Target Selective Inhibitor Library

目录号 L3500

サイズ 価格(税別)  
予めDMSOに溶解しています
100uL/well (10mM solution) JPY 1591555.53
2x100uL/well (10mM solution) JPY 2931343.88
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Target Selective Inhibitor Library内容

Selleckの分子ライブラリーが使用されている文献(2)

お客様叙述(10)

  • The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).

    Nature 2015 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck

    FRA1 downregulation during RAFi treatment drives the reactive secretome. c, Relative mRNA levels of FRA1 during vemurafenib exposure [0.1-1 uM]. d, Representative immunofluorescence staining of A375/A375R tumours for GFP (A375R, green) and FRA1 (red) after vehicle or vemurafenib treatment (5 days). DAPI, 49,6-diamidino-2-phenylindole. Scale bars, 50 um.

    Nature 2015 520(7547), 368-72. Vemurafenib (PLX4032, RG7204) purchased from Selleck

  • Phosphorylation of PPARg in epididymal white adipose tissue in ob/ob mice after treatment with MEK inhibitors. Gene expression in ob/ob epididymal white adipose tissue after treatment with vehicle or either of two MEK inhibitors, PD0325901 or GSK1120212 (n = 7, 7 and 8, respectively). Areas under the curve and gene expression were analysed by analysis of variance.

    Nature 2015 517(7534), 391-5. PD0325901 purchased from Selleck

    A,ERK phosphorylation in A375 expressing indicated ORFs following treatment with DMSO or 1 μM of PLX4720, RAF265, CI-1040 or AZD6244. B,ERK phosphorylation in A375 expressing indicated ORFs following treatment with DMSO, PLX4720 (1 μM) or PLX4720 in combination with CI-1040 or AZD6244 (all 1 μM).

    Nature 2010 468, 968-972. Selumetinib (AZD6244) purchased from Selleck

  • Survival curves for isogenic cell line pairs and melanoma cultures treated with the indicated AZD6244 concentration for 72 h (relative to DMSO treated controls; mean6s.e.m., n55). PLX4032 resistant cells were grown with PLX4032. Dashed line, 50% cell killing.

    Nature 2010 468, 973-977. Selumetinib (AZD6244) purchased from Selleck

    (G) Nocodazole-arrested HeLa cells were treated with VX-680 and MG132 and stained for CENP-E (Green), pT422 (Red) and DNA (Blue). (H) pT422 fluorescence intensity was normalized to the total CENP-E fluorescence. Plots show the mean of > 15 cells per condition from two independent experiments.

    Cell 2010 142, 444–455. Tozasertib (VX-680, MK-0457) purchased from Selleck

  • Cancer Cell 2013 24, 766-76. MK-2206 2HCl purchased from Selleck

    Effects on PI3K signaling. Tumor cells were treated with DMSO, BEZ-235 (5uM, 1uM), BKM-120 (5uM, 1uM), RAD-001(5uM, 1uM) or cyclopamine (2.5uM, 1uM) for 3 hr. Cells were lysed and protein was analyzed for phosphorylation of AKT and S6 (pAKT and pS6) or for GAPDH by Western blotting.

    Cancer Cell 2012 21(2), 155-67. Everolimus (RAD001) purchased from Selleck

  • Comparison between Genetic Ablation of Cdc20 and Current Mitotic Drugs (C) Transformed Cdc20(lox/lox); RERT(+/Cre) MEFs were subcutaneously injected into the two flanks of SCID mice, and tumors were scored every 2-3 days.These mice were injected i.p. (three injections per week) with 4-OHT or mitotic drugs (taxol, vincristine, and BI2536) when tumors reached about 200 mm3 of volume (day 11; arrow) (n = 8 mice per group). (D) Representative images of these fibrosarcomas 3 days after injection with 4-OHT (to generate Cdc20(D/D) cells), BI2536, or taxol. These mice were injected with 10 μM BrdU to score DNA replication. CA3, immunodetection of active caspase 3. Scale bars, 50 or 10 μM (insets).

    Cancer Cell 2010 18, 641–654. BI 2536 purchased from Selleck

    (a,b) RPE1 cells transfected with control or either of two B56-PP2A siRNA pools (1, 2) were incubated in MG132 (10µM, 15 min), followed by the addition of BI2536 (40 nM) or DMSO for 45 min. (a) The frequency of mitotic cells with few or absent cold-stable K-bres . (b) Maximum-intensity projection of tubulin (green) and an overlay with kinetochores (CREST, red) in B56-PP2A-siRNA (pool 2) cells treated with DMSO or BI2536 (40 nM). Insets are 3 enlargement of the optical sections spanning the outlined centromeres.

    Nat Cell Biol 2011 13, 1265-71. BI 2536 purchased from Selleck

製品特性&メリット

・生物活性が確認されている、633種類のターゲット選択化合物ライブラリーです。

・それぞれの化合物はターゲット分子との相互作用能に基づいて選別されています。そのため、オフ・ターゲット作用は最小限に抑えられています。

・非メインターゲットに比べて選択性は100倍以上高いです。

・PI3K/Akt、MAPK、PTK、JAK、アポトーシスなど広範な経路を標的にしています。

・ターゲット分子を選別するためのツールとなります。

・構造的に多様で、薬効および細胞透過性が確認されています。

・詳しい構造説明と、お客様からのレビューなど豊富な情報があります。

・NMRとHPLC検査で製品の高純度を保証しています。

製品詳細情報

調合: 633種ターゲットセレクティブ阻害剤の集めは予めDMSO溶液に溶解します
96well: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
安定性: in DMSO
in DMSO
出荷方式: ブルーアイス物流
包装: 不活性ガス(Inert gas)

Target Selective Inhibitor Library製品説明

L3500

HTS パートナ

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