4PpeIl3\SClZXzsdy=> NVTzVoU4OTh|OUezOFU>
U-87-MG MnfXSpVv[3Srb36gZZN{[Xl? MXWxJO69VQ>? NIHXRoFFVVOR MWfy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MWeyN|M{PTVyNh?=
MDA-MB-231 MUfGeY5kfGmxbjDhd5NigQ>? NWLaVJNTOSEQvF2= M{jne2ROW09? Mm\wdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NFXrNVczOzN|NUWwOi=>
A-2780 NV;jbXFmTnWwY4Tpc44h[XO|YYm= NFLQd4wyKM7:TR?= NVHOenJ2TE2VTx?= NFzaN3Bz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> NVi3U3ZIOjN|M{W1NFY>
SK-OV-3 M2TJR2Z2dmO2aX;uJIF{e2G7 NVTBSHJCOSEQvF2= NWjDT5d6TE2VTx?= NGjUUpVz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M1jNWFI{OzN3NUC2
LXFA-629 M{PwUWZ2dmO2aX;uJIF{e2G7 NVPGN5RlOSEQvF2= NYTSe|RzTE2VTx?= MX7y[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= Mk[1NlM{OzV3ME[=
NCI-H1650 MWTGeY5kfGmxbjDhd5NigQ>? MnXUNUDPxE1? MkTDSG1UVw>? M1XyRZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NUnIeHZ4OjN|M{W1NFY>
PC-3 NF3ySm9HfW6ldHnvckBie3OjeR?= NGDxdVcyKM7:TR?= NXL2bGpwTE2VTx?= M1n2bJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MUeyN|M{PTVyNh?=
RAW264.7 M1vU[WZ2dmO2aX;uJIF{e2G7 NWDMWGR5hjJyIN88US=> MlnxSG1UVw>? MWjpcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= M4PBTFI1OzV4OEG0
mouse peritoneal macrophages MWPGeY5kfGmxbjDhd5NigQ>? NGjNO|h,OjBizszN MXHEUXNQ M{nPemxRWy:LRl6t{tPjiJO|dHnteYxifGWmIGTOSk3PuSCycn;keYN1cW:wIIfpeIghUUN3MDDv[kA3NjNibl2= NWOy[|JmOjR|NU[4NVQ>
A549 NEP3XI9HfW6ldHnvckBie3OjeR?= NW\CUI1khjJyIN88US=> NHL3boRFVVOR MX\pcohq[mm2czDMVHMucW6mdXPl[EBEYEOOODDwdo9lfWO2aX;uJJdqfGhiSVO1NEBw\iBzNESuPUBvVQ>? MVeyOFM2PjhzNB?=
MDA-231 MVTGeY5kfGmxbjDhd5NigQ>? M2rDVp4yOCEQvF2= Mor3d5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u M1XpRlI3PDB5OESz
MCF-7 MVLGeY5kfGmxbjDhd5NigQ>? MXX+NVAh|ryP NYHK[2Jre3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v NHfqRoczPjRyN{i0Ny=>
MDA-435 MXnGeY5kfGmxbjDhd5NigQ>? MXP+NVAh|ryP NInwPG9{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> NGrtXlczPjRyN{i0Ny=>
PC3 NGLBTItHfW6ldHnvckBie3OjeR?= MVP+NVAh|ryP NFewcoJFVVOR NGjNZYV{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> M1zaXVI3QTF|NkC4

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27; 

PubMed: 23335506     

whole cell protein extracts were isolated from ECFCs or ADSCs following pretreatment with DMSO (−) or 1 μm LY2228820 dimesylate (+) for 30 min prior to the addition of 10 ng/ml VEGF, bFGF, EGF, or 100 ng/ml IL-6, and then the extracts were subjected to Western blot analysis using antisera directed against p-p38, p38α, p38β, p-MK2, total MK2, p-HSP27, total HSP27, and β-actin as a loading control.

p-S6K ; 

PubMed: 26844273     

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

23335506 26844273
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]
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  • 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]
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  • Animal Models: Lipopolysaccharide (LPS)-induced Balb/c mice
  • 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
Smiles CC(C)(C)CN1C2=C(C=CC(=N2)C3=C(N=C(N3)C(C)(C)C)C4=CC=C(C=C4)F)N=C1N.CS(=O)(=O)O.CS(=O)(=O)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID