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-156104
    CaMKIIα-PHOTAC 2481744-33-4
    CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Molecules such as PHOTAC can catalyze the ubiquitination and degradation of target proteins through the endogenous proteasome under specific wavelengths of light. CaMKIIα-PHOTAC reduces synaptic function under light conditions, and it attenuates the intensity of evoked field excitatory postsynaptic potentials in the mouse hippocampus in response to physiological stimuli. CaMKIIα-PHOTAC plays a critical role in maintaining long-term potentiation and memory capacity in subcellular dendritic domains.
    CaMKIIα-PHOTAC
  • HY-163865
    PROTAC SMARCA2 degrader-13 2568276-72-0
    SMARCA2 degrader-2 (compound I-322) 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-13
  • HY-181705
    PROTAC RTA Degrader-1
    PROTAC RTA Degrader-1 (Compound 3A) is a ricin toxin A chain (RTA) PROTAC degrader. PROTAC RTA Degrader-1 forms stable ternary complexes, maintains sustained hydrogen bonding interactions, and exhibits distinct interaction energy. PROTAC RTA Degrader-1 is applicable to research related to ricin toxin poisoning.
    PROTAC RTA Degrader-1
  • HY-153536
    PROTAC BTK Degrader-3 2563861-90-3
    PROTAC BTK Degrader-3 is a potent BTK degrader with a DC50 value of 10.9 nM of BTK degradation in Mino cells. PROTAC BTK Degrader-3 has the potential for B-cell malignancies, including chronic lymphoid malignancies research.
    PROTAC BTK Degrader-3
  • HY-172368
    PROTAC CARM1/IKZF3 degrader-1
    PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
    PROTAC CARM1/IKZF3 degrader-1
  • HY-181949
    PROTAC BRD9 Degrader-10
    PROTAC BRD9 Degrader-10 is a PROTAC degrader targeting BRD9, with an IC50 of 2.97 μM against BRD9. PROTAC BRD9 Degrader-10 induces BRD9 degradation via the ubiquitin-proteasome system by recruiting the VHL E3 ubiquitin ligase. PROTAC BRD9 Degrader-10 reduces the viability and inhibits the proliferation of myeloid leukemia cells. PROTAC BRD9 Degrader-10 is applicable for the research of acute myeloid leukemia.
    PROTAC BRD9 Degrader-10
  • HY-180961
    His-TERRα 2408835-49-2
    His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer.
    His-TERRα
  • HY-179060
    LAG-3 PROTAC-1
    LAG-3 PROTAC-1 is a potent LAG-3 PROTAC degrader with a DC50 of 0.27 μM. LAG-3 PROTAC-1 can be used in cancer immunology research (pink: LAG-3 ligand (HY-179061); blue: CRBN ligand (HY-10984); black: linker; CRBN ligand + linker (HY-131888A)).
    LAG-3 PROTAC-1
  • HY-180983
    Azo-PROTAC-4C-trans
    Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that can efficiently degrade the BCR-ABL fusion protein and ABL protein. Azo-PROTAC-4C-trans exhibits potent selective anti-proliferative activity against K562 cells. Azo-PROTAC-4C-trans allows real-time, reversible regulation of its activity via UV (to inactivate it) /visible light (to activate it) irradiation. Azo-PROTAC-4C-trans can be used for the study of myeloid leukemia.
    Azo-PROTAC-4C-trans
  • HY-181409
    PROTAC EZH2 Degrader-40 3093642-40-8
    PROTAC EZH2 Degrader-40 (compound 56) is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.35 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-40 can be used for the research of diffuse large B-cell lymphoma.
    PROTAC EZH2 Degrader-40
  • HY-181301
    PROTAC EZH2 Degrader-18 3093642-34-0
    PROTAC EZH2 Degrader-18 (compound E-CH2-B4) is a PROTAC protein degrader targeting EZH2. PROTAC EZH2 Degrader-18 is applicable to lymphoma-related research.
    PROTAC EZH2 Degrader-18
  • HY-160547
    PROTAC AR Degrader-5 2703021-51-4
    PROTAC AR Degrader-5 (compound A46) is a potent AR PROTACs degrader with an IC50 value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration.
    PROTAC AR Degrader-5
  • HY-174862
    dASK1 3064086-31-0
    dASK1 is a selective and cereblon (CRBN)-based PROTAC degrader of apoptosis signal-regulating kinase 1 (ASK1). dASK1 forms a stable ternary complex with ASK1, facilitating ASK1 rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 demonstrates potent ASK1 degradation. dASK1 can be used for the research of steatohepatitis.
    dASK1
  • HY-184329
    PROTAC AURKB Degrader-1 3114874-73-3
    PROTAC AURKB Degrader-1 is a selective AURKB PROTAC degrader with a DC50 value of 0.6 nM. PROTAC AURKB Degrader-1 promotes ubiquitination and degradation of AURKB. PROTAC AURKB Degrader-1 downregulates the expression levels of chromosomal passenger complex components Borealin, INCENP, Survivin as well as the transcription factor YY1. PROTAC AURKB Degrader-1 induces G2/M phase arrest and triggers Apoptosis in cells. PROTAC AURKB Degrader-1 serves as a chemical probe for biological studies of the chromosomal passenger complex. PROTAC AURKB Degrader-1 can be used in research related to acute myeloid leukemia, colorectal cancer, and non-small cell lung cancer.
    PROTAC AURKB Degrader-1
  • HY-174870
    PROTAC ERα Degrader-11
    PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)).
    PROTAC ERα Degrader-11
  • HY-180571
    LUF7996 3104736-80-0
    LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto.
    LUF7996
  • HY-174469
    PROTAC PI3K/110β degrader-2 3070438-79-5
    PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer.
    PROTAC PI3K/110β degrader-2
  • HY-168869
    Tamoxifen-PEG-Clozapine 3104316-29-9
    Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer.
    Tamoxifen-PEG-Clozapine
  • HY-145925C
    (S,R)-CFT8634 2704617-95-6
    (S,R)-CFT8634 (compound 176) is a selective and orally active PROTAC-class BRD9 protein degrader. (S,R)-CFT8634 has the potential to study BRD9-mediated diseases, including but not limited to abnormal cell proliferation. (S,R)-CFT8634 consists of a target protein ligand (red part) BRD9 ligand-5 (HY-169988), an E3 ligase ligand (blue part) CRBN ligand-11 (HY-169989), and a PROTAC linker (black part) 1-(3,3-Difluoro-4-piperidinyl)piperazine (HY-169991). E3 ligase ligand and linker can form E3 Ligase Ligand-linker Conjugate 142 (HY-169990).
    (S,R)-CFT8634
  • HY-162741
    PROTAC SMARCA2/4-degrader-33 2568276-36-6
    PROTAC SMARCA2/4-degrader-33 (compound I-277) is a PROTAC degrader targeting SMARCA2 and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC50s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment.
    PROTAC SMARCA2/4-degrader-33
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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