LY2228820

製品コードS1494

カスタマーフィードバック(4)

  • 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.

製品安全説明書

p38 MAPK阻害剤の選択性比較

生物活性

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。
靶点
p38α [1]
(Cell-free assay)
7 nM
In vitro試験

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 NHTkOGRMcW6jc3WgZZN{[Xl? M1vEbZ45ODBibl2= NF7aflBFVVOR NGfNSJNqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= Ml[0NVg{QTd|NEW=
U266 MlSyT4lv[XOnIHHzd4F6 M33sU545ODBibl2= NHvUcYNFVVOR MmWybY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 MX[xPFM6PzN2NR?=
MM.1S MnLrT4lv[XOnIHHzd4F6 MWT+PFAxKG6P NFjiOm1FVVOR NEjlS5RqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NHrET5IyQDN7N{O0OS=>
RPMI-Dox40 NH\5bXBMcW6jc3WgZZN{[Xl? MVn+PFAxKG6P NFTMXVBFVVOR MUfpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? M3PZ[FE5Ozl5M{S1
RPMI-LR5 NYriSZQ6U2mwYYPlJIF{e2G7 NHXEVHp,QDByIH7N NHHsbGNFVVOR NGnnV2RqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NELYUWMyQDN7N{O0OS=>
INA-6 NWOwdFRLU2mwYYPlJIF{e2G7 M2HmV545ODBibl2= MmDaSG1UVw>? Moi2bY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M2LuXlE5Ozl5M{S1
RPMI-8226 NILjUW9EgXSxeHnjbZR6KGG|c3H5 MUD+NVAxOCCwTR?= NX[xN|I4TE2VTx?= Ml\Wco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 MUGxPFM6PzN2NR?=
U266 NFfnXZJEgXSxeHnjbZR6KGG|c3H5 MoDRglExODBibl2= MXTEUXNQ MXvuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NXnBNYVYOTh|OUezOFU>
MM.1S NYLGVWtFS3m2b4jpZ4l1gSCjc4PhfS=> M1\oU54yODByIH7N Mm\jSG1UVw>? MWfuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NYHGNlg{OTh|OUezOFU>
RPMI-Dox40 NEPVd4pEgXSxeHnjbZR6KGG|c3H5 NUXDR2dNhjFyMECgcm0> NGLjSWZFVVOR MVnuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NGDjVJAyQDN7N{O0OS=>
RPMI-LR5 NX33e4JKS3m2b4jpZ4l1gSCjc4PhfS=> NEXESIV,OTByMDDuUS=> NFn6[3NFVVOR Mkfqco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 M1myVVE5Ozl5M{S1
INA-6 NHmzWGhEgXSxeHnjbZR6KGG|c3H5 MkjWglExODBibl2= NFHUZ3lFVVOR NXf2Smlsdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 NFfLU4syQDN7N{O0OS=>
CD14+ MmO2SpVv[3Srb36gZZN{[Xl? M37zSp45ODBibl2= Ml;RSG1UVw>? M2PiSolvcGmkaYTzJI9{fGWxY3zhd5Rw\2WwZYPpd{Bnem:vIFPENVQheG:|aYTpeoUh[2WubIO= NI\lbGQyQDN7N{O0OS=>
U-87-MG MYLGeY5kfGmxbjDhd5NigQ>? NYrYXpo3OSEQvF2= Mnr3SG1UVw>? MkjSdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MWWyN|M{PTVyNh?=
MDA-MB-231 M{XC[WZ2dmO2aX;uJIF{e2G7 NH3JW4UyKM7:TR?= NEj0eG1FVVOR MUXy[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MnHTNlM{OzV3ME[=
A-2780 MlXBSpVv[3Srb36gZZN{[Xl? M{jhblEh|ryP M32yfWROW09? NGr6OY5z\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MmrlNlM{OzV3ME[=
SK-OV-3 MVjGeY5kfGmxbjDhd5NigQ>? NFPXcnoyKM7:TR?= Mo\iSG1UVw>? M4PydZJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M2LFUVI{OzN3NUC2
LXFA-629 MmfjSpVv[3Srb36gZZN{[Xl? NXmzRZJyOSEQvF2= MonGSG1UVw>? MlOxdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= MoDyNlM{OzV3ME[=
NCI-H1650 MkC4SpVv[3Srb36gZZN{[Xl? M{jOOlEh|ryP MXPEUXNQ M2OwbJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NXTURm1OOjN|M{W1NFY>
PC-3 NVv5Upk3TnWwY4Tpc44h[XO|YYm= NUny[3c3OSEQvF2= M3vnNWROW09? NWfNOYJUemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NVjKOlgzOjN|M{W1NFY>
RAW264.7 NHjQTGRHfW6ldHnvckBie3OjeR?= NVOzU5RDhjJyIN88US=> NVX1dnd4TE2VTx?= NEDhfllqdmirYnn0d{BCdmm|b335Z4lvNXO2aX31cIF1\WRiTVuyJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOzVwMzDuUS=> MojqNlQ{PTZ6MUS=
mouse peritoneal macrophages M1jpemZ2dmO2aX;uJIF{e2G7 NFTTdHh,OjBizszN MYrEUXNQ MlWzUHBUN0mITj5Ot-KBm3O2aX31cIF1\WRiVF7GMe6yKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFYvOyCwTR?= NX76NIhYOjR|NU[4NVQ>
A549 NIH2TFNHfW6ldHnvckBie3OjeR?= Ml3FglIxKM7:TR?= MYDEUXNQ MlfTbY5pcWKrdIOgUHBUNWmwZIXj[YQhS1iFTEigdJJw\HWldHnvckB4cXSqIFnDOVAhd2ZiMUS0Mlkhdk1? Mlj6NlQ{PTZ6MUS=
MDA-231 MmjmSpVv[3Srb36gZZN{[Xl? M1e1TZ4yOCEQvF2= Mk\Pd5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u M4rPelI3PDB5OESz
MCF-7 NHjCNXlHfW6ldHnvckBie3OjeR?= MmXmglExKM7:TR?= NFnQc4J{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MnfBNlY1ODd6NEO=
MDA-435 MUTGeY5kfGmxbjDhd5NigQ>? MXr+NVAh|ryP MV\zeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MVeyOlQxPzh2Mx?=
PC3 NGGy[2tHfW6ldHnvckBie3OjeR?= MlrhglExKM7:TR?= NXvq[np2TE2VTx?= NVTWdlRye3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v MUKyOlkyOzZyOB?=

... Click to View More Cell Line Experimental Data

In vivo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]

プロトコル(参考用のみ)

キナーゼアッセイ:[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.
細胞アッセイ: [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.
    (参考用のみ)
動物実験:[1]
+ 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
    (参考用のみ)

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 Saline 30 mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 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。

化学情報

分子量 612.74
化学式

C24H29FN6.2CH4O3S

CAS No. 862507-23-1
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

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

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

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

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

p38 MAPK信号経路図

p38 MAPK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID