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.

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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 MYXLbY5ie2ViYYPzZZk> NUTzd2pihjhyMDDuUS=> NV\pWXE{TE2VTx?= Ml7lbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NUPYNGNiOTh|OUezOFU>
U266 MlqyT4lv[XOnIHHzd4F6 NHraTm9,QDByIH7N MY\EUXNQ NEnQUHlqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MVqxPFM6PzN2NR?=
MM.1S NYD0W4k3U2mwYYPlJIF{e2G7 MkPyglgxOCCwTR?= MmTGSG1UVw>? NX7T[IVYcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 MXSxPFM6PzN2NR?=
RPMI-Dox40 NGj0bI5McW6jc3WgZZN{[Xl? MkLLglgxOCCwTR?= MoXOSG1UVw>? MWjpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MnzvNVg{QTd|NEW=
RPMI-LR5 NV;NToFHU2mwYYPlJIF{e2G7 Mny5glgxOCCwTR?= MU\EUXNQ NH7GXVNqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MkPWNVg{QTd|NEW=
INA-6 NH7EUIdMcW6jc3WgZZN{[Xl? NIXP[|l,QDByIH7N NWHNZ4U4TE2VTx?= M{fHPYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NFTIRWoyQDN7N{O0OS=>
RPMI-8226 MUXDfZRwgGmlaYT5JIF{e2G7 MYH+NVAxOCCwTR?= MlLsSG1UVw>? NFnQd2VvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> M2HKT|E5Ozl5M{S1
U266 NF3TWJBEgXSxeHnjbZR6KGG|c3H5 M3LkTJ4yODByIH7N NGDj[G1FVVOR NWL6c3hqdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NWPxZZY2OTh|OUezOFU>
MM.1S MnGyR5l1d3irY3n0fUBie3OjeR?= NH3XO4t,OTByMDDuUS=> MnLoSG1UVw>? NHGzOHNvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NXy1Vm5ZOTh|OUezOFU>
RPMI-Dox40 NV24dFRiS3m2b4jpZ4l1gSCjc4PhfS=> NF\GUmZ,OTByMDDuUS=> NU\neotbTE2VTx?= NUiyVmZydm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NYfNcpRlOTh|OUezOFU>
RPMI-LR5 NE\KWWlEgXSxeHnjbZR6KGG|c3H5 M3myTp4yODByIH7N M2DDRWROW09? Ml;aco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 MUGxPFM6PzN2NR?=
INA-6 M{HpUGN6fG:6aXPpeJkh[XO|YYm= NIG0W3F,OTByMDDuUS=> M17ydGROW09? MUHuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NVXxfW0{OTh|OUezOFU>
CD14+ MnzNSpVv[3Srb36gZZN{[Xl? NFT4bVV,QDByIH7N NFLp[VFFVVOR Ml;HbY5pcWKrdIOgc5N1\W:lbHHzeI9o\W6nc3nzJIZzd21iQ1SxOEBxd3OrdHn2[UBk\Wyucx?= MXSxPFM6PzN2NR?=
U-87-MG NVjUVmlWTnWwY4Tpc44h[XO|YYm= MoLNNUDPxE1? NXnwVHpKTE2VTx?= NGHnXYJz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MXGyN|M{PTVyNh?=
MDA-MB-231 NWnBelZtTnWwY4Tpc44h[XO|YYm= MlHNNUDPxE1? M{XQPGROW09? M1jQeJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NV7GSnBuOjN|M{W1NFY>
A-2780 MmXnSpVv[3Srb36gZZN{[Xl? NV[4OWF7OSEQvF2= M2XZc2ROW09? M1O5ZZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NX7iUJp[OjN|M{W1NFY>
SK-OV-3 NV7jUFd2TnWwY4Tpc44h[XO|YYm= NFvi[nUyKM7:TR?= NUDtdXdPTE2VTx?= MlXJdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= M{HlPVI{OzN3NUC2
LXFA-629 NWHYU2w6TnWwY4Tpc44h[XO|YYm= MoDGNUDPxE1? NHLadGxFVVOR MoXZdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NX7Jbo9pOjN|M{W1NFY>
NCI-H1650 MUPGeY5kfGmxbjDhd5NigQ>? NHHDZYoyKM7:TR?= MX;EUXNQ M{nyS5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NUfJS3loOjN|M{W1NFY>
PC-3 NIj4WYpHfW6ldHnvckBie3OjeR?= M3y0S|Eh|ryP MVjEUXNQ MoTIdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NHTVUZYzOzN|NUWwOi=>
RAW264.7 NHTydGJHfW6ldHnvckBie3OjeR?= MlX2glIxKM7:TR?= MnHwSG1UVw>? MYjpcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= MkHtNlQ{PTZ6MUS=
mouse peritoneal macrophages MkTkSpVv[3Srb36gZZN{[Xl? MnSwglIxKM7:TR?= M{TLZWROW09? MXnMVHMwUU[QLd8z5qCUe3SrbYXsZZRm\CCWTl[t{tEheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gOk4{KG6P NH\ZPGQzPDN3NkixOC=>
A549 MoL1SpVv[3Srb36gZZN{[Xl? MnnVglIxKM7:TR?= NILSO|VFVVOR NID5OopqdmirYnn0d{BNWFNvaX7keYNm\CCFWFPMPEBxem:mdXP0bY9vKHerdHigTWM2OCCxZjCxOFQvQSCwTR?= Mn:xNlQ{PTZ6MUS=
MDA-231 MUHGeY5kfGmxbjDhd5NigQ>? M1Hhe54yOCEQvF2= M17EZZN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NUfWVXpqOjZ2MEe4OFM>
MCF-7 NH3pR5RHfW6ldHnvckBie3OjeR?= MYn+NVAh|ryP MV7zeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NFq1NFczPjRyN{i0Ny=>
MDA-435 NF65SlhHfW6ldHnvckBie3OjeR?= MWX+NVAh|ryP MYLzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MWGyOlQxPzh2Mx?=
PC3 NFTMVHRHfW6ldHnvckBie3OjeR?= NIrXd4F,OTBizszN MoH6SG1UVw>? NULScpJze3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v M17n[|I3QTF|NkC4

... 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]

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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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