Target Selective Inhibitor Library

目录号 L3500

605 target selective inhibitors

规格 价格  
100uL/well (10mM solution) RMB 74920.68
2x100uL/well (10mM solution) RMB 138001.81


Target Selective Inhibitor Library目录



  • 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

    The inhibitor PD173074 (A) or PD184352 (B) was administered to one uterine horn of Hand2d/d mice on day 3 of pregnancy (n = 5). The other horn served as vehicle-treated control. Uterine horns were collected on the morning of day 4, and sections were subjected to IHC to detect p-FRS2, p-ERK1/2, and Ki-67. (C) IHC of pERa and Muc-1 in uterine sections of Hand2d/d mice treated with PD173074 or PD184352.

    Science 2011 331, 912-916. PD184352 (CI-1040) 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. VX-680 (Tozasertib, 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 unique collection of validated bioactive compounds covering over 174 targets

• Each compound was selected based on its ability to principally interact with a single target, leading to minimal off-target activity

• Selectivity is at least 100-fold higher relative to non-primary target(s)

•Targets cover a wide variety of signaling pathways, including PI3K/Akt, MAPK, PTK, JAK, apoptosis, and others!

• This unique tool is ideal for studying mechanisms of action or for target screening

• Compounds are structurally diverse, biologically active, and cell permeable

• Selleck provides rich supporting documentation which includes compound structure, IC50, and customer reviews

• Compounds are NMR and HPLC validated to ensure our customers receive high purity compounds


配制: A unique collection of 605 target selective inhibitors supplied as pre-dissolved DMSO solutions
容器: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
稳定性: 溶于DMSO
发货: 蓝冰物流
包装: 惰性气体

Target Selective Inhibitor Library组成

HTS Facility Partners