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 (1334)
Related Products (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC RIPK1 Degrader-1
0 ImagesCat. No.: HY-175370Purity: 99.66%PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma.
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WWZ-11-098
0 ImagesCat. No.: HY-181490WWZ-11-098 is a selective CDK6 PROTAC degrader with DC50 of 2.6 nM. WWZ-11-098 induces degradation of CDK6 in a CRBN-dependent manner, while sparing CDK1, CDK2, CDK4, and CDK9. WWZ-11-098 induces apoptosis, G1-S cell cycle arrest and shows anti-proliferative activity in cancer cells. WWZ-11-098 exhibits antitumor efficacy in a xenograft model without signs of toxicity. WWZ-11-098 can be used for the research of leukemia.
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PROTAC pan-KRAS degrader-1
0 ImagesCat. No.: HY-176489CAS No.: 3043908-63-7PROTAC pan-KRAS degrader-1 is a pan-KRAS PROTAC degrader for degrading different KRAS mutation types, such as G12D, G12C, G12V, and G13D. PROTAC pan-KRAS degrader-1 potently degrades KRAS mutation (G12D) in AGS cells, with a DC50 of 1.1 nM, Dmax of 95%. PROTAC pan-KRAS degrader-1 can be used to search diseases caused by KRAS mutation or amplification, especially cancers such as breast cancer, bladder cancer, gastric cancer, etc.
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EBET-1055
0 ImagesCat. No.: HY-161346EBET-1055 is a bromodomain and extra-terminal (BET) PROTAC degrader. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures.
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cis-MZ 1 hydrate
0 ImagesCat. No.: HY-107425BPurity: 99.0%
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NR-11c
0 ImagesCat. No.: HY-159798Purity: 99.75%NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)).
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TrimTAC1
0 ImagesCat. No.: HY-169355CAS No.: 3095569-91-5TrimTAC1 is a TRIM21-based PROTAC degrader targeting BRD4, with a DC50 of 0.649 nM. TrimTAC1 selectively degrades multimeric proteins, including those localized in biomolecular condensates, while exerting no effect on monomeric proteins in the dilute phase. This degradation effect can be blocked by Bortezomib (HY-10227) or TAK-243 (HY-100487). TrimTAC1 can be used in research related to pancreatic cancer and autoimmune diseases.
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MS115 TFA
0 ImagesCat. No.: HY-173561ACAS No.: 3109377-61-6MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 TFA promotes PRMT5/MEP50 ubiquitination and degradation. MS115 TFA shows anticancer activity against breast cancer.
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MS83
0 ImagesCat. No.: HY-139620CAS No.: 2762181-19-9MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells.
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PROTAC survivin degrader-1
0 ImagesCat. No.: HY-186212CAS No.: 3079079-69-6
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ERK-CLIPTAC
0 ImagesCat. No.: HY-153735CAS No.: 2087490-46-6ERK-CLIPTAC is a ERK CLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer.
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PROTAC AR Degrader-12
0 ImagesCat. No.: HY-179433Purity: 98.52%PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer.
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PF15 TFA
0 ImagesCat. No.: HY-143286APurity: 99.72%PF15 TFA is an orally active FLT3-ITD PROTAC degrader with a DC50 of 76.7 nM and an IC50 of 36 nM against FLT3-ITD. PF15 TFA induces FLT3-ITD protein degradation, thereby downregulating its phosphorylation level. PF15 TFA inhibits the proliferation of FLT3-ITD-positive cells and reduces the phosphorylation level of STAT5, a downstream molecule of FLT3-ITD. PF15 TFA exhibits efficacy in in vivo xenograft models of acute myeloid leukemia and prolongs survival. PF15 TFA can be used for the research of acute myeloid leukemia.
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PROTAC CDK6 Degrader 1
0 ImagesCat. No.: HY-180277Purity: 98.89%PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC50 of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC50 > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML).
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MS115
0 ImagesCat. No.: HY-173561CAS No.: 3109377-60-5MS115 is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 promotes PRMT5/MEP50 ubiquitination and degradation. MS115 shows anticancer activity against breast cancer.
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PROTAC HDAC4 Degrader-2
0 ImagesCat. No.: HY-184524CAS No.: 3035189-46-6PROTAC HDAC4 Degrader-2 is a class IIa selective negative control for HDAC4 PROTAC degraders, with an IC50 of 0.15 μM against HDAC4 and a cellular IC50 of 0.18 μM. PROTAC HDAC4 Degrader-2 fails to effectively recruit the VHL E3 ligase, and thus does not induce significant degradation of HDAC4 protein.
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PTD10
0 ImagesCat. No.: HY-154860CAS No.: 2642231-19-2PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease.
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STAT3-D11-PROTAC-VHL
0 ImagesCat. No.: HY-172767STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting Signal Transducer and Activator of Transcription 3 (STAT3). STAT3-D11-PROTAC-VHL exhibits anti-tumor activity with IC50 values of 1335 nM and 1973 nM against HeLa and MCF-7 cells, respectively. STAT3-D11-PROTAC-VHL binds to the DNA-binding domain of STAT3 and recruits the E3 ligase VHL to form a ternary complex, leading to the ubiquitination of STAT3 and subsequent degradation by the proteasome. STAT3-D11-PROTAC-VHL also inhibits tumor cell growth, induces cell cycle arrest and apoptosis, and suppresses tumor immune evasion.
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aTAG 4531
0 ImagesSynonyms: CFT-4531aTAG 4531 is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC50 of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a Ki of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation.
