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Results for "

C481S

" in MedChemExpress (MCE) Product Catalog:

15

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-130983
    N-piperidine Ibrutinib hydrochloride

    		Btk Ligands for Target Protein for PROTAC Cancer
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
    N-piperidine Ibrutinib hydrochloride
  • HY-122562
    MT-802
    2 Publications Verification

    		 PROTACs Btk Inflammation/Immunology Cancer
    MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL) .
    MT-802
  • HY-112215
    Nemtabrutinib
    3 Publications Verification

    ARQ-531; MK-1026

    		 Btk Inflammation/Immunology Cancer
    ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
    Nemtabrutinib
  • HY-136531
    XMU-MP-3

    		Btk Apoptosis Cancer
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis .
    XMU-MP-3
  • HY-144170
    RET-IN-14

    		RET Btk Cancer
    RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research
    RET-IN-14
  • HY-147580
    BTK-IN-10

    		Btk Cancer
    BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111) .
    BTK-IN-10
  • HY-169228
    WS-11

    		Btk Cancer
    WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds .
    WS-11
  • HY-147582
    BTK-IN-12

    		Btk Cancer
    BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8) .
    BTK-IN-12
  • HY-153705
    BTK-IN-25

    		Btk Cancer
    BTK-IN-25 (compound 71) is a potent inhibitor of BTK, and inhibits BTK(C481S) with an IC50 value of 0.77 nM. BTK-IN-25 inhibits BTK in DOHH2 cells with an IC50 value of 1 nM .
    BTK-IN-25
  • HY-153951S
    BTK-IN-26

    		Btk Inflammation/Immunology Cancer
    BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research .
    BTK-IN-26
  • HY-151211
    BTK-IN-16

    		Btk Inflammation/Immunology Cancer
    BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
    BTK-IN-16
  • HY-19834
    Fenebrutinib
    Maximum Cited Publications
    9 Publications Verification

    GDC-0853

    		 Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
    Fenebrutinib
  • HY-124153
    GNE-431

    		Btk Cardiovascular Disease Inflammation/Immunology
    GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases .
    GNE-431
  • HY-153220
    NX-2127

    		PROTACs Btk Cancer
    NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . 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 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
    NX-2127
  • HY-155072
    PROTAC BTK Degrader-5

    		PROTACs Btk Cancer
    PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297；Pink:BKT inhibitor (HY-150898)) 1.
    PROTAC BTK Degrader-5

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