LY2228820

Catalog No.S1494

LY2228820 Chemical Structure

Molecular Weight(MW): 612.74

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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4 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. 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. 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. 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. LY2228820 purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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 MkfTT4lv[XOnIHHzd4F6 MYL+PFAxKG6P MoLQSG1UVw>? MlrBbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NVLXfo9NOTh|OUezOFU>
U266 NEPQ[YVMcW6jc3WgZZN{[Xl? NGjvW|B,QDByIH7N MomySG1UVw>? Mk\wbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 MVmxPFM6PzN2NR?=
MM.1S NYDFOndvU2mwYYPlJIF{e2G7 MofBglgxOCCwTR?= MYLEUXNQ NXXKS3NTcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 NGL4fIgyQDN7N{O0OS=>
RPMI-Dox40 M2LVOGtqdmG|ZTDhd5NigQ>? M17JUJ45ODBibl2= Mo\rSG1UVw>? M3zoRYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MlTvNVg{QTd|NEW=
RPMI-LR5 MVrLbY5ie2ViYYPzZZk> NXriTJl2hjhyMDDuUS=> NHrOc4hFVVOR NF;se5ZqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MVmxPFM6PzN2NR?=
INA-6 MoPHT4lv[XOnIHHzd4F6 NXXWRmtyhjhyMDDuUS=> M2K2fGROW09? NXnNPHRWcW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 MXuxPFM6PzN2NR?=
RPMI-8226 MnjER5l1d3irY3n0fUBie3OjeR?= MYL+NVAxOCCwTR?= M{Cyd2ROW09? MlTxco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 NXjPTXVwOTh|OUezOFU>
U266 NV\YOlNkS3m2b4jpZ4l1gSCjc4PhfS=> NUi3ZmVkhjFyMECgcm0> NEXTe4pFVVOR M1frd45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> MYGxPFM6PzN2NR?=
MM.1S M3K0eWN6fG:6aXPpeJkh[XO|YYm= MW\+NVAxOCCwTR?= M3f4V2ROW09? MnTkco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 Mn\hNVg{QTd|NEW=
RPMI-Dox40 NFPSTo5EgXSxeHnjbZR6KGG|c3H5 MX\+NVAxOCCwTR?= MXPEUXNQ MXvuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NX;QNGdmOTh|OUezOFU>
RPMI-LR5 NFvLRlhEgXSxeHnjbZR6KGG|c3H5 NHPQXXp,OTByMDDuUS=> M330SGROW09? MVLuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M3W2PFE5Ozl5M{S1
INA-6 MXjDfZRwgGmlaYT5JIF{e2G7 NX;LcpBzhjFyMECgcm0> M{PxV2ROW09? Mnjpco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 NEDpXFcyQDN7N{O0OS=>
CD14+ MU\GeY5kfGmxbjDhd5NigQ>? Mnq0glgxOCCwTR?= M{XSXmROW09? MlXhbY5pcWKrdIOgc5N1\W:lbHHzeI9o\W6nc3nzJIZzd21iQ1SxOEBxd3OrdHn2[UBk\Wyucx?= MmTZNVg{QTd|NEW=
U-87-MG MVjGeY5kfGmxbjDhd5NigQ>? NH;FSpMyKM7:TR?= M2TydGROW09? NVfuVJk1emWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> M3GzRlI{OzN3NUC2
MDA-MB-231 MVfGeY5kfGmxbjDhd5NigQ>? NH3xPHQyKM7:TR?= NHjJO2dFVVOR NGLBNoZz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M4G3b|I{OzN3NUC2
A-2780 M4rWfWZ2dmO2aX;uJIF{e2G7 NVv4R4ZVOSEQvF2= NHPzNnhFVVOR M2rHb5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MVyyN|M{PTVyNh?=
SK-OV-3 MXnGeY5kfGmxbjDhd5NigQ>? MnjsNUDPxE1? M1nxXmROW09? NFT2N2Rz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MX2yN|M{PTVyNh?=
LXFA-629 NHvRVo9HfW6ldHnvckBie3OjeR?= M2f4TFEh|ryP NHnGZ5NFVVOR MmHDdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MmLqNlM{OzV3ME[=
NCI-H1650 M13J[mZ2dmO2aX;uJIF{e2G7 M171R|Eh|ryP Mlq2SG1UVw>? NX3oVnluemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> Mme2NlM{OzV3ME[=
PC-3 Mn3zSpVv[3Srb36gZZN{[Xl? NVrIc|d6OSEQvF2= Mn7BSG1UVw>? M1;WPJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NELPXZEzOzN|NUWwOi=>
RAW264.7 Mn3uSpVv[3Srb36gZZN{[Xl? NXvieXBEhjJyIN88US=> M3\2WGROW09? NGLmZYRqdmirYnn0d{BCdmm|b335Z4lvNXO2aX31cIF1\WRiTVuyJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOzVwMzDuUS=> NEK2bYYzPDN3NkixOC=>
mouse peritoneal macrophages NELwTJpHfW6ldHnvckBie3OjeR?= MVH+NlAh|ryP MmLtSG1UVw>? MVfMVHMwUU[QLd8z5qCUe3SrbYXsZZRm\CCWTl[t{tEheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gOk4{KG6P M{DZZ|I1OzV4OEG0
A549 MoPQSpVv[3Srb36gZZN{[Xl? NWWzOm9VhjJyIN88US=> MoGxSG1UVw>? NHT4doZqdmirYnn0d{BNWFNvaX7keYNm\CCFWFPMPEBxem:mdXP0bY9vKHerdHigTWM2OCCxZjCxOFQvQSCwTR?= MnS1NlQ{PTZ6MUS=
MDA-231 NUfKcoJITnWwY4Tpc44h[XO|YYm= MoHPglExKM7:TR?= NHW4NHp{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> NFzNPZYzPjRyN{i0Ny=>
MCF-7 M{iwVmZ2dmO2aX;uJIF{e2G7 NUW5dXdThjFyIN88US=> NFO3dZh{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> M1zVfFI3PDB5OESz
MDA-435 MVvGeY5kfGmxbjDhd5NigQ>? MVj+NVAh|ryP MmPZd5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u M{jTSFI3PDB5OESz
PC3 MXLGeY5kfGmxbjDhd5NigQ>? M363NZ4yOCEQvF2= MlPISG1UVw>? NF7Jbll{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MUiyOlkyOzZyOB?=

... 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
+ 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
+ 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
+ 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 (163.2 mM) warming
DMSO 4 mg/mL warmed (6.52 mM)
Ethanol 3 mg/mL (4.89 mM)
In vivo Saline 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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 Recruiting Adult Glioblastoma Centre Jean Perrin|National Cancer Institute, France|ARC Foundation for Cancer Research June 2015 Phase 1|Phase 2
NCT02322853 Recruiting Postmenopausal|Metastatic Breast Cancer Centre Francois Baclesse|National Cancer Institute, France|ARC Foundation for Cancer Research January 2015 Phase 2
NCT01663857 Recruiting 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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID