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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Cited by 21 Publications

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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 MXnLbY5ie2ViYYPzZZk> M17QfJ45ODBibl2= M1nhXGROW09? NFHuVVVqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= Mke3NVg{QTd|NEW=
U266 M2HUVWtqdmG|ZTDhd5NigQ>? M3f5eJ45ODBibl2= NF34eJRFVVOR M3Sz[IlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= M2HtVlE5Ozl5M{S1
MM.1S NXPrXoZXU2mwYYPlJIF{e2G7 MnnaglgxOCCwTR?= MmrvSG1UVw>? MkC3bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M1j3S|E5Ozl5M{S1
RPMI-Dox40 MXzLbY5ie2ViYYPzZZk> MYX+PFAxKG6P MUfEUXNQ MVPpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NVXHSmNSOTh|OUezOFU>
RPMI-LR5 NGPyb|hMcW6jc3WgZZN{[Xl? MYL+PFAxKG6P M3T3OmROW09? M4H4N4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NGrrOHUyQDN7N{O0OS=>
INA-6 NE\mc5FMcW6jc3WgZZN{[Xl? NIXXPHB,QDByIH7N MnXtSG1UVw>? NVjSPJBicW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 M2LMTVE5Ozl5M{S1
RPMI-8226 MUTDfZRwgGmlaYT5JIF{e2G7 M{KydZ4yODByIH7N NHO4T3JFVVOR M2XDSI5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> Ml;KNVg{QTd|NEW=
U266 MX7DfZRwgGmlaYT5JIF{e2G7 M3r2cp4yODByIH7N NV3WTmJ4TE2VTx?= MmLnco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M4\oNlE5Ozl5M{S1
MM.1S NEHncmJEgXSxeHnjbZR6KGG|c3H5 M{DWTp4yODByIH7N MXPEUXNQ MUfuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MWqxPFM6PzN2NR?=
RPMI-Dox40 MonQR5l1d3irY3n0fUBie3OjeR?= NFfBdYZ,OTByMDDuUS=> MWXEUXNQ Mn76co8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 MVGxPFM6PzN2NR?=
RPMI-LR5 M4f1bWN6fG:6aXPpeJkh[XO|YYm= NVzv[IhQhjFyMECgcm0> Ml;lSG1UVw>? NGTpXZBvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> M1PnUVE5Ozl5M{S1
INA-6 NFK4boxEgXSxeHnjbZR6KGG|c3H5 MYP+NVAxOCCwTR?= M3v0S2ROW09? NFPjc25vdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NVSz[YVKOTh|OUezOFU>
CD14+ MV\GeY5kfGmxbjDhd5NigQ>? MmD0glgxOCCwTR?= M2THe2ROW09? NHLmW2ZqdmirYnn0d{Bwe3Snb3PsZZN1d2enbnXzbZMh\nKxbTDDSFE1KHCxc3n0bZZmKGOnbHzz NV3RfGxvOTh|OUezOFU>
U-87-MG MX3GeY5kfGmxbjDhd5NigQ>? MnXUNUDPxE1? MWHEUXNQ MXTy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MoDYNlM{OzV3ME[=
MDA-MB-231 NEfGVZNHfW6ldHnvckBie3OjeR?= M3HjdVEh|ryP NUXQNplETE2VTx?= NHHHNYFz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> Mme5NlM{OzV3ME[=
A-2780 NYLKdno3TnWwY4Tpc44h[XO|YYm= NGXhSFgyKM7:TR?= NYDBdopuTE2VTx?= MYLy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NYjB[mQ2OjN|M{W1NFY>
SK-OV-3 M1TTZ2Z2dmO2aX;uJIF{e2G7 NHzmV|UyKM7:TR?= MWnEUXNQ MlrldoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NVLBcVVSOjN|M{W1NFY>
LXFA-629 NGD4VHlHfW6ldHnvckBie3OjeR?= NVXsXpRpOSEQvF2= NFnXUo1FVVOR MmL4doVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NXPsfI02OjN|M{W1NFY>
NCI-H1650 NV61TnZNTnWwY4Tpc44h[XO|YYm= MV:xJO69VQ>? MnewSG1UVw>? MlTldoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NXfYOJlyOjN|M{W1NFY>
PC-3 NVWwcJo3TnWwY4Tpc44h[XO|YYm= MonzNUDPxE1? MWLEUXNQ NXm5VGFjemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> M2LwU|I{OzN3NUC2
RAW264.7 MWDGeY5kfGmxbjDhd5NigQ>? NHezT2Z,OjBizszN NYLF[oZWTE2VTx?= MVrpcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= NVvrcXUyOjR|NU[4NVQ>
mouse peritoneal macrophages MXXGeY5kfGmxbjDhd5NigQ>? M2PvWJ4zOCEQvF2= NYH5NXZUTE2VTx?= NES1RlhNWFNxSV\OMe6{6oDVc4TpcZVt[XSnZDDUUmYu|rFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhPi5|IH7N NH;vTVMzPDN3NkixOC=>
A549 Moq2SpVv[3Srb36gZZN{[Xl? NHr3NXl,OjBizszN MlPKSG1UVw>? M{fFdYlvcGmkaYTzJGxRWy2rbnT1Z4VlKEO[Q1y4JJBzd2S3Y4Tpc44hf2m2aDDJR|UxKG:oIEG0OE46KG6P MlHnNlQ{PTZ6MUS=
MDA-231 MV\GeY5kfGmxbjDhd5NigQ>? Mm\XglExKM7:TR?= M4LufZN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NGnn[4MzPjRyN{i0Ny=>
MCF-7 NULW[WVMTnWwY4Tpc44h[XO|YYm= NFHQXIJ,OTBizszN MlT2d5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u M1;OdlI3PDB5OESz
MDA-435 NELCeZRHfW6ldHnvckBie3OjeR?= NXLkUlBRhjFyIN88US=> MYnzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MnmwNlY1ODd6NEO=
PC3 M4\IO2Z2dmO2aX;uJIF{e2G7 M3TUcJ4yOCEQvF2= NV2wTXVqTE2VTx?= MWDzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NIftVmMzPjlzM{[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]
+ Expand

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):
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID