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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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 MlnYT4lv[XOnIHHzd4F6 MmXHglgxOCCwTR?= NFfNVmhFVVOR NIrqbWlqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MYexPFM6PzN2NR?=
U266 MWDLbY5ie2ViYYPzZZk> MnXUglgxOCCwTR?= M3rGWWROW09? NF;EPFBqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MUixPFM6PzN2NR?=
MM.1S NXPIeZpKU2mwYYPlJIF{e2G7 M{LiWZ45ODBibl2= NEnDdHFFVVOR NGrOXJVqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NXXmWphtOTh|OUezOFU>
RPMI-Dox40 MV3LbY5ie2ViYYPzZZk> Mn3wglgxOCCwTR?= NILwZ4lFVVOR NYLUelZPcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 MVexPFM6PzN2NR?=
RPMI-LR5 MnXzT4lv[XOnIHHzd4F6 Mk\rglgxOCCwTR?= MV7EUXNQ MlLvbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NUHEfnZGOTh|OUezOFU>
INA-6 MYrLbY5ie2ViYYPzZZk> MUn+PFAxKG6P NFfURplFVVOR M1TxdolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MmfGNVg{QTd|NEW=
RPMI-8226 MnzhR5l1d3irY3n0fUBie3OjeR?= MVP+NVAxOCCwTR?= MUjEUXNQ NYXUTnhydm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NIjo[FgyQDN7N{O0OS=>
U266 NF7YU3ZEgXSxeHnjbZR6KGG|c3H5 MVf+NVAxOCCwTR?= NWnFV3llTE2VTx?= MYTuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M3;1NVE5Ozl5M{S1
MM.1S M1m5eGN6fG:6aXPpeJkh[XO|YYm= NEDHWYl,OTByMDDuUS=> M37M[WROW09? MojGco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 NFzKeGUyQDN7N{O0OS=>
RPMI-Dox40 MkC5R5l1d3irY3n0fUBie3OjeR?= NYnSTYFThjFyMECgcm0> MWHEUXNQ M36xeI5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M4nDdlE5Ozl5M{S1
RPMI-LR5 NVS5b4ozS3m2b4jpZ4l1gSCjc4PhfS=> M3HBW54yODByIH7N MXXEUXNQ NULOb|FNdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NVT1cYZ3OTh|OUezOFU>
INA-6 MXrDfZRwgGmlaYT5JIF{e2G7 NHj2bFF,OTByMDDuUS=> Ml7oSG1UVw>? MVzuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NGDsfVAyQDN7N{O0OS=>
CD14+ NYDTS4lQTnWwY4Tpc44h[XO|YYm= NYjkO5J2hjhyMDDuUS=> NG\ESGVFVVOR MWnpcohq[mm2czDvd5Rmd2OuYYP0c4dmdmW|aYOg[pJwdSCFREG0JJBwe2m2aY\lJINmdGy| NX7Zc3ltOTh|OUezOFU>
U-87-MG NEnuO3RHfW6ldHnvckBie3OjeR?= NGLLbGEyKM7:TR?= MYHEUXNQ MoKxdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= M3LyUVI{OzN3NUC2
MDA-MB-231 MmP5SpVv[3Srb36gZZN{[Xl? NISw[YsyKM7:TR?= NVrrSYI6TE2VTx?= MmK3doVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MVKyN|M{PTVyNh?=
A-2780 NUXndYQ{TnWwY4Tpc44h[XO|YYm= M4PMeFEh|ryP NV\VbFRpTE2VTx?= M{W5d5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NEHPZ3MzOzN|NUWwOi=>
SK-OV-3 NHK3XoFHfW6ldHnvckBie3OjeR?= MWKxJO69VQ>? MonaSG1UVw>? NEHFZZRz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> Mn6yNlM{OzV3ME[=
LXFA-629 MoLRSpVv[3Srb36gZZN{[Xl? M1\ybFEh|ryP MV\EUXNQ MYny[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NWjHOXU1OjN|M{W1NFY>
NCI-H1650 NXvNVYhYTnWwY4Tpc44h[XO|YYm= NXHIeHh3OSEQvF2= NEftNZlFVVOR M3zGfpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NF;2SJgzOzN|NUWwOi=>
PC-3 NIG4OY5HfW6ldHnvckBie3OjeR?= NV[1WFhbOSEQvF2= M33FW2ROW09? NWHZe4tlemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NFTBUpYzOzN|NUWwOi=>
RAW264.7 MmPCSpVv[3Srb36gZZN{[Xl? MnfzglIxKM7:TR?= NH\DO|BFVVOR NHjXfWtqdmirYnn0d{BCdmm|b335Z4lvNXO2aX31cIF1\WRiTVuyJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOzVwMzDuUS=> MYGyOFM2PjhzNB?=
mouse peritoneal macrophages M4fZ[GZ2dmO2aX;uJIF{e2G7 M2DyNJ4zOCEQvF2= NWKxfoFRTE2VTx?= M3fKV2xRWy:LRl6t{tPjiJO|dHnteYxifGWmIGTOSk3PuSCycn;keYN1cW:wIIfpeIghUUN3MDDv[kA3NjNibl2= M1qyclI1OzV4OEG0
A549 MknMSpVv[3Srb36gZZN{[Xl? NXu4cFNUhjJyIN88US=> MVTEUXNQ NE\1N4xqdmirYnn0d{BNWFNvaX7keYNm\CCFWFPMPEBxem:mdXP0bY9vKHerdHigTWM2OCCxZjCxOFQvQSCwTR?= NEfyTIIzPDN3NkixOC=>
MDA-231 NYDlN4FtTnWwY4Tpc44h[XO|YYm= NIfZbmt,OTBizszN NWO0VHI3e3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v Mn\INlY1ODd6NEO=
MCF-7 M2\UZWZ2dmO2aX;uJIF{e2G7 NGXGVVV,OTBizszN NEjIO3R{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MYmyOlQxPzh2Mx?=
MDA-435 MkfpSpVv[3Srb36gZZN{[Xl? NIDuVZF,OTBizszN Mk\Md5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u NF:zPHEzPjRyN{i0Ny=>
PC3 M{foXmZ2dmO2aX;uJIF{e2G7 MYP+NVAh|ryP MUDEUXNQ NYL4UpM{e3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v NG[xe4UzPjlzM{[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