1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-145816
    JPS016 2669785-77-5
    JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 reduces the viability of colon cancer cells and induces Apoptosis. JPS016 activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 is applicable to research related to colon cancer and sepsis cardiomyopathy.
    JPS016
  • HY-182775
    PROTAC KAT6 Degrader-1
    PROTAC KAT6 Degrader-1 is a CRBN-dependented KAT6 PROTAC degrader. PROTAC KAT6 Degrader-1 inhibits cancer cells proliferation.
    PROTAC KAT6 Degrader-1
  • HY-161494
    XYD190 3040121-23-8
    XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496)).
    XYD190
  • HY-111841
    PROTAC CRABP-II Degrader-2 1225383-38-9
    PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
    PROTAC CRABP-II Degrader-2
  • HY-181553
    PROTAC BRD4 Degrader-44
    PROTAC BRD4 Degrader-44 is a BRD4 PROTAC degrader with a DC50 of 16 nM. PROTAC BRD4 Degrader-44 is applicable to studies on membrane-permeable PROTACs.
    PROTAC BRD4 Degrader-44
  • HY-175610
    PROTAC FLT3/JAK2/BRD4 Degrader-1 3067695-20-6
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)).
    PROTAC FLT3/JAK2/BRD4 Degrader-1
  • HY-181359
    PROTAC EZH2 Degrader-30 3093642-31-7
    PROTAC EZH2 Degrader-30 (compound 67) is ais a PROTAC protein degrader targeting EZH2 with an IC50 of 6.22 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-30 can be used for the research of diffuse large B-cell lymphoma.
    PROTAC EZH2 Degrader-30
  • HY-168863
    FF2049
    FF2049 is a selective HDAC PROTAC degrader (DC50 = 257 nM for HDAC1). FF2049 promotes ubiquitination and degradation of HDAC. FF2049 promotes Apoptosis. FF2049 can be used for the research of hematological and solid cancer (Pink: POI ligand 1 (HY-168864); Blue: E3 ligase FEM1B ligand (HY-168865)).
    FF2049
  • HY-163871
    PROTAC SMARCA2/4-degrader-18 2568276-91-3
    PROTAC SMARCA2/4-degrader-18 (Compound I-348) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-18 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159531); Black: Linker (HY-76547); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-18
  • HY-161650
    PROTAC BRD4 Degrader-26 3050769-37-1
    PROTAC BRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC, which degrades 80% BRD4 at 1 μM by using photocleavable linker. PROTAC BRD4 Degrader-26 will be deactivated by UV light. (Pink: ligand for target protein BRD4 ligand 6 (HY-161651); Black: linker (HY-161653); Blue: E3 ligase ligand Thalidomide 4-fluoride (HY-41547))
    PROTAC BRD4 Degrader-26
  • HY-149328
    phoBET1 3033545-34-2
    phoBET1 is a photocaged-PROTAC. phoBET1 can achieve BRD4 degradation and effectively suppress tumor growth.
    phoBET1
  • HY-163872
    PROTAC SMARCA2/4-degrader-10 2568277-33-6
    PROTAC SMARCA2/4-degrader-10 (compound I-399) is a potent SMARCA2 degrader with an DC50 value of <100 nM. PROTAC SMARCA2/4-degrader-10 has the potential for the research of cancer (Blue:SMARCA2/4 ligand, (HY-159542); Black: linker (HY-W088435); Pink:VHL ligand (HY-125845)).
    PROTAC SMARCA2/4-degrader-10
  • HY-185652
    dTAG-TRIMTAC 3070832-72-0
    dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.
    dTAG-TRIMTAC
  • HY-181412
    PROTAC EZH2 Degrader-43 3093642-24-8
    PROTAC EZH2 Degrader-43 (compound 59) is a PROTAC protein degrader targeting EZH2 with an IC50 of 21.73 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-43 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-43
  • HY-143328
    PROTAC BRD4 Degrader-17 2585561-49-3
    PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
    PROTAC BRD4 Degrader-17
  • HY-143905
    PROTAC TTK degrader-2 2953426-48-5
    PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.
    PROTAC TTK degrader-2
  • HY-178176
    PROTAC CB1R Degrader-1
    PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)).
    PROTAC CB1R Degrader-1
  • HY-159016
    SIAIS630121-NC 3094092-93-7
    SIAIS630121-NC (compound 630121-NC) is a negative control for NAMPT (nicotinamide phosphoribosyltransferase) PROTAC degrader SIAIS630121. SIAIS630121-NC shows no NAMPT degradation capability at all.
    SIAIS630121-NC
  • HY-163920
    PROTAC HDAC8 Degrader-1 3057302-08-3
    Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC50 of 0.27 nM in A549 cells.
    PROTAC HDAC8 Degrader-1
  • HY-162745
    SMARCA2 degrader-20 2568273-85-6
    SMARCA2 degrader-20 is a PROTAC SMARCA2 degrader with a DC50 less than 100 nM in A549 cells.
    SMARCA2 degrader-20
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