Ralimetinib (LY2228820)

For research use only. Not for use in humans.

Catalog No.S1494

29 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 29 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 NFKxNWNMcW6jc3WgZZN{[Xl? MUT+PFAxKG6P NH7IRYVFVVOR MYTpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NUXsfJBlOTh|OUezOFU>
U266 NILCd|dMcW6jc3WgZZN{[Xl? NV3nXGt[hjhyMDDuUS=> MWXEUXNQ NXXuUZZWcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 M16zO|E5Ozl5M{S1
MM.1S MYHLbY5ie2ViYYPzZZk> NIHnVlB,QDByIH7N MXHEUXNQ NG\NTWxqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= M4XGVFE5Ozl5M{S1
RPMI-Dox40 NEDFRXVMcW6jc3WgZZN{[Xl? M37aXZ45ODBibl2= MYnEUXNQ MWTpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NFzBelYyQDN7N{O0OS=>
RPMI-LR5 MnGxT4lv[XOnIHHzd4F6 Mnn5glgxOCCwTR?= MYXEUXNQ MlHobY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M2ThdFE5Ozl5M{S1
INA-6 MWnLbY5ie2ViYYPzZZk> NIPPR2R,QDByIH7N MkjtSG1UVw>? MoHzbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NWjvU203OTh|OUezOFU>
RPMI-8226 MWLDfZRwgGmlaYT5JIF{e2G7 MVP+NVAxOCCwTR?= Mo\4SG1UVw>? M1P1W45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NF;4RVgyQDN7N{O0OS=>
U266 M4\BVmN6fG:6aXPpeJkh[XO|YYm= MmrTglExODBibl2= MUTEUXNQ MoTXco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 MXexPFM6PzN2NR?=
MM.1S NXP1XYlXS3m2b4jpZ4l1gSCjc4PhfS=> MYj+NVAxOCCwTR?= NUP1d4FHTE2VTx?= MV;uc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M3;yW|E5Ozl5M{S1
RPMI-Dox40 M4X1VmN6fG:6aXPpeJkh[XO|YYm= Mme4glExODBibl2= MWfEUXNQ M2rVV45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M1HW[lE5Ozl5M{S1
RPMI-LR5 NFf6RlJEgXSxeHnjbZR6KGG|c3H5 NH[1fmF,OTByMDDuUS=> MWDEUXNQ NIDMephvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NWT1bIhnOTh|OUezOFU>
INA-6 MmfUR5l1d3irY3n0fUBie3OjeR?= NVK1Um5XhjFyMECgcm0> Mor4SG1UVw>? MnHUco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 NEHaS4wyQDN7N{O0OS=>
CD14+ M2\WSWZ2dmO2aX;uJIF{e2G7 MnrBglgxOCCwTR?= MV\EUXNQ Mn7HbY5pcWKrdIOgc5N1\W:lbHHzeI9o\W6nc3nzJIZzd21iQ1SxOEBxd3OrdHn2[UBk\Wyucx?= MoLONVg{QTd|NEW=
U-87-MG NWLLfHgyTnWwY4Tpc44h[XO|YYm= M3G3[lEh|ryP Mn21SG1UVw>? NGi1PVFz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M2XFeVI{OzN3NUC2
MDA-MB-231 M3T6bWZ2dmO2aX;uJIF{e2G7 NF;ufYoyKM7:TR?= NXrGNnFOTE2VTx?= NUTYNIw6emWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NH7wZmMzOzN|NUWwOi=>
A-2780 M{TYe2Z2dmO2aX;uJIF{e2G7 NVTsXmJrOSEQvF2= MorJSG1UVw>? M4HNe5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MoDNNlM{OzV3ME[=
SK-OV-3 NWfUNYNOTnWwY4Tpc44h[XO|YYm= NGLMTFcyKM7:TR?= NEToUJVFVVOR MXTy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MoPhNlM{OzV3ME[=
LXFA-629 NUTEO|B3TnWwY4Tpc44h[XO|YYm= M33lTVEh|ryP MUHEUXNQ MkPOdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NIX1c2YzOzN|NUWwOi=>
NCI-H1650 M4PSWWZ2dmO2aX;uJIF{e2G7 Ml7oNUDPxE1? MXTEUXNQ M4nHPJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NH;ldnkzOzN|NUWwOi=>
PC-3 MVXGeY5kfGmxbjDhd5NigQ>? NWO4Roh1OSEQvF2= NVW4W4ROTE2VTx?= MV7y[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NGH2RZMzOzN|NUWwOi=>
RAW264.7 NEeyVFBHfW6ldHnvckBie3OjeR?= NEPFdoF,OjBizszN M4n4bmROW09? NHGzfHhqdmirYnn0d{BCdmm|b335Z4lvNXO2aX31cIF1\WRiTVuyJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOzVwMzDuUS=> MWiyOFM2PjhzNB?=
mouse peritoneal macrophages Mn7USpVv[3Srb36gZZN{[Xl? NIjNWnN,OjBizszN NYjQSGVMTE2VTx?= M3nMSGxRWy:LRl6t{tPjiJO|dHnteYxifGWmIGTOSk3PuSCycn;keYN1cW:wIIfpeIghUUN3MDDv[kA3NjNibl2= Mm\wNlQ{PTZ6MUS=
A549 NH3mTmtHfW6ldHnvckBie3OjeR?= NIP3fHV,OjBizszN NFP1SHFFVVOR MoLLbY5pcWKrdIOgUHBUNWmwZIXj[YQhS1iFTEigdJJw\HWldHnvckB4cXSqIFnDOVAhd2ZiMUS0Mlkhdk1? NFna[IczPDN3NkixOC=>
MDA-231 NFP1SG9HfW6ldHnvckBie3OjeR?= NXrM[2lohjFyIN88US=> NFrWNGZ{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MWCyOlQxPzh2Mx?=
MCF-7 MV7GeY5kfGmxbjDhd5NigQ>? M4LwTJ4yOCEQvF2= M2nFPZN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> MlGyNlY1ODd6NEO=
MDA-435 MXTGeY5kfGmxbjDhd5NigQ>? NV;Xb3lWhjFyIN88US=> M2f3bpN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NGHFTVUzPjRyN{i0Ny=>
PC3 M{fJSWZ2dmO2aX;uJIF{e2G7 M1nPNp4yOCEQvF2= NYDTdXA4TE2VTx?= NHLMN4h{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> NFHoSnczPjlzM{[wPC=>

... 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
  • 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):
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)C[N]1C(=NC2=C1N=C(C=C2)C3=C(N=C([NH]3)C(C)(C)C)C4=CC=C(F)C=C4)N.C[S](O)(=O)=O.C[S](O)(=O)=O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID