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bifunctional degrader

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-138642
    Vepdegestrant
    5+ Cited Publications

    ARV-471

    		 PROTACs Estrogen Receptor/ERR Cancer
    Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
    Vepdegestrant
  • HY-153341
    Tagarafdeg

    CFT1946

    		 PROTACs Raf Cancer
    Tagarafdeg (CFT1946) is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. Tagarafdeg can be used in tumor research .
    Tagarafdeg
  • HY-111519
    dTRIM24
    5+ Cited Publications

    		 PROTACs Epigenetic Reader Domain Cancer
    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
    dTRIM24
  • HY-176528
    PROTAC ERK5 degrader-1

    		ERK PROTACs Cancer
    PROTAC ERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. PROTAC ERK5 degrader-1 induces ERK5 degradation via VHL-mediated proteasome pathway in MOLT-4 cells. PROTAC ERK5 degrader-1 can be used for the study of a disease or disorder characterized by aberrant ERK5 activity, such as acute lymphoblastic leukemia .
    PROTAC ERK5 degrader-1
  • 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-148061
    DB1113

    		PROTACs Bcr-Abl CDK Salt-inducible Kinase (SIK) Cyclin G-associated Kinase (GAK) MAP4K MAPKAPK2 (MK2) Ferroptosis ULK LIM Kinase (LIMK) Cancer
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity .
    DB1113
  • HY-153821
    PROTAC KRAS G12C degrader-2

    		Ras PROTACs Cancer
    PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS .
    PROTAC KRAS G12C degrader-2
  • HY-138632
    PROTAC BRD4 Degrader linker conjugate

    		PROTACs Epigenetic Reader Domain PROTAC-Linker Conjugates for PAC Cancer
    PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)) .\n
    PROTAC BRD4 Degrader linker conjugate
  • HY-171860
    FC-14369

    		PROTACs HIV Infection Cancer
    FC-14369 is a PROTAC degrader targeting the HIV-1 Nef protein, with a DC50 value of 160 nM. Through its bifunctional structure, FC-14369 binds to Nef and the Cereblon E3 ubiquitin ligase, induces Nef ubiquitination and proteasomal degradation, restores the expression of cell-surface CD4 and MHC-I, and inhibits HIV-1 replication. FC-14369 can be used in research on HIV infection and AIDS. FC-14369 is applicable to studies related to HIV-1 infection .
    FC-14369
  • HY-144258
    PD-1/PD-L1-IN-14

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    PD-1/PD-L1-IN-14 (compound 17) is a bifunctional inhibitor of PD-1/PD-L1 interactions, with an IC50 of 27.8 nM. PD-1/PD-L1-IN-14 (compound 17) inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1 .
    PD-1/PD-L1-IN-14
  • HY-162809
    XMU-MP-9

    		Ras Cancer
    XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used for the study of colon, lung and pancreatic cancer .
    XMU-MP-9
  • HY-123109
    (S,R,S)-AHPC-Boc

    VH032-Boc

    		 Ligands for E3 Ligase Cancer
    (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology .
    (S,R,S)-AHPC-Boc
  • HY-148062
    RSS0680

    		PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK Others
    RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC with protein kinase degradation activity (Pink: FLT3-IN-17 (HY-148070); Black: Linker (HY-W041970); Blue: E3 ligase Ligand (HY-112078)). RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
    RSS0680
  • 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-161235
    BTX-7312

    		SOS1 Molecular Glues Ras Cancer
    BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers pERK and pS6 and shows antiproliferative activity in various KRAS-mutated cells .
    BTX-7312
  • HY-145403
    PROTAC BRD9 Degrader-4

    		PROTACs Cancer
    PROTAC BRD9 Degrader-4 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-4
  • HY-123109A
    (S,S,S)-AHPC-Boc

    (S,S,S)-VH032-Boc

    		 Ligands for E3 Ligase Cancer
    (S,S,S)-AHPC-Boc is the isomer of (S,R,S)-AHPC-Boc (HY-123109), and can be used as an experimental control. (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology .
    (S,S,S)-AHPC-Boc
  • HY-161233A
    BTX-6654 formate

    		PROTACs SOS1 ERK Cancer
    BTX-6654 formate is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 formate reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
    BTX-6654 formate
  • HY-170405
    YB-3–17

    		PROTACs mTOR Cancer
    YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC50=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC50=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC50 of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))
    YB-3–17
  • HY-145400
    PROTAC BRD9 Degrader-3

    		PROTACs Cancer
    PROTAC BRD9 Degrader-3 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-3
  • HY-161233
    BTX-6654

    		PROTACs SOS1 ERK Cancer
    BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations .
    BTX-6654
  • HY-138642S
    Vepdegestrant-d5

    ARV-471-d5

    		 Isotope-Labeled Compounds Cancer
    Vepdegestrant-d5 (ARV-471-d5) is the deuterium labeled Vepdegestrant (HY-138642). Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a DC50 of about 2 nM .
    Vepdegestrant-d5
  • HY-163811
    BRD9 Degrader-4

    		Molecular Glues Epigenetic Reader Domain Cancer
    BRD9 Degrader-4 (BRD9c), a bifunctional molecular glue, is a potent BRD9 degrader with a DC50 of ≤25 nM. BRD9 Degrader-4 has anti-cancer effects .
    BRD9 Degrader-4
  • HY-153820
    PROTAC BRD4 Degrader-20

    		Epigenetic Reader Domain PROTACs Cancer
    PROTAC BRD4 Degrader-20 (compound 195) is an bifunctional compound and an degrader of BRD4 .
    PROTAC BRD4 Degrader-20
  • HY-142881
    D-MoDE-A (1)

    		LYTACs Others
    D-MoDE-A (1) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).
    D-MoDE-A (1)
  • HY-161236
    KRAS ligand 4

    		Molecular Glues SOS1 Ras Cancer
    KRAS ligand 4 (compound 2) is a bifunctional molecular glue degrader based on SOS1. KRAS ligand 4 reduces downstream signaling markers pERK and pS6 and displays anti-additional activity in cells with multiple KRAS mutations .
    KRAS ligand 4
  • HY-138642A
    (Rac)-Vepdegestrant

    (Rac)-ARV-471

    		 Estrogen Receptor/ERR PROTACs Cancer
    (Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
    (Rac)-Vepdegestrant
  • HY-170769
    FLT3 Ligand-Linker Conjugate 1

    		Target Protein Ligand-Linker Conjugates FLT3 Cancer
    FLT3 Ligand-Linker Conjugate 1 (compound 7) contains the FLT3 ligand and a PROTAC linker, which can recruit the E3 ligase VHL. FLT3 Ligand-Linker Conjugate 1 can be used to synthesize the PROTAC RSS0680 (HY-148062). PROTAC RSS0680 is a bifunctional compound that targets protein degradation of kinases .
    FLT3 Ligand-Linker Conjugate 1
  • HY-179562
    BTK degrader-2

    		Btk Cancer
    BTK degrader-2 (Example 2) is a BTK dual-functional degrading agent, which causes the degradation of BTK through the ubiquitin-proteasome pathway. BTK degrader-2 can be used for the study of B-cell-related diseases .
    BTK degrader-2
  • HY-163812
    ER degrader 9

    		Molecular Glues Estrogen Receptor/ERR Cancer
    ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
    ER degrader 9
  • HY-145395
    PROTAC BRD9 Degrader-2

    		PROTACs Cancer
    PROTAC BRD9 Degrader-2 is a BRD9 bifunctional degrader for researching cancer.
    PROTAC BRD9 Degrader-2
  • HY-142885
    M-MoDE-A (2)

    		LYTACs Others
    M-MoDE-A (2) is a bifunctional small molecule that mediates the degradation of extracellular proteins through the asialoglycoprotein receptor (ASGPR).
    M-MoDE-A (2)
  • HY-153665
    Deg-1

    		Biochemical Assay Reagents Others
    Deg-1 is a a bifunctional probe with a cleavage group and a covalent binding group. Deg-1 covalently binds to the target nucleic acid, and serves as click-degrader to cleave a nucleic acid molecule. Deg-1 has potential to selectively cleave target nucleic acids in cells . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
    Deg-1
  • HY-175445
    GNE-5472

    		PROTACs Estrogen Receptor/ERR IAP NF-κB TNF Receptor Apoptosis Cancer
    GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer .
    GNE-5472
  • HY-171441
    STAT6 degrader-1

    		STAT Inflammation/Immunology Cancer
    STAT6 degrader-1 (Compound 21) is a bifunctional molecular glue degrader of STAT6 that recruits E3 ubiquitin ligase. STAT6 degrader-1 induces proteasomal degradation of STAT6. STAT6 degrader-1 is applicable to the research of cancer, inflammatory diseases and colorectal cancer .
    STAT6 degrader-1
  • HY-181499
    RA190-PEG1-NH2

    		Proteasome Cancer
    RA190-PEG1-NH2 (Compound S16), RA190 (HY-100739) derivative, is a Proteasome ligand. RA190-PEG1-NH2 can be used to synthesis FKBP12 CAP-TAC degrader RAFKBP12 (HY-181498) .
    RA190-PEG1-NH2
  • HY-178519
    JQ-1 (carboxylic acid)-NH-C8-COOH

    		Target Protein Ligand-Linker Conjugates Cancer
    JQ-1 (carboxylic acid)-NH-C8-COOH is a synthetic target protein ligand-conjugate linker, which can be used to synthesize JQ1-S(GlcNAc)Cq (HY-178510). JQ1-S(GlcNAc)Cq is a potent Sugar-Coated PROTAC bifunctional degrader with anti-tumor activity .
    JQ-1 (carboxylic acid)-NH-C8-COOH
  • HY-171342
    Mal-C2-amide-C10-tri-GalNAc

    		LYTACs Inflammation/Immunology
    Mal-C2-amide-C10-tri-GalNAc (Compound 1226) is an asialoglycoprotein receptor (ASGPR) binding ligand fragment and a component of lysosome-targeted bifunctional molecules. Mal-C2-amide-C10-tri-GalNAc promotes the sequestration and degradation of extracellular target molecules in lysosomes. Mal-C2-amide-C10-tri-GalNAc is used in the research of autoimmune diseases .
    Mal-C2-amide-C10-tri-GalNAc
  • HY-180485
    PROTAC D16-M1P2

    		PROTACs Wee1 CDK Cancer
    PROTAC D16-M1P2 is an orally active PKMYT1 PROTAC degrader with a DC50 of 0.7 nM. PROTAC D16-M1P2 also inhibits the activity of PKMYT1 with an IC50 of 7.6 nM. PROTAC D16-M1P2 inhibits pCDK1 with an IC50 of 9 nM. PROTAC D16-M1P2 has demonstrated significant anti-tumor efficacy in mouse models and can be used for research on breast cancer .
    PROTAC D16-M1P2
  • HY-181607
    TEAD ligand-Linker Conjugate 3

    		YAP Others
    TEAD ligand-Linker Conjugate 3 (the blue structure + black structure of A536 in the literature) is a conjugate of a TEAD1-targeting ligand and a linker. TEAD ligand-Linker Conjugate 3 can be coupled with an IAP ligand (HY-181531) to form an IAP-recruiting bifunctional protein degrader (IPD) (HY-181594), also known as a SNIPER degrader. This TEAD SNIPER simultaneously binds to the TEAD1 palmitoylation pocket and the BIR3 domain of cIAP1 to form a ternary complex, efficiently inducing the ubiquitination and degradation of both TEAD1 and cIAP1 (DC50=110 nM, Dmax=51%; IC50=122 nM for cIAP1). TEAD ligand-Linker Conjugate 3 and its synthesized SENIPER molecule can be utilized in research on Hippo pathway dysregulation-related diseases, such as NF2-mutant tumors .
    TEAD ligand-Linker Conjugate 3
  • HY-182964
    WY165

    		ClpP Cardiovascular Disease Neurological Disease Metabolic Disease Cancer
    WY165 is a bifunctional molecule comprising TR79, an activator of the mitochondrial protease complex caseinolytic protease P (ClpP), linked to desthiobiotin. WY165 mediates selective degradation of monomeric streptavidin (mSA) and its fusion proteins localized to the mitochondrial matrix with a DC50 of 197 nM. WY165 restores mitochondrial morphology by reducing the level of mSA fused to short transmembrane protein 1 (mSA-STMP1) in cells overexpressing mSA-STMP1. WY165 can be used for research in cancer, neurodegenerative diseases, cardiovascular diseases, and metabolic diseases .
    WY165

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