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TMD8

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28

Inhibitors & Agonists

1

Inhibitory Antibodies

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-153321
    Bexobrutideg
    1 Publications Verification

    NX-5948; BTK-IN-24

    		 PROTACs Btk Inflammation/Immunology Cancer
    Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    Bexobrutideg
  • HY-P99349
    Loncastuximab tesirine

    Loncastuximab tesirine-lpyl; ADCT-402

    		 Antibody-Drug Conjugates (ADCs) Apoptosis Cancer
    Loncastuximab tesirine is a human cluster of differentiation 19 (CD19)-directed antibody-drug conjugate (ADC). The antibody portion is Loncastuximab (HY-P99711), and the drug-linker conjugate for ADC is Tesirine (HY-128952). Once bound to CD19 on the cell membrane, loncastuximab tesirine is rapidly internalised and triggers cell death. Loncastuximab tesirin induces cell apoptosis, it can be used for the research of diffuse large B-cell lymphoma .
    Loncastuximab tesirine
  • HY-160142
    UBX-382

    		PROTACs Btk Syk MEK ERK Cancer
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
    UBX-382
  • HY-157763
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1

    		PROTAC-Linker Conjugates for PAC Btk Cancer
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding BTK bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces BTK degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo BTK degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)) .
    Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1
  • HY-15805
    KIN-8194

    		Src Btk Cancer
    KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
    KIN-8194
  • HY-174850
    CFON-026

    		Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-154860
    PTD10

    		PROTACs Btk Apoptosis Caspase Bcl-2 Family NF-κB Akt Inflammation/Immunology Cancer
    PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .
    PTD10
  • HY-175541
    TQ-3959

    		PROTACs Btk Cancer
    TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
    TQ-3959
  • HY-163295
    BTK degrader-1

    		ADC Payload Btk Cancer
    BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect .
    BTK degrader-1
  • HY-177750
    TD-522

    		Molecular Glues Apoptosis Cancer
    TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .
    TD-522
  • HY-172217
    DNMT1-IN-5

    		DNA Methyltransferase Apoptosis Cancer
    DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
    DNMT1-IN-5
  • HY-150593
    IRAK4-IN-16

    		IRAK Cancer
    IRAK4-IN-16 (compound 4) is a potent IRAK4 (interleukin-1 receptor associated kinase 4) inhibitor, with an IC50 of 2.5 nM. IRAK4-IN-16 shows cytotoxicity activity against OCI-LY10, TMD8, Ramos and HT cells, with IC50 values of 0.2, 0.2, 0.6, and 2.7 μM, respectively .
    IRAK4-IN-16
  • HY-174129
    TM471-1

    		Btk Apoptosis Cancer
    TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
    TM471-1
  • HY-173143
    BTK-IN-42

    		Btk Cancer
    BTK-IN-42 (Compound 11a) is a Btk inhibitor. BTK-IN-42 can effectively inhibit the growth and migration of tumor cells TMD8, with IC50 values of 2.61 and 5.34 μM for TMD8 and T9 cells respectively. It shows promise for research in the field of anti-cancer .
    BTK-IN-42
  • HY-153321A
    (R,R)-Bexobrutideg

    (R,R)-NX-5948; (R,R)-BTK-IN-24

    		 Drug Isomer PROTACs Btk Inflammation/Immunology Cancer
    (R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
    (R,R)-Bexobrutideg
  • HY-156553
    BTK-IN-27

    		Btk Inflammation/Immunology Cancer
    BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases .
    BTK-IN-27
  • HY-164462
    BHA536

    		PKC NF-κB Apoptosis Cancer
    BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
    BHA536
  • HY-150594
    IRAK4-IN-17

    		IRAK NF-κB Cancer
    IRAK4-IN-17 (Compound 5) is a potent IRAK4 inhibitor with the IC50 of 1.3 nM . IRAK4-IN-17 can be used in large B-cell lymphoma (DLBCL) research .
    IRAK4-IN-17
  • 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
  • HY-173125
    FDU73

    		PROTACs Btk Cancer
    FDU73 is a highly effective and selective BTK PROTAC degrader with a DC50 of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity . (Pink: BTK ligand-14 (HY-173126); Black: Linker (HY-168297); Blue: E3 ligase ligand 59 (HY-173378); E3 ligase ligand+Linker (HY-173127))
    FDU73
  • HY-145884
    BTK-IN-8

    		Btk Inflammation/Immunology
    BTK-IN-8 is a potent and selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM) .
    BTK-IN-8
  • HY-181623
    PROTAC BTK degrader-14

    		PROTACs Btk Cancer
    PROTAC BTK degrader-14 (compound 112) is a PROTAC protein degrader targeting BTK. PROTAC BTK degrader-14 can be used for the research of cancer .
    PROTAC BTK degrader-14
  • HY-183819
    CRBN ligand-903-trans-1,4-cyclohexanediamine-Boc

    		E3 Ligase Ligand-Linker Conjugates Cancer
    CRBN ligand-903-trans-1,4-cyclohexanediamine-Boc is a cereblon (CRBN) ligand and ligase binding ligand (LBL) used in synthesis of p300 protein degraders, also designated as compound 28f. CRBN ligand-903-trans-1,4-cyclohexanediamine-Boc is tert-butyl (trans-4-(4-(2,4-dioxotetrahydropyrimidin-1(2H)-yl)-1-methoxy-2-naphthamido)cyclohexyl)carbamate, a CRBN ligand intermediate for synthesis of degrader 28.
    CRBN ligand-903-trans-1,4-cyclohexanediamine-Boc
  • HY-183817
    GNE-781-COOH

    		Ligands for Target Protein for PROTAC Epigenetic Reader Domain Cancer
    GNE-781-COOH is a CBP/p300 degrader. GNE-781-COOH also acts as a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC), which can be used to synthesize PROTAC CBP/P300 Degrader-4 (HY-183802) .
    GNE-781-COOH
  • HY-183802
    PROTAC CBP/P300 Degrader-4

    		PROTACs Histone Acetyltransferase Cancer
    PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC50 of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies .
    PROTAC CBP/P300 Degrader-4
  • HY-181547
    HBC-12551

    		Btk Cancer
    HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTK C481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma .
    HBC-12551
  • HY-182797
    NHWL071065

    		Molecular Glues IKZF Family IFNAR Cancer
    NHWL071065 is a CRBN-targeting IKZF1/IKZF3 molecular glues degrader. NHWL071065 selectively degrades IKZF1 and IKZF3 in lymphoma cells via the ubiquitin-proteasome pathway. NHWL071065 inhibits the proliferation of lymphoma cells. NHWL071065 downregulates proteins involved in cytoskeleton assembly, cell adhesion and immune regulation in cells, while upregulating proteins related to the type I IFN signaling pathway. NHWL071065 can be used in the research of lymphoma .
    NHWL071065

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