Kinesin

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Kinesin Inhibitors (6)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1452 Ispinesib (SB-715992) Ispinesib (SB-715992) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Phase 2.
  • Nat Methods, 2015, 10.1038/nmeth.3363
  • Nat Commun, 2015, 10.1038/ncomms8668
  • Mol Oncol, 2014, 8(8):1548-60
S2182 SB743921 SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2.
  • J Med Chem, 2013, 56(5):1878-93
  • Mol Oncol, 2014, 8(8):1404-18
  • Cell Death Dis, 2014, 5:e1177
S2731 AZ 3146 AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit.
  • J Biol Chem, 2013, 288(49):35149-58
  • Oncogenesis, 2014, 3:e100
S7090 GSK923295 GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. Phase 1.
S7488 MPI-0479605 MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.
S7355 ARQ 621 ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1452 Ispinesib (SB-715992) <1 mg/mL 103 mg/mL 103 mg/mL
S2182 SB743921 22 mg/mL 111 mg/mL 111 mg/mL
S2731 AZ 3146 <1 mg/mL 28 mg/mL 91 mg/mL
S7090 GSK923295 <1 mg/mL 100 mg/mL 100 mg/mL
S7488 MPI-0479605 <1 mg/mL 62 mg/mL 2 mg/mL
S7355 ARQ 621 <1 mg/mL 100 mg/mL 100 mg/mL
Tags: KSP inhibition | Kinesin inhibition | Kinesin assay | Kinesin phosphorylation | Kinesin cancer | KSP inhibitors cancer | KSP inhibitor clinical trial | Kinesin inhibitors list | Kinesin inhibitor review
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