Cytochrome P450

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  1. 7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).
  2. integrin αvβ3 antagonist

    Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.
  3. 10-Oxo Docetaxel (Docetaxel Impurity 1) is a novel taxoid having remarkable anti-tumor properties and a Docetaxel intermediate.
  4. Microtubule-Targeting Agent

    ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
  5. tubulin polymerization inhibitor

    BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
  6. Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively.
  7. Arp2/3 complex inhibitor

    CK-869 is an Actin-Related Protein 2/3 (ARP2/3) complex inhibitor, with an IC50 of 7 μM.
  8. Arp2/3 complex inhibitor

    CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex, and binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation.
  9. Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.
  10. β-tubulin polymerization inhibitor

    Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.
  11. Ombrabulin hydrochloride is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
  12. Kif15 inhibitor

    Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
  13. Kif15 inhibitor

    Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member 15 (Kif15), and is used for the research of cellular proliferative diseases.
  14. αvβ3 integrin antagonist

    MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide αvβ3 integrin antagonist with an IC50 of 80 nM.
  15. PAK1 inhibitor

    IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).
  16. Tubulin assembly inhibitor

    Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity.
  17. tubulin polymerization inhibitor

    Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
  18. β-tubulin polymerization inhibitor

    Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
  19. microtubule inhibitor

    Rosabulin is a potent microtubule inhibitor, with anti-cancer activities.
  20. cytotoxic tubulin modifier

    Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates. Auristatin F inhibits cell division by blocking the polymerisation of tubulin.
  21. cytotoxic tubulin modifier

    Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
  22. Dolastatin 10 (DLS 10) is a potent antimitotic peptide, isolated from the marine mollusk Dolabela auricularia, that inhibits tubulin polymerization.
  23. microtubule-disrupting agent

    Verubulin (MPC-6827) is a microtubule-disrupting agent with potent and broad-spectrum in vitro and in vivo cytotoxic activities, and acts as a promising candidate for the treatment of multiple cancer types.
  24. tubulin polymerization inhibitor

    McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.
  25. integrin α5β1 antagonist

    ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  26. HSET/KIFC1 inhibitor

    AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
  27. integrin α5β1 antagonist

    ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
  28. DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
  29. kinesin Eg5 inhibitor

    Litronesib (Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5.
  30. microtubule targeting agent

    Eribulin (E7389) is a microtubule targeting agent that is used in the treatment of metastatic breast cancer.
  31. Tau and Aβ aggregation inhibitor

    PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.
  32. MPS1 kinase inhibitor

    BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
  33. MPS1 kinase inhibitor

    Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
  34. Mps1 inhibitor

    Empesertib (BAY 1161909) is a potent Mps1 inhibitor, with an IC50 of < 1 nM.
  35. microtubule-disrupting agent

    Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities.
  36. Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.
  37. MPS1 inhibitor

    NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
  38. PAK inhibitor

    GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.
  39. mitotic/tubulin inhibitor

    D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.
  40. MPS1 inhibitor

    CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.
  41. tubulin polymerisation inhibitor

    Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo.
  42. αVβ3 integrin inhibitor

    Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
  43. auristatin microtubule inhibitor

    PF-06380101 (Aur0101), an auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue.
  44. microtubule assembly and microtubule dynamics inhibitor

    Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15, as an inhibitor of microtubule assembly and microtubule dynamics.
  45. α4 integrin receptor inhibitor

    Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
  46. mitosis-specific kinesin Eg5 inhibitor

    Litronesib is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.
  47. dual Mps1/Plk1 inhibitor

    Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
  48. integrin-ligand interactions inhibitor

    RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation.
  49. myosin-II inhibitor

    2,3-Butanedione monoxime (BDM, Diacetyl monoxime, Diacetylmonoxime) is the well-characterized, low-affinity, non-competitive inhibitor of skeletal muscle myosin-II and inhibits skeletal and cardiac muscle contraction.
  50. LP-261 is a novel tubulin targeting anticancer agent that binds at the colchicine site on tubulin, inducing G2/M arrest. Screening in the NCI60 cancer cell lines resulted in a mean GI50 of approximately 100 nM.

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