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α4-α6

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-110208
    BRD9876
    1 Publications Verification

    		 Kinesin Microtubule/Tubulin Cancer
    BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
    BRD9876
  • HY-122247
    PVZB1194

    		Kinesin Cancer
    PVZB1194 is a biphenyl-type inhibitor of Kinesin-5 ATPase activity that binds to the α4/α6 site of the motor domain in a nucleotide competitive manner. PVZB1194 has an IC50 of 0.12 μM for KSP ATPase. PVZB1194 induces mitotic arrest with the formation of a monopolar spindle, and inhibits HeLa cells proliferatio (IC50: 5.5 μM). PVZB1194 can be used in the study of tumors .
    PVZB1194
  • HY-120874
    PF-06372865

    		GABA Receptor Neurological Disease
    PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
    PF-06372865
  • HY-162518
    Eg5-IN-3

    		Kinesin Microtubule/Tubulin Cancer
    Eg5-IN-3 (5) is an Eg5 inhibitor that targets the novel allosteric pocket (α4/α6/L11). Eg5-IN-3 (5) causes tubulin assembly distortion with irregular morphology, resulting in a typical mitotic arrest similar to Monastrol (HY-101071A) .
    Eg5-IN-3

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