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Xcessbio New Products

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  1. (S)-crizotinib, MTH1 Inhibitor

    Catalog No. M60208
    A novel potent, selective and cell permeable MTH1 inhibitor.
  2. 4SC-202, HDAC/LSD1 Dual Inhibitor

    Catalog No. M60230
    A potent, selective and orally bioavailable HDAC/LSD1 dual Inhibitor.
  3. A-366, G9a/GLP HMTase Inhibitor

    Catalog No. M60210
    A novel highly potent, selective and cell permeable G9a/GLP histone lysine methyltransferase inhibitor.
  4. A01, Smurf1 E3 Ubiquitin Ligase Inhibitor

    Catalog No. M60249
    A potent and selective Smurf1 E3 ubiquitin ligase inhibitor.
  5. AAE-581

    Catalog No. M60434
    Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S. IC50 value: Target: cathepsin K The cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.
  6. AC220

    Catalog No. M60435
    Quizartinib is a uniquely potent and selective Flt3 inhibitor with Kd (FLT3 binding affinity) of 1.6±0.7 nM in Biochemical assay.
  7. AC55541

    Catalog No. M60426
    AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM. IC50 value: 200-1000 nM(EC50) [1] Target: PAR2 agonist Neither AC-55541 nor AC-264613 had activity at any of the other PAR receptor subtypes, nor did they have any significant affinity for over 30 other molecular targets involved in nociception. Visualization of EYFP-tagged PAR2 receptors showed that each compound stimulated internalization of PAR2 receptors. AC-55541 was well absorbed when administered intraperitoneally to rats, reaching micromolar peak plasma concentrations. AC-55541 was stable to metabolism by liver microsomes and maintained sustained exposure in rats, with elimination half-lives of 6.1 h. Intrapaw administration of AC-55541 or AC-264613 elicited robust and persistent thermal hyperalgesia and edema. Coadministration of either a tachykinin 1 (neurokinin 1) receptor antagonist or a transient receptor potential vanilloid (TRPV) 1 antagonist completely blocked these effects. Systemic administration of either AC-55541 or AC-264613 produced a similar degree of hyperalgesia as was observed when the compounds were administered locally.
  8. AdipoRon, Adiponectin Receptor/AdipoR agonist

    Catalog No. M60152
    A novel, highly potent, selective and orally active small molecule agonist of adiponectin receptor (AdipoR).
  9. ADX47273

    Catalog No. M60433
    ADX-47273 is a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5(EC50=170 nM). IC50 value: 170 nM(EC50) [1] [2] Target: positive allosteric modulator (PAM) of mGluR5
  10. AG-120 (Ivosidenib), IDH1 Inhibitor

    Catalog No. M60318
    A potent, selective and reversible inhibitor of IDH1 in clinical trials.
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