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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5 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.

  • 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. 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

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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 M4XLNWtqdmG|ZTDhd5NigQ>? MXv+PFAxKG6P NWXPPFlLTE2VTx?= MVXpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MWqxPFM6PzN2NR?=
U266 NYHmbZZ[U2mwYYPlJIF{e2G7 MUn+PFAxKG6P MnzBSG1UVw>? MUHpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? M3XZXFE5Ozl5M{S1
MM.1S NXLCU5hVU2mwYYPlJIF{e2G7 MkSwglgxOCCwTR?= NIr3PIFFVVOR M1nTcolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NWXVdI5tOTh|OUezOFU>
RPMI-Dox40 NYi1bohJU2mwYYPlJIF{e2G7 MVr+PFAxKG6P NFPjOXpFVVOR NEXxO4pqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NUj5cYl4OTh|OUezOFU>
RPMI-LR5 NYrWdoZpU2mwYYPlJIF{e2G7 NX\Y[WhShjhyMDDuUS=> MkLZSG1UVw>? MVfpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MV:xPFM6PzN2NR?=
INA-6 NHvsOohMcW6jc3WgZZN{[Xl? MYj+PFAxKG6P M{jjPGROW09? Mn7LbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NFWwRmgyQDN7N{O0OS=>
RPMI-8226 NHW2V3pEgXSxeHnjbZR6KGG|c3H5 M17Ve54yODByIH7N NEKwSYFFVVOR NW\kT|Rldm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NYKzdI9pOTh|OUezOFU>
U266 M4W3[2N6fG:6aXPpeJkh[XO|YYm= M2nBdZ4yODByIH7N NE\jOGFFVVOR MXfuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MUWxPFM6PzN2NR?=
MM.1S NWTHRWE3S3m2b4jpZ4l1gSCjc4PhfS=> MYf+NVAxOCCwTR?= NEPwV4hFVVOR NEPnTmZvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> NGXWUW0yQDN7N{O0OS=>
RPMI-Dox40 MVvDfZRwgGmlaYT5JIF{e2G7 NHzE[IN,OTByMDDuUS=> MnTCSG1UVw>? NXXkUIJPdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 M1zGd|E5Ozl5M{S1
RPMI-LR5 NGLZWWNEgXSxeHnjbZR6KGG|c3H5 MkH3glExODBibl2= NF3jS|ZFVVOR NVHnOow2dm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NFjZcVgyQDN7N{O0OS=>
INA-6 M{PHNGN6fG:6aXPpeJkh[XO|YYm= Mme0glExODBibl2= M{HSOWROW09? MnWzco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M{PNW|E5Ozl5M{S1
CD14+ MW\GeY5kfGmxbjDhd5NigQ>? MXL+PFAxKG6P MmHaSG1UVw>? NY\TTHNlcW6qaXLpeJMhd3O2ZX;jcIF{fG:pZX7ld4l{KG[{b32gR2QyPCCyb4PpeIl3\SClZXzsdy=> NVW1bYhsOTh|OUezOFU>
U-87-MG MmL5SpVv[3Srb36gZZN{[Xl? NW\2[|RkOSEQvF2= MonPSG1UVw>? M4P2Z5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M1K2W|I{OzN3NUC2
MDA-MB-231 MnXVSpVv[3Srb36gZZN{[Xl? NVLTdlNQOSEQvF2= M4H6fmROW09? M3rrVZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M2jJZlI{OzN3NUC2
A-2780 MkTXSpVv[3Srb36gZZN{[Xl? MmnhNUDPxE1? Mn\zSG1UVw>? M1TneZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NH;VOngzOzN|NUWwOi=>
SK-OV-3 NGfqZo9HfW6ldHnvckBie3OjeR?= M4nTb|Eh|ryP MWnEUXNQ M3fWOpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M2\ZcFI{OzN3NUC2
LXFA-629 NU\odGV6TnWwY4Tpc44h[XO|YYm= M4LNWFEh|ryP MULEUXNQ NVXWV|FLemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MVGyN|M{PTVyNh?=
NCI-H1650 M{C2S2Z2dmO2aX;uJIF{e2G7 M{PCPVEh|ryP MnW1SG1UVw>? MYjy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MnzzNlM{OzV3ME[=
PC-3 NHjqPWRHfW6ldHnvckBie3OjeR?= MXKxJO69VQ>? NUjkepdwTE2VTx?= M135fpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NXiwNoIzOjN|M{W1NFY>
RAW264.7 NFHuNmVHfW6ldHnvckBie3OjeR?= M{TLeZ4zOCEQvF2= M1fZRWROW09? NYrqT4dkcW6qaXLpeJMhSW6rc3;tfYNqdi2|dHnteYxifGWmIF3LNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDN3LkOgcm0> MXuyOFM2PjhzNB?=
mouse peritoneal macrophages MkPySpVv[3Srb36gZZN{[Xl? NVzJc5YzhjJyIN88US=> NWr1c|BOTE2VTx?= M{GzSGxRWy:LRl6t{tPjiJO|dHnteYxifGWmIGTOSk3PuSCycn;keYN1cW:wIIfpeIghUUN3MDDv[kA3NjNibl2= M{nrV|I1OzV4OEG0
A549 NHntfVZHfW6ldHnvckBie3OjeR?= NVf5VGJmhjJyIN88US=> NUO2S|BoTE2VTx?= NE\EUYlqdmirYnn0d{BNWFNvaX7keYNm\CCFWFPMPEBxem:mdXP0bY9vKHerdHigTWM2OCCxZjCxOFQvQSCwTR?= NHqyN3kzPDN3NkixOC=>
MDA-231 NETJZm5HfW6ldHnvckBie3OjeR?= NEi1UoF,OTBizszN MU\zeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NF[3TnkzPjRyN{i0Ny=>
MCF-7 NXSwflN{TnWwY4Tpc44h[XO|YYm= MX7+NVAh|ryP NIP3NmN{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> NGTXVFEzPjRyN{i0Ny=>
MDA-435 MYXGeY5kfGmxbjDhd5NigQ>? NIr3cnd,OTBizszN NIOzPWt{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MUGyOlQxPzh2Mx?=
PC3 M2r4R2Z2dmO2aX;uJIF{e2G7 NWXMVJQ{hjFyIN88US=> MWHEUXNQ NEjwe5l{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> M2PSbFI3QTF|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 individually and in order:
Saline
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
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 Active, not 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID