2. Signaling Pathways
  3. PROTAC
  4. PROTACs

PROTACs

PROTACs

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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.

PROTACs Isoform Specific Products:

PROTACs Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-162742
    PROTAC SMARCA2 degrader-16 2568276-37-7
    PROTAC SMARCA2 degrader-16 (compound I-278) is a PROTAC degrader targeting SMARCA2; it degrades SMARCA2 proteins in A549 cells with an DC50 <100 nM, and a maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2 degrader-16
  • HY-175392
    PROTAC sEH-degrader-3 3093413-94-3
    PROTAC sEH-degrader-3 (Compound 1a) is a targeted sEH PROTAC degrader that can selectively degrade sEH in the cytosol without affecting sEH in peroxisomes. PROTAC sEH-degrader-3 degrades sEH through a CRBN-dependent lysosomal pathway rather than the proteasome, with an IC50 of 0.8 nM against hsEH. PROTAC sEH-degrader-3 can inhibit endoplasmic reticulum stress and can be used in the research of inflammation, metabolic diseases, and other diseases related to endoplasmic reticulum stress. (Pink: sEH inhibitor (HY-114266); Black: Linker (HY-W008352); Blue: E3 Ligase Ligand (HY-14658)).
    PROTAC sEH-degrader-3
  • HY-159457
    PROTAC SMARCA2/4-degrader-6 2568277-87-0
    PROTAC SMARCA2/4-degrader-6 (compound I-438) is a SMARCA2/4 degrader. PROTAC SMARCA2/4-degrader-6 has the potential for the research of cancer. (Pink: SMARCA2/4 ligand, (HY-159545); Black: linker (HY-W006635); Blue: VHL ligand (HY-112078)).
    PROTAC SMARCA2/4-degrader-6
  • HY-178472
    AurAP14
    AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker).
    AurAP14
  • HY-162240
    SJH1-51B
    SJH1-51B is a potent PROTAC degrader of BRD4. SJH1-51B has anti-tumor effect.
    SJH1-51B
  • HY-161173
    PROTAC SOS1 degrader-5 2836273-61-9
    PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC50 of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC50 of 5 nM.
    PROTAC SOS1 degrader-5
  • HY-130612
    PROTAC BRD2/BRD4 degrader-1 2570470-42-5
    PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
    PROTAC BRD2/BRD4 degrader-1
  • HY-175459
    PROTAC FAK degrader 3
    PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3 induces FAK degradation dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker).
    PROTAC FAK degrader 3
  • HY-146422
    PROTAC EGFR degrader 5 2409793-36-6
    PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFRDel19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.
    PROTAC EGFR degrader 5
  • HY-175358
    PROTAC USP7 Degrader-1
    PROTAC USP7 Degrader-1 (Compound 40) is a ubiquitin-specific protease 7 (USP7) PROTAC degrader with a DC50 of 25 nM. PROTAC USP7 Degrader-1 can be used for cancers like acute myeloid leukemia (AML) research. Pink: USP7 ligand (HY-175359); Blue: VHL ligase ligand (HY-112078); Black: linker
    PROTAC USP7 Degrader-1
  • HY-174811
    PROTAC BRD4 Degrader-33
    PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model. Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
    PROTAC BRD4 Degrader-33
  • HY-158325
    PROTAC FLT-3 degrader 4 2956722-48-6
    PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor).
    PROTAC FLT-3 degrader 4
  • HY-162282
    PROTAC METTL3-14 degrader 1
    PROTAC METTL3-14 degrader 1 (compound 30) is a PROTAC degrader of METTL3-14. PROTAC METTL3-14 degrader 1 shows a 50% or higher degradation of METTL3 and/or METTL14(Pink: Ligand for target protein (HY-115717); Black: Linker (HY-168686); Blue: Ligand for E3 ligase (HY-10984)).
    PROTAC METTL3-14 degrader 1
  • HY-156566
    PROTAC BRD4 Degrader-21 2503036-46-0
    PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research.
    PROTAC BRD4 Degrader-21
  • HY-169389
    OICR41114
    OICR41114 (PROTAC 4) is a WDR5-targeting PROTAC degrader. OICR41114 degrades endogenous WDR5 with an EC50 and Dmax values of 40 nM and 49%, respectively. OICR41114 degrades HiBiT-tagged WDR5 in a proteasome-dependent manner. OICR41114 is composed of target protein ligand (red part) Dimethyl-F-OICR-9429-COOH (HY-141799), E3 ligase ligand (blue part) OICR-8268-acrylic acid (HY-169390) and PROTAC linker (black part) Amino-PEG9-amine (HY-140210). The conjugate of E3 ligase ligand and linker is OICR-8268-acrylic acid-amino-PEG9-amine (HY-169391).
    OICR41114
  • HY-173369
    PROTAC MAGL degrader-1
    PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249).
    PROTAC MAGL degrader-1
  • HY-162589
    Lw13
    Lw13 is a Hsp90-targeting PROTAC and achieves maximum degradation at a concentration of 0.05 μM in Siha cells. Lw13 induces cell apoptosis and exhibits potent anti-tumor activity both in vitro and in vivo(Sturcture Note:(Blue: Cereblon ligand (HY-A0003), Black: linker；Pink: Hsp90 inhibitor SNX-5422 (HY-10213)).
    Lw13
  • HY-149495
    CP-07
    CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer.
    CP-07
  • HY-174877
    PROTAC HDAC6 degrader 6
    PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ∼50% Dmax only upon activation to its cis-state with 390 nm light irradiation. Pink: HDAC6 ligand; Blue: CRBN ligase ligand (HY-A0003); Black: linker
    PROTAC HDAC6 degrader 6
  • HY-158036
    PROTAC STING Degrader-2 3023095-61-3
    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
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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