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BTK ligand10

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153220

    PROTACs Btk Cancer
    NX-2127 is a a PROTAC targeting Bruton’s Tyrosine Kinase (Btk) with oral activity. NX-2127 is composed of PROTAC target protein ligand BTK ligand 10 (HY-168302) (red part), E3 ligase ligand Thalidomide 5-fluoride (HY-W087383) (blue part) and PROTAC Linker (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304). NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells .
    NX-2127
  • HY-168302

    Ligands for Target Protein for PROTAC Tyrosinase Cancer
    BTK ligand 10 is a Ligand for Target Protein for PROTAC. CDK8 ligand 1 can be used to synthesize (R)-NX-2127 (HY-153220A) .
    BTK ligand 10
  • HY-153220A

    PROTACs Btk Inflammation/Immunology Cancer
    (R)-NX-2127 (compound 28) is a a PROTAC targeting Bruton’s Tyrosine Kinase (Btk) with oral activity. (R)-NX-2127 is composed of PROTAC target protein ligand BTK ligand 10 (HY-168302) (red part), E3 ligase ligand Thalidomide 5-fluoride (HY-W087383) (blue part) and PROTAC Linker (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304) .
    (R)-NX-2127

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