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.
PROTACs Isoform Specific Products
All Product Categories
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PROTACs Related Products (1355)
Related Products (1355)
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Antibodies (1)
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PROTACs Isoform Comparison
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LC-2 epimer
0 ImagesCat. No.: HY-137516ACAS No.: 2502156-12-7
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Akt RIMTAC-1
0 ImagesCat. No.: HY-187500Akt RIMTAC-1 is a Akt RIMTAC degrader (a PROTAC-like agent) with a DC50 of 3.52 μM. Akt RIMTAC-1 forms a ternary complex with AKT and RIPK1, and recruits the VHL E3 ligase complex to mediate ubiquitination and proteasomal degradation. Akt RIMTAC-1 does not alter AKT1 mRNA levels (pink: AKT ligand-5 (HY-187501); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-23166)).
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PROTAC BRD4 Degrader-43
0 ImagesCat. No.: HY-181164PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection. (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))
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GNF-2-deg
0 ImagesCat. No.: HY-161804GNF-2-deg is a PROTAC degrader targeting the dengue virus envelope protein (DENV E protein), with a DC50 of 0.83 μM in Huh7.5 cells. GNF-2-deg induces CRBN- and proteasome-dependent proteolysis of intracellular E protein. GNF-2-deg inhibits E protein-mediated membrane fusion and blocks viral particle production. GNF-2-deg reduces viral yield in infected cells and retains activity against E protein βOG pocket mutant virus-like particles (VLP). GNF-2-deg can be used in the research of dengue virus infection, Zika virus infection, Japanese encephalitis, West Nile virus infection and yellow fever.
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PROTAC PI3Kδ degrader-1
0 ImagesCat. No.: HY-176239PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model.
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PROTAC ATR degrader-3
0 ImagesCat. No.: HY-182016CAS No.: 3126270-11-6PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.
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PROTAC CBP/EP300 degrader-1
0 ImagesCat. No.: HY-184453PROTAC CBP/EP300 Degrader-5 is a CBP and EP300 PROTAC degrader. PROTAC CBP/EP300 Degrader-5 relies on the ubiquitin-proteasome pathway to preferentially induce ubiquitination and degradation of EP300 rather than CBP. PROTAC CBP/EP300 Degrader-5 induces G1 phase cell cycle arrest and triggers Apoptosis. PROTAC CBP/EP300 Degrader-5 is applicable to research related to EP300-dependent malignant tumors.
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dASK1-VHL
0 ImagesCat. No.: HY-174858dASK1-VHL is an orally active PROTAC degrader targeting ASK1. dASK1-VHL can effectively bind VHL and promote the selective degradation of ASK1. dASK1-VHL effectively reduces ASK1 protein levels, inhibits the activation of p38 MAPK, and reduces liver lipid content. dASK1-VHL provides new ideas for the study of Metabolic dysfunction-associated steatohepatitis (MASH).
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PROTAC EGFR degrader 17
0 ImagesCat. No.: HY-180917CAS No.: 3065209-64-2
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PROTAC SOS1 degrader-10
0 ImagesCat. No.: HY-161654CAS No.: 3043923-74-3PROTAC SOS1 degrader-10 is a SOS1 PROTAC degrader dependent on CRBN and the proteasome. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS-mutant cancer cells SW620, A549 and DLD-1, with DC50 values of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits ERK phosphorylation. PROTAC SOS1 degrader-10 suppresses the proliferation of KRAS-mutant cancer cells via antiproliferative activity. PROTAC SOS1 degrader-10 can be used in studies related to KRAS-mutant cancers.
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rel-Vepdegestrant
0 ImagesCat. No.: HY-138642BCAS No.: 2614417-52-4Synonyms: rel-ARV-471; rel-PF-07850327(Rac)-Vepdegestrant is the relative configuration of Vepdegestrant (HY-138642). Vepdegestrant is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM.
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PROTAC SMARCA2/4 degrader-27
0 ImagesCat. No.: HY-162834CAS No.: 2375564-54-6PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research[1].
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LJM133
0 ImagesCat. No.: HY-183007LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC50 values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer.
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DOT1L705
0 ImagesCat. No.: HY-181787CAS No.: 3050756-34-5
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PROTAC SMARCA2 degrader-30
0 ImagesCat. No.: HY-168257CAS No.: 2408393-67-7
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PROTAC BRD4 Degrader-3
0 ImagesCat. No.: HY-135558CAS No.: 2313234-00-1
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JHK-02-108-2
0 ImagesCat. No.: HY-184910JHK-02-108-2 is a PROTAC degrader targeting CDK6, with an EC50 of 0.22 μM and a Kd of 1.9 μM. JHK-02-108-2 selectively promotes CRBN-dependent ubiquitination and proteasomal degradation of CDK6. JHK-02-108-2 induces sustained cell cycle arrest at the G1 phase. JHK-02-108-2 reduces the phosphorylation level of retinoblastoma protein. JHK-02-108-2 can be used in research related to acute myeloid leukemia and glioblastoma.
