Ralimetinib (LY2228820)

For research use only.

Catalog No.S1494

42 publications

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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Selleck's Ralimetinib (LY2228820) has been cited by 42 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.
Targets
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 MW\LbY5ie2ViYYPzZZk> MXT+PFAxKG6P MWLEUXNQ NYL2[mpUcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 NUfLPXNxOTh|OUezOFU>
U266 MYLLbY5ie2ViYYPzZZk> NILTOmZ,QDByIH7N M17yVmROW09? MWjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NUfmV4d4OTh|OUezOFU>
MM.1S MVrLbY5ie2ViYYPzZZk> NXzscpNThjhyMDDuUS=> NUKxWmJSTE2VTx?= M2XwSYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MX2xPFM6PzN2NR?=
RPMI-Dox40 NEf1[WZMcW6jc3WgZZN{[Xl? MYn+PFAxKG6P NIXTWGpFVVOR NVrqVodJcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 M3qzT|E5Ozl5M{S1
RPMI-LR5 MlTiT4lv[XOnIHHzd4F6 M2PWVZ45ODBibl2= MlLsSG1UVw>? M4r5TolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= M{fxdFE5Ozl5M{S1
INA-6 NWDTW3VHU2mwYYPlJIF{e2G7 NV:5Sol5hjhyMDDuUS=> M2XIVmROW09? NWfUc2U{cW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 NIfYdJkyQDN7N{O0OS=>
RPMI-8226 MX;DfZRwgGmlaYT5JIF{e2G7 MXP+NVAxOCCwTR?= NXPOUlRYTE2VTx?= MUDuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NULZd4J5OTh|OUezOFU>
U266 NYrN[4hZS3m2b4jpZ4l1gSCjc4PhfS=> NHG5XZR,OTByMDDuUS=> MVPEUXNQ MkTnco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 NFPU[ZQyQDN7N{O0OS=>
MM.1S MWrDfZRwgGmlaYT5JIF{e2G7 NH7P[Yl,OTByMDDuUS=> M2P1dWROW09? MnHyco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M1\JSlE5Ozl5M{S1
RPMI-Dox40 MkXPR5l1d3irY3n0fUBie3OjeR?= M2HYbp4yODByIH7N MYTEUXNQ NVzYWItOdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 Mm\hNVg{QTd|NEW=
RPMI-LR5 M4fXfGN6fG:6aXPpeJkh[XO|YYm= Ml7jglExODBibl2= MUPEUXNQ M4nS[Y5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NHvkfY0yQDN7N{O0OS=>
INA-6 MnXUR5l1d3irY3n0fUBie3OjeR?= NVTSdGlnhjFyMECgcm0> MY\EUXNQ NI\pUHBvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> MnfnNVg{QTd|NEW=
CD14+ M3jqPGZ2dmO2aX;uJIF{e2G7 NI\Ifm9,QDByIH7N NH6wSFBFVVOR MnzVbY5pcWKrdIOgc5N1\W:lbHHzeI9o\W6nc3nzJIZzd21iQ1SxOEBxd3OrdHn2[UBk\Wyucx?= NXOzbIJ1OTh|OUezOFU>
U-87-MG M1LUTGZ2dmO2aX;uJIF{e2G7 NF\PfYoyKM7:TR?= NYHKbJNKTE2VTx?= NFHEPZdz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> Ml;xNlM{OzV3ME[=
MDA-MB-231 NF74RXJHfW6ldHnvckBie3OjeR?= NVfKdnFGOSEQvF2= NGnVdIFFVVOR NECyN3Jz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> Ml;ONlM{OzV3ME[=
A-2780 Ml[5SpVv[3Srb36gZZN{[Xl? NWHNUpFEOSEQvF2= NYG5fYxFTE2VTx?= NV3mWmVpemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MXuyN|M{PTVyNh?=
SK-OV-3 NELHW4hHfW6ldHnvckBie3OjeR?= NXXXeFlWOSEQvF2= NWDlVFBUTE2VTx?= MWPy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NF:z[|gzOzN|NUWwOi=>
LXFA-629 NX7yWlBETnWwY4Tpc44h[XO|YYm= NFPGSIUyKM7:TR?= MY\EUXNQ NXzIV|d6emWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> M{PFO|I{OzN3NUC2
NCI-H1650 MoPDSpVv[3Srb36gZZN{[Xl? M2DpXFEh|ryP MkLJSG1UVw>? M1frUJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MoXzNlM{OzV3ME[=
PC-3 M3GzOGZ2dmO2aX;uJIF{e2G7 NVfCXHlpOSEQvF2= NX[0ZXlWTE2VTx?= MlPtdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NWXCOVZTOjN|M{W1NFY>
RAW264.7 MkXXSpVv[3Srb36gZZN{[Xl? MnHQglIxKM7:TR?= NIf3XXdFVVOR MVHpcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= NGLlVVczPDN3NkixOC=>
mouse peritoneal macrophages NUe3PGl3TnWwY4Tpc44h[XO|YYm= MlrrglIxKM7:TR?= M3K4fGROW09? MYrMVHMwUU[QLd8z5qCUe3SrbYXsZZRm\CCWTl[t{tEheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gOk4{KG6P NYS4V|ZVOjR|NU[4NVQ>
A549 Mny2SpVv[3Srb36gZZN{[Xl? NVLtSm13hjJyIN88US=> MkjrSG1UVw>? MoTxbY5pcWKrdIOgUHBUNWmwZIXj[YQhS1iFTEigdJJw\HWldHnvckB4cXSqIFnDOVAhd2ZiMUS0Mlkhdk1? NV25R2trOjR|NU[4NVQ>
MDA-231 MlTlSpVv[3Srb36gZZN{[Xl? MV3+NVAh|ryP NYe4eWxQe3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v Mn3NNlY1ODd6NEO=
MCF-7 MYfGeY5kfGmxbjDhd5NigQ>? NYjBXFFDhjFyIN88US=> NGP2enJ{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> NXq4co5pOjZ2MEe4OFM>
MDA-435 NWXMdlduTnWwY4Tpc44h[XO|YYm= NGnOZYd,OTBizszN M2K0VZN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NE\POFQzPjRyN{i0Ny=>
PC3 NX24UJdKTnWwY4Tpc44h[XO|YYm= M2TWVZ4yOCEQvF2= NEDzclBFVVOR NF24cHl{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MoDTNlY6OTN4MEi=

... Click to View More Cell Line Experimental Data

Assay
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]

Protocol

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):
Saline
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
Formula

C24H29FN6.2CH4O3S

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