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Highly selective inhibitors

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  • Alisertib | Potent and selective inhibitor of Aurora A / Destabilizes Myc
    Alisertib (MLN8237, 1028486-01-2) is a highly selective and potent (IC50 = 1 nM) cell permeable inhibitor of Aurora A with off-target binding at GABAA (IC50 = 490 nM).1 It disrupts the Aurora A-Myc complex leading to Myc...

  • AZD6244 | ERK inhibitor
    AZD6244 (606143-53-6) is a potent, selective, and non-ATP competitive inhibitor of MEK1/2 (IC50 MEK1 = 14 nM) and ERK 1/2 phosphorylation (IC50 = 10 nM).1,2 AZD6244 is in clinical trials for treating various cancers...

  • AZD8055 | mTOR kinase inhibitor
    AZD8055 (1009298-09-2) is a potent and highly selective inhibitor of mammalian target of rapamycin kinase (mTOR) kinase (IC50 = 0.8 nM).1,2  mTOR acts as a nutrient/energy/redox sensor and a controller of protein...

  • Imatinib mesylate | 220127-57-1 | Structure | Supplier
    Imatinib (220127-57-1) is a tyrosine kinase inhibitor specific for abl (IC50 = 0.038 μM)1, PDGF-R (IC50 = 0.3 μM)1 and c-kit (IC50 = 0.1 μM)2. It is a clinically useful anti-cancer drug approved for the treatment of...

  • IntelliScreen Highly Selective Kinase Inhibitor Library 1 plate 100 ul/well
  • Linsitinib | Inhibits IGF-1R kinase and InsR kinase
    Linsitinib (867460-71-2) is a potent and selective dual inhibitor of insulin-like growth factor 1 (IGF-1R) kinase and insulin receptor (InsR) kinase (IC50’s = 35 and 75 nM respectively).1  It has been investigated...

  • MK-2206 | Potent and selective AKT inhibitor
    MK-2206 is a potent and selective allosteric inhibitor of Akt (IC50’s: Akt1 = 5 nM, Akt2 = 12 nM, Akt3 = 65 nM) that enhances the in vitro and in vivo antitumor efficacy of several standard chemotherapeutic agents.1 It...

  • ML167 | Clk4 inhibitor
    ML167 (1285702-20-6) is a highly selective cell permeable inhibitor of Cdc2-like kinase 4 (Clk4) - IC50 = 136nM. It displays at least 10-fold greater selectivity over the related kinases Clk1(1.52 μM), Clk2(1.65μM),...

  • NVP-BGJ398 | Pan-specific FGFR inhibitor
    NVP-BGJ398 (872511-34-1) is a potent and selective pan-FGFR inhibitor (IC50 = 0.9nM, 1.4 nM, 1.0 nM, and 60 nM for FGFR1,2,3,4 respectively).1  It has also been used in a mouse model of Achondroplasia (most common form...

  • Roscovitine | 186692-46-6 | Structure | Supplier
    Roscovitine (186692-46-6) is a potent and selective inhibitor of cyclin-dependent kinases displaying higher potency and selectivity compared to olomoucine.  p34 cdc2 IC50 = 0.2 µM.  Also inhibits p33cdk2 and...

  • Ruxolitinib | JAK inhibitor
    Potent and selective JAK1&2 inhibitor, IC50s=2.7, 4.5 and 322 nM forJAK1, JAK2 and JAK3 respectively.1  Blocks IL-6 signaling (IC50=281 nM) and proliferation of JAK2V617F+ Ba/F3 cells (IC50=127 nM).2 Inhibits the...

  • SMI-4a | 438190-29-5 | Structure | Supplier
    SMI-4a (438190-29-5) is a selective, ATP-competitive inhibitor of the Pim protein kinases (IC50 = 24 and 100 nM for Pim-1 and Pim-2 respectively). Selective over a panel of ~50 other kinases.1 Induces cell cycle arrest...

  • Tofacitinib | JAK inhibitor
    Tofacitinib (477600-75-2) is a potent pan-JAK inhibitor, IC50s=1, 20 and 112 nM for JAK3, JAK2 and JAK1 respectively.1 Displays potent antiinflammatory2 and immunosuppressant3 activity. Promotes a white-to-brown metabolic...

  • Trametinib | MEK inhibitor
    Trametinib (871700-17-3) is a highly potent (IC50 uMEK1 = 0.7 nM, pp-MEK1 = 14.9 nM)1 and selective MEK inhibitor displaying selective inhibition of proliferation in various BRAF mutant cancer cell lines (IC50 ACHN = 9.8 nM;...

  • Vatalanib 2HCl | VEGFRK inhibitor
    Vatalanib 2HCl (212141-51-0) is a potent, selective inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC50 = 77 nM) and VEGFR-2 (FLK-1/KDR, IC50 = 37 nM).1 Weaker inhibitor of other tyrosine kinases including...

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