2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Btk
  5. Btk Degrader

Btk Degrader

Btk Degraders (24):

Cat. No. Product Name Effect Purity
  • HY-153321
    NX-5948
    		Degrader 99.33%
    NX-5948 (BTK-IN-24) 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. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 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).
  • HY-153803
    GBD-9
    		Degrader 99.76%
    GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML).
    GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
  • HY-160141
    Catadegbrutinib
    		Degrader
    BGB-16673 (BGB-16673; BTK-IN-29) is an orally active, selectively chimeric degradation activator compound (CDAC), targeting BTK (IC50=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma.
  • HY-153357
    NRX-0492
    		Degrader 98.16%
    NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC50 ≤ 0.2 nM, DC90 ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).
  • HY-122830
    DD-03-171
    		Degrader 98.72%
    DD-03-171 is a BTK PROTAC degrader, the BTK IC50 a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells. (Pink: BTK inhibitor (HY-168292); Black: linker (HY-28875); Blue: CRBN Ligand (HY-131717))
  • HY-153220A
    (R)-NX-2127
    		Degrader 98.93%
    (R)-NX-2127 ((R)-Compound 28) is an isomer of the BTK PROTAC degrader NX-2127 (HY-153220). (Pink: BTK ligand 10 (HY-168302); Black: (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303); Blue: Thalidomide 5-fluoride (HY-W087383).
  • HY-163295
    BTK degrader-1
    		Degrader
    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.
  • HY-160142
    UBX-382
    		Degrader
    UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells.
  • HY-156746
    DBt-10
    		Degrader
    DBt-10 is a potent BTK PROTAC degrader (DC50: 137 nM). Blue: DCAF1 binder (HY-149934); Black: linker; Pink: BTK ligand.
  • HY-157763
    PROTAC BTK Degrader-8
    		Degrader
    PROTAC BTK Degrader-8 (compound 3) is an effective PROTAC BTK degrader that can be coupled to an ADC antibody to form a PAC.
  • HY-149391
    PROTAC BTK Degrader-6
    		Degrader
    PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6).
  • HY-122828
    PROTAC BTK Degrader-2
    		Degrader
    PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels.
  • HY-173125
    FDU73
    		Degrader
    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))
  • HY-172822
    TLT8
    		Degrader
    TLT8 is a ByeTAC protein degrader targeting BTK. TLT8 non-covalently binds to Rpn-13 and BTK, thereby inducing BTK degradation. TLT8 can be used in chronic lymphocytic leukemia research. (Rpn-13 ligand: HY-159808; BTK ligand: HY-Z3101; linker: HY-172823).
  • HY-156745
    DDa-1
    		Degrader
    DDa-1 is a potent BTK degrader (DC50: 90 nM). Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BTK ligand (HY-107447).
  • HY-155072
    PROTAC BTK Degrader-5
    		Degrader
    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.
  • HY-160966
    PROTAC BTK Degrader-10
    		Degrader
    PROTAC BTK Degrader-10 (Example 1P) is a PROTAC degrader for BTK. PROTAC BTK Degrader-10 can be used for research of chronic lymphocytic leukemia (CLL)(Pink: ligand for target protein (HY-170758); Black: linker (HY-W392857); Blue: ligand for E3 ligase Cereblon (HY-W733176))
  • HY-170413
    PROTAC BTK Degrader-12
    		Degrader
    PROTAC BTK Degrader-12 (EXAMPLE 19) is a PROTAC-based BTK degrader (Pink & black: BTK ligand & linker (HY-170414); Black: linker (HY-30105); Blue: VHL ligand ( HY-W245311)).
  • HY-154860
    PTD10
    		Degrader
    PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation. (Pink: Btk ligand (HY-19834); Blue: E3 ligase ligand (HY-14658); Black: linker (HY-Y0966); E3 ligase ligand + linker (HY-131717)).
  • HY-159947
    PROTAC BTK Degrader-11
    		Degrader
    PROTAC BTK Degrader-11 is a PROTAC degrader that can break down BTK, with a DC50 of 1.7 nM. PROTAC BTK Degrader-11 can be used in cancer research. (Pink: target protein ligand (HY-159956); Black: linker; Blue: E3 ligase (HY-150839)).