LY2228820は一種の新たで、有効なp38 MAPK阻害剤で、無細胞試験でIC50値が7 nMですが、p38 MAPKの活性を変えません。臨床 1/2。

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  • 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.


p38 MAPK阻害剤の選択性比較


製品説明 LY2228820は一種の新たで、有効なp38 MAPK阻害剤で、無細胞試験でIC50値が7 nMですが、p38 MAPKの活性を変えません。臨床 1/2。
p38α [1]
(Cell-free assay)
7 nM

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 MlzsT4lv[XOnIHHzd4F6 NV\obo5zhjhyMDDuUS=> M{HzWGROW09? M4rhVolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NInzVo8yQDN7N{O0OS=>
U266 NVjPSlA1U2mwYYPlJIF{e2G7 NHjXS|R,QDByIH7N M3ezcmROW09? NXn4ToQycW6qaXLpeJMheGixc4Doc5J6dGG2aX;uJI9nKEiVUEK3 M1KwZ|E5Ozl5M{S1
MM.1S MWTLbY5ie2ViYYPzZZk> MXX+PFAxKG6P MV3EUXNQ MYDpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MYGxPFM6PzN2NR?=
RPMI-Dox40 MX7LbY5ie2ViYYPzZZk> Mn;3glgxOCCwTR?= Mni0SG1UVw>? MoHqbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NGrYRXEyQDN7N{O0OS=>
RPMI-LR5 NGqyVFlMcW6jc3WgZZN{[Xl? M3nKNZ45ODBibl2= M2jxWWROW09? M3X5ZolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NVfyVHlrOTh|OUezOFU>
INA-6 NHi4WW9McW6jc3WgZZN{[Xl? MnzvglgxOCCwTR?= NIiwOXJFVVOR MnPJbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NHv2[JYyQDN7N{O0OS=>
RPMI-8226 NEfqc2VEgXSxeHnjbZR6KGG|c3H5 NV\vO5hHhjFyMECgcm0> MYjEUXNQ M{DENY5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M2LCXFE5Ozl5M{S1
U266 NFfLbmtEgXSxeHnjbZR6KGG|c3H5 NGTXemt,OTByMDDuUS=> NVSzbGVwTE2VTx?= NG\LfoZvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> MV:xPFM6PzN2NR?=
MM.1S Mn[4R5l1d3irY3n0fUBie3OjeR?= NH;nTFR,OTByMDDuUS=> NYjjXWp3TE2VTx?= M2\jVo5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> Ml\XNVg{QTd|NEW=
RPMI-Dox40 M33LT2N6fG:6aXPpeJkh[XO|YYm= MX7+NVAxOCCwTR?= NF\vS2hFVVOR M4nyT45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M3\kR|E5Ozl5M{S1
RPMI-LR5 NVG5TWhPS3m2b4jpZ4l1gSCjc4PhfS=> MmnaglExODBibl2= M3PrXmROW09? MYLuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M3rPOlE5Ozl5M{S1
INA-6 MYTDfZRwgGmlaYT5JIF{e2G7 MWr+NVAxOCCwTR?= NYL5c|lVTE2VTx?= NYfDeoNkdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 MnX1NVg{QTd|NEW=
CD14+ M1X1e2Z2dmO2aX;uJIF{e2G7 NUT5ZYw{hjhyMDDuUS=> MYDEUXNQ NVLLU5Y1cW6qaXLpeJMhd3O2ZX;jcIF{fG:pZX7ld4l{KG[{b32gR2QyPCCyb4PpeIl3\SClZXzsdy=> M4fGPVE5Ozl5M{S1
U-87-MG M3exb2Z2dmO2aX;uJIF{e2G7 M3TxVlEh|ryP MWPEUXNQ M1nwXpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NF;SdGEzOzN|NUWwOi=>
MDA-MB-231 NVfON4VoTnWwY4Tpc44h[XO|YYm= M3Xk[VEh|ryP M4L3R2ROW09? MUny[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MYOyN|M{PTVyNh?=
A-2780 MlnYSpVv[3Srb36gZZN{[Xl? NGLnPJIyKM7:TR?= NHfRPIFFVVOR NULzUnZiemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NELWS2IzOzN|NUWwOi=>
SK-OV-3 M3PoPWZ2dmO2aX;uJIF{e2G7 NUH6NIZmOSEQvF2= NVnrU4FkTE2VTx?= MY\y[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NXzYUFhGOjN|M{W1NFY>
LXFA-629 NHfSOY5HfW6ldHnvckBie3OjeR?= MX[xJO69VQ>? M1PodGROW09? MUTy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MkjWNlM{OzV3ME[=
NCI-H1650 MoPDSpVv[3Srb36gZZN{[Xl? MV:xJO69VQ>? MXHEUXNQ M4PCcJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M3juUFI{OzN3NUC2
PC-3 MYXGeY5kfGmxbjDhd5NigQ>? M2e0elEh|ryP M3\ZUGROW09? M3;HS5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MVOyN|M{PTVyNh?=
RAW264.7 NEfXNYJHfW6ldHnvckBie3OjeR?= NW[zSYZ7hjJyIN88US=> M134bWROW09? Mnu3bY5pcWKrdIOgRY5qe2:veXPpck1{fGmvdXzheIVlKE2NMjDwbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFM2NjNibl2= MUmyOFM2PjhzNB?=
mouse peritoneal macrophages NEDUe2NHfW6ldHnvckBie3OjeR?= MVH+NlAh|ryP NGTXV3BFVVOR NULQWJlGVFCVL1nGUk3Pu+LCk4P0bY12dGG2ZXSgWG5HNc7zIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDZwMzDuUS=> NUnNfGpqOjR|NU[4NVQ>
A549 NH\FN3pHfW6ldHnvckBie3OjeR?= MoTBglIxKM7:TR?= NVv3W|l7TE2VTx?= MXHpcohq[mm2czDMVHMucW6mdXPl[EBEYEOOODDwdo9lfWO2aX;uJJdqfGhiSVO1NEBw\iBzNESuPUBvVQ>? M3:2NlI1OzV4OEG0
MDA-231 M1LodmZ2dmO2aX;uJIF{e2G7 NHLNZlF,OTBizszN NUn0V41Re3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v NGPncWMzPjRyN{i0Ny=>
MCF-7 M37CW2Z2dmO2aX;uJIF{e2G7 NFjW[Id,OTBizszN M{LWeZN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> MlzwNlY1ODd6NEO=
MDA-435 MV\GeY5kfGmxbjDhd5NigQ>? NHuxSmh,OTBizszN NV;kcnVUe3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v MlS4NlY1ODd6NEO=
PC3 MmLPSpVv[3Srb36gZZN{[Xl? Ml;OglExKM7:TR?= NYf2fJR1TE2VTx?= MkPFd5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u NUTWXHdQOjZ7MUO2NFg>


体内試験 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]


+ 展開

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.
細胞試験: [2, 3]
+ 展開
  • 細胞株: MM cells, including INA6, RPMI-8226, U266, and RPMI-Dox40
  • 濃度: 200 nM–800 nM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
+ 展開
  • 動物モデル: Lipopolysaccharide (LPS)-induced Balb/c mice
  • 製剤: Dissolved in 1% CMC/0.25% Tween 80 in water
  • 投薬量: 0–20 mg/kg
  • 投与方法: Oral bid dosing for 14 days

溶解度 (25°C)

体外 Water 100 mg/mL (163.2 mM) warming
DMSO 4 mg/mL warmed (6.52 mM)
Ethanol 3 mg/mL (4.89 mM)
体内 順序で溶剤を入れること:
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 612.74


CAS No. 862507-23-1
別名 N/A





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


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



Handling Instructions


  • * 必須

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID