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Pathways Recommended: Stem Cell/Wnt Cell Cycle/DNA Damage
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BTK-C481S mutant cells

" in MedChemExpress (MCE) Product Catalog:
Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153220
    Zelebrudomide

    NX-2127

    		 PROTACs Btk Inflammation/Immunology Cancer
    Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
    Zelebrudomide
  • HY-160167A
    (R,R)-Birelentinib

    (R,R)-DZD8586

    		 Btk Cancer
    (R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC50 values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC50 is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies .
    (R,R)-Birelentinib
  • HY-181996
    BTK-IN-47

    		Btk Caspase Apoptosis PARP Cancer
    BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies .
    BTK-IN-47

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