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Pathways Recommended: PROTAC
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PROTAC Linker-1

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39

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4

Click Chemistry

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108371
    Boc-C1-PEG2-C4-Cl

    PROTAC Linker 1

    		 PROTAC Linkers Cancer
    Boc-C1-PEG2-C4-Cl (PROTAC Linker 1) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .
    Boc-C1-PEG2-C4-Cl
  • HY-129938
    PROTAC BRD4 Degrader-24

    		PROTAC-Linker Conjugates for PAC Cancer
    PROTAC BRD4 Degrader-24 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker .
    PROTAC BRD4 Degrader-24
  • HY-101838
    dBET1
    Maximum Cited Publications
    15 Publications Verification

    		 PROTACs Epigenetic Reader Domain Cancer
    dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker .
    dBET1
  • HY-147174
    PROTAC_ERRα

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker .
    PROTAC_ERRα
  • HY-W259932
    Lenalidomide 5'-piperazine

    		Ligands for E3 Ligase Cancer
    Lenalidomide 5'-piperazine is a functionalized cerebellar ligand for PROTAC development that binds an E3 ligand to terminal piperazine for subsequent chemical reactions to produce a protein deactivator with a rigid linker .
    Lenalidomide 5'-piperazine
  • HY-103634
    dFKBP-1
    1 Publications Verification

    		 PROTACs FKBP Cancer
    dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker .
    dFKBP-1
  • HY-75005
    1-Boc-4-carboxymethyl piperazine

    		PROTAC Linkers Cancer
    1-Boc-4-carboxymethyl piperazine is a PROTAC linker. 1-Boc-4-carboxymethyl piperazine can be used in the synthesis of PROTACs (e.g. PROTAC IRAK4 degrader-12 (HY-168586)) .
    1-Boc-4-carboxymethyl piperazine
  • HY-162608
    PROTAC JAK1 degrader 1

    		PROTACs Cancer
    PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC50 of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker) .
    PROTAC JAK1 degrader 1
  • HY-163440
    PROTAC NAMPT Degrader-1

    		PROTACs NAMPT Cancer
    PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC50 value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC50 value of 0.12μM against A2780 cells. (Structure Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .
    PROTAC NAMPT Degrader-1
  • HY-161177
    PROTAC KRAS G12D degrader 2

    		PROTACs Ras Infection
    PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .
    PROTAC KRAS G12D degrader 2
  • HY-162412
    PROTAC AR/AR-V7 degrader-1

    		PROTACs Adrenergic Receptor Apoptosis Cancer
    PROTAC AR/AR-V7 degrader-1 (27c) is a PROTAC-based and dual AR, AR-V7 degrader, with DC50 values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .
    PROTAC AR/AR-V7 degrader-1
  • HY-147052
    Boc-Pip-butyn

    		PROTAC Linkers Cancer
    Boc-Pip-butyn is an Alkyl/ether-based PROTAC linker . Boc-Pip-butyn is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Boc-Pip-butyn
  • HY-158036
    PROTAC STING Degrader-2

    		PROTACs STING Others Inflammation/Immunology
    PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC50=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .
    PROTAC STING Degrader-2
  • HY-161615
    PROTAC ATR degrader-2

    		Apoptosis PROTACs Cancer
    PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
    PROTAC ATR degrader-2
  • HY-111546
    BI-3663
    1 Publications Verification

    		 PROTACs FAK Cancer
    BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .
    BI-3663
  • HY-W190796A
    Mal-PEG3-NH2 TFA

    		PROTAC Linkers Cancer
    Mal-PEG3-NH2 TFA is a linear heterobifunctional PEG crosslinker with Maleimide (HY-W007324) and amine. Mal-PEG3-NH2 TFA is a non-degradable (non-cleavable) PROTAC linker .
    Mal-PEG3-NH2 TFA
  • HY-162791
    (1s,4s)-C1-Piperidine-C1-cyclohexane-C1

    		PROTAC Linkers Cancer
    (1s,4s)-C1-Piperidine-C1-cyclohexane-C1 is a PROTAC linker. (1s,4s)-C1-Piperidine-C1-cyclohexane-C1 can be used to synthesize PROTAC SMARCA2/4-degrader-33 (HY-162741) .
    (1s,4s)-C1-Piperidine-C1-cyclohexane-C1
  • HY-157228
    ACBI3

    		PROTACs Others Cancer
    ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995) .
    ACBI3
  • HY-169372
    (S,R,S)-AHPC-CO-C4-bromine

    		E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-CO-C4-bromine is an E3 Ligase Ligand-linker Conjugate for PROTAC synthesis. (S,R,S)-AHPC-CO-C4-bromine is composed of an E3 Ligase Ligand (HY-125845) and a linker
    (S,R,S)-AHPC-CO-C4-bromine
  • HY-158048
    UNC9036

    		PROTACs STING Inflammation/Immunology
    UNC9036 is a PROTAC-based STING degrader, with a DC50 of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Structure Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker) .
    UNC9036
  • HY-133736
    PROTAC BRD4 Degrader-5-CO-PEG3-N3

    		PROTAC-Linker Conjugates for PAC ADC Cytotoxin Cancer
    PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    PROTAC BRD4 Degrader-5-CO-PEG3-N3
  • HY-158383
    Pomalidomide-CO-C3-PEG4-C6-NH2

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Pomalidomide-CO-C3-PEG4-C6-NH2 is an E3 ligase ligand-linker conjugate part of PROTAC PIPIB degrader 1 (HY-158381). Pomalidomide consists of the E3 ligase ligand Pomalidomide (HY-10984) and a linker .
    Pomalidomide-CO-C3-PEG4-C6-NH2
  • HY-130435
    DBCO-PEG4-amine

    		ADC Linker PROTAC Linkers Cancer
    DBCO-PEG4-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG4-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-amine can be used in the synthesis of FPM-PEG4-DBCO (a homobifunctional azide-to-azide cross-linker) . DBCO-PEG4-amine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    DBCO-PEG4-amine
  • HY-162362
    MS8709

    		PROTACs GLP Receptor Cancer
    MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .
    MS8709
  • HY-162702
    AZ'3137

    		Androgen Receptor PROTACs Cancer
    AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
    AZ'3137
  • HY-143883
    MS143

    		PROTACs Akt Cancer
    MS143 is a potent PROTAC AKT degrader (DC50=46 nM and GI50=0.8 μM in PC3 cells). MS143 induces rapid and robust AKT degradation in a concentration- and time-dependent manner via hijacking the ubiquitin-proteasome system. MS143 can suppress cancer cell growth (Pink: AKT ligand (HY-15431); Blue: E3 ligase ligand (HY-125845); Black: linker) .
    MS143
  • HY-163229
    (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc

    		Ligands for E3 Ligase Autophagy Cancer
    (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc
  • HY-163814
    CDK2 degrader 1

    		PROTACs CDK Cancer
    CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) .
    CDK2 degrader 1
  • HY-163230
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc

    		Ligands for E3 Ligase Autophagy Cancer
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc
  • HY-158113
    CBPD-409

    		Histone Acetyltransferase PROTACs Cancer
    CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
    CBPD-409
  • HY-161369
    CBPD-268

    		PROTACs Histone Acetyltransferase Cancer
    CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
    CBPD-268
  • HY-130604
    DT2216
    1 Publications Verification

    		 Bcl-2 Family PROTACs Apoptosis Cancer
    DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .
    DT2216
  • HY-161410
    WH244

    		PROTACs Apoptosis Bcl-2 Family Cancer
    WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC50=0.6 nM, BCL-2: DC50=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker) .
    WH244
  • HY-163226
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc

    		Ligands for E3 Ligase Autophagy Cancer
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc
  • HY-163227
    (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc

    		Ligands for E3 Ligase Autophagy Cancer
    (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc
  • HY-162704
    JMV7048

    		PROTACs Cancer
    JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .
    JMV7048
  • HY-168555
    YJ1206

    		CDK PROTACs Apoptosis Cancer
    YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
    YJ1206
  • HY-153321
    NX-5948

    BTK-IN-24

    		 Btk PROTACs Inflammation/Immunology Cancer
    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: ligand for target protein; Blue: CRBN; Black: linker) .
    NX-5948
  • HY-159147
    SIA​​IS039

    		PROTACs ROS Kinase Apoptosis Cancer
    SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
    SIA​​IS039

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