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.
Alle PROTACs Isoform-spezifische Produkte anzeigen
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PROTACs Verwandte Produkte (1334)
Verwandte Produkte (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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Pomalidomide-NH-PEG6-amide-C2-CPI-1612
0 ImagesArt. -Nr.: HY-161250Pomalidomide-NH-PEG6-amide-C2-CPI-1612 is a CBP/EP300 PROTAC degrader with a DC50 value of 1.3 μM. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 mediates the formation of a ternary complex between CRBN and the core of CBP, with an EC50 of 1.2 μM. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 inhibits cancer cell growth and exhibits cell line-specific degradation activity. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 can be used in research related to multiple myeloma and leukemia.
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AY-4
0 ImagesArt. -Nr.: HY-174867CAS. Nr.: 3091513-13-9AY-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)).
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BY13
0 ImagesArt. -Nr.: HY-176225CAS. Nr.: 3117131-00-4BY13 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.
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CaMKIIα-PHOTAC
0 ImagesArt. -Nr.: HY-156104CAS. Nr.: 2481744-33-4CaMKIIα-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.
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PROTAC SMARCA2 degrader-13
0 ImagesArt. -Nr.: HY-163865CAS. Nr.: 2568276-72-0PROTAC SMARCA2 degrader-13 is a PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-13 induces ubiquitination of SMARCA2 and SMARCA4 and mediates their degradation via the proteasome. PROTAC SMARCA2 degrader-13 can be used in cancer-related research.
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PROTAC RTA Degrader-1
0 ImagesArt. -Nr.: HY-181705PROTAC 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.
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PROTAC BTK Degrader-3
0 ImagesArt. -Nr.: HY-153536CAS. Nr.: 2563861-90-3
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PROTAC CARM1/IKZF3 degrader-1
0 ImagesArt. -Nr.: HY-172368PROTAC 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))
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PROTAC BRD9 Degrader-10
0 ImagesArt. -Nr.: HY-181949PROTAC 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.
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HaloPROTAC 4
0 ImagesArt. -Nr.: HY-187337HaloPROTAC 4 is a HaloPROTAC degrader with a pIC50 of 8.1 against human CRBN. HaloPROTAC 4 binds to CRBN to recruit the CUL4CRBN E3 ubiquitin ligase complex, and covalently binds to HaloTag fusion proteins, thereby inducing proteasome-dependent degradation of HaloTag fusion proteins. HaloPROTAC 4 serves as a protein knockdown tool for chemogenetic-related studies.
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His-TERRα
0 ImagesArt. -Nr.: HY-180961CAS. Nr.: 2408835-49-2His-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.
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Jak1 RIMTAC-1
0 ImagesArt. -Nr.: HY-187502Jak1 RIMTAC-1 is a JAK1 RIMTAC degrader (a PROTAC-like agent) with a DC50 of 322.8 nM. Jak1 RIMTAC-1 forms a ternary complex with JAK1 and RIPK1, thereby recruiting the VHL E3 ligase complex to ubiquitinate JAK1 via the ubiquitin-proteasome system and mediate its subsequent proteasomal degradation. Jak1 RIMTAC-1 does not alter JAK1 mRNA levels (pink: Jak1 ligand-1 (HY-187503); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-B0704)).
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Azo-PROTAC-4C-trans
0 ImagesArt. -Nr.: HY-180983Azo-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.
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dASK1
0 ImagesArt. -Nr.: HY-174862CAS. Nr.: 3064086-31-0dASK1 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.
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PROTAC AURKB Degrader-1
0 ImagesArt. -Nr.: HY-184329CAS. Nr.: 3114874-73-3PROTAC 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.
