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-162967
    MS8588 3060519-94-7
    MS8588 is the first DUBTACs for cGAS, a key component of the cGAS-STING pathway.
    MS8588
  • HY-162626
    FGFR2 degrader 1
    FGFR2 degrader 1 (compound 28E) is a selectively PROTACS degrader of FGFR2, with the DC50 of 0.645 nM. FGFR2 plays an important role in cancer research (Pink: ligand of target protein; (HY-13304) black: linker; blue: ligand of E3 ligase).
    FGFR2 degrader 1
  • HY-168722
    PROTAC PARP1 degrader-3
    PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader for PARP1 with a DC50 of 58.14 nM. PROTAC PARP1 degrader-3 exhibits cytotoxicity in cancer cell SW-620 and LOVO with IC50 of 1.63 μM and 2.84 μM. PROTAC PARP1 degrader-3 exhibits a synergistic effect with SN-38 (HY-13704) in BRCA-mutated colon cancer cell with a combination index (CI) of 0.487. (Blue: Ligand for E3 ligase Cereblon (HY-23095); Pink: Ligand for target protein (HY-10619); Black: Linker (HY-16872))
    PROTAC PARP1 degrader-3
  • HY-159453
    PROTAC SMARCA2/4-degrader-2 2568277-76-7
    SMARCA2/4-degrader-2 (compound I-431) 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-2
  • HY-D2336
    PROTAC Aster-A degrader-1
    PROTAC Aster-A degrader-1 (compound NGF3) is a degrader of the sterol transport protein Aster-A. PROTAC Aster-A degrader-1 can be used as a fluorescence probe. (Red: Aster-A inhibitor, black: linker, Blue: E3 ligase ligand).
    PROTAC Aster-A degrader-1
  • HY-168637
    SIAIS562055
    SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity. (Pink: SOS1 ligand (HY-168638); Black: linker (HY-W539874); Blue: E3 ligase ligand (HY-W076696)).
    SIAIS562055
  • HY-141878
    di-Ellipticine-RIBOTAC 2767983-76-4
    Di-Ellipticine-RIBOTAC (Compound 7) is a RNA RIBOTAC degrader, capable of specifically binding and degrading r(G4C2)exp. Di-Ellipticine-RIBOTAC only cuts the expanded GGGGCC repeat RNA in the pathogenic factor of amyotrophic lateral sclerosis/ frontotemporal dementia (c9ALS/FTD) - the chromosome 9 open reading frame 72 (9orf72) gene (r(G4C2)exp), and has no effect on normal short repetitive sequences. Di-Ellipticine-RIBOTAC significantly improves the pathological phenotype of c9ALS/FTD in cells and mouse models. Di-Ellipticine-RIBOTAC can be used for the study of c9ALS/FTD.
    di-Ellipticine-RIBOTAC
  • HY-155643
    PROTAC TG2 degrader-1 3033465-55-0
    PROTAC TG2 degrader-1 (compound 11) is a von Hippel-Lindau (VHL)-based PROTAC targeting tissue transglutaminase (TG2) with a KD of 68.9 μM. PROTAC TG2 degrader-1 reduces TG2 in ovarian cancer cells in a proteasome-dependent manner.
    PROTAC TG2 degrader-1
  • HY-174401
    PROTAC HDAC6 degrader 5
    PROTAC HDAC6 degrader 5 (Compound 5a) is a highly selective PROTAC targeting HDAC6. PROTAC HDAC6 degrader 5 can effectively degrade HDAC6 in cells (IC50 = 43 nM). PROTAC HDAC6 degrader 5 reduces HDAC6 levels through proteasome- and CRBN-dependent mechanisms (Pink: Target protein ligand (HY-174408), Target protein ligand + linker (HY-174409); Blue: Pomalidomide (HY-10984), Pomalidomide 4'-alkylC3-azide (HY-139341)).
    PROTAC HDAC6 degrader 5
  • HY-153938
    PROTAC PTPN2 degrader-2 2912307-38-9
    PROTAC PTPN2 degrader-2 (example 187B) is a potent PTPN2 degrader with potential for studying cancer or metabolic diseases.
    PROTAC PTPN2 degrader-2
  • HY-161250
    Pomalidomide-NH-PEG6-amide-C2-CPI-1612
    Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader, which contains a CRBN ligands Pomalidomide, a 24-atom linker with 6 PEG units and a HAT inhibitor CPI-1612. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 exhibits antiproliferative effects in cells multiple myeloma cells LP1 (with a DC50 of 1.2 μM), MM1S and various cancer cell lines, especially the leukemia cells.
    Pomalidomide-NH-PEG6-amide-C2-CPI-1612
  • HY-174867
    AY-4
    AY-4 (Compound AY-4) is an efficient PROTAC degrader targeting FTH1 (Kd = 3.17 nM). AY-4 effectively upregulates the levels of ferrous (Fe2+) and ferric (Fe3+) ions in cells. AY-4 is a potential anticancer candidate compound that regulates iron homeostasis through ferritin degradation and enhances the efficacy of existing drugs. AY-4 can effectively reduce the level of FTH1 in breast cancer cells (Pink: FTH1 ligand AY-2 (HY-174871); Blue: E3 ligand Pomalidomide (HY-10984); Black: Linker, Pomalidomide-PEG3-acid (HY-174872)).
    AY-4
  • HY-176225
    BY13
    BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model. Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
    BY13
  • HY-161108
    PROTAC Chk1 degrader-1 2597167-34-3
    PROTAC Chk1 degrader-1 (Compound PROTAC-2 ) is a potent PROTAC-targeted degrader of Chk1 with a DC50 of 1.33 μM. PROTAC Chk1 degrader-1 can be used in cancer research.
    PROTAC Chk1 degrader-1
  • 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-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-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-176919
    PROTAC STAT6 degrader-3 3077385-98-6
    PROTAC STAT6 degrader-3 (Compound I-677) is a potent STAT6 PROTAC degrader with a DC50 of less than 1 nM. PROTAC STAT6 degrader-3 can be used for research on allergic/inflammatory diseases and cancer.
    PROTAC STAT6 degrader-3
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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