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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Phe-PEG1-Dasa
0 ImagesCat. No.: HY-180962CAS No.: 3037776-73-8Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia.
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JPS014
0 ImagesCat. No.: HY-145815CAS No.: 2669785-76-4JPS014 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 can be used for the research of colon cancer.
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RD-23
0 ImagesCat. No.: HY-168867CAS No.: 3053537-06-4RD-23 is an orally active and selective RET PROTAC degrader, with DC50 values of 5.6 nM and 11.7 nM against RETWT and RETG810C mutants, respectively. RD-23 inhibits purified RET kinase activity with an IC50 of 0.371 nM. RD-23 suppresses the activation of downstream Shc signaling and induces apoptosis. RD-23 can be used for the research of RET-related cancers.
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dCE-2
0 ImagesCat. No.: HY-161958dCE-2 is a CBP/EP300 PROTAC degrader with a DC50 of 40 nM against CBP. dCE-2 forms a ternary complex with the bromodomains of CBP/EP300 and the CRBN E3 ligase, driving proteasomal degradation of CBP/EP300 via positive cooperativity. dCE-2 is applicable to research related to multiple myeloma, prostate cancer, and neuroblastoma.
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PROTAC BTK Degrader-13
0 ImagesCat. No.: HY-168963PROTAC BTK Degrader-13 is a reagent targeting BTK, with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 degrades BTK in a proteasome-dependent manner and inhibits BTK-mediated downstream signaling pathways by reducing the phosphorylation levels of BTK and p38 MAPK. PROTAC BTK Degrader-13 exerts selective cytotoxic effects on BTK-overexpressing lymphoma cells and ITK-positive cells. PROTAC BTK Degrader-13 can be used in studies related to B-cell lymphoma.
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YN14 (mixture of diastereomers)
0 ImagesCat. No.: HY-155356ACAS No.: 3053689-54-3YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356). YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth.
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PROTAC FLT3/CHK1 Degrader-1
0 ImagesCat. No.: HY-178858PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML).
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PROTAC BET Degrader-18
0 ImagesCat. No.: HY-184335CAS No.: 3097564-20-7PROTAC BET Degrader-18 is a PROTAC targeting BET, with a DC50 of 0.676 nM in HEK293-BRD4-HiBiT-KI cells. PROTAC BET Degrader-18 mainly targets and degrades BRD4 (EC50 = 59.91 nM), and exhibits weak degradation activity against BRD2. PROTAC BET Degrader-18 inhibits the expression of downstream oncoprotein c-Myc, thereby inducing cell cycle arrest and apoptosis, while suppressing oncoprotein expression. PROTAC BET Degrader-18 shows antiproliferative activity against acute myeloid leukemia cells and triple-negative breast cancer cells. PROTAC BET Degrader-18 demonstrates antitumor efficacy in xenograft mouse models. PROTAC BET Degrader-18 can be used for the research of acute myeloid leukemia and triple-negative breast cancer.
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PROTAC TEAD1/IAP degrader-2
0 ImagesCat. No.: HY-181537PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research.
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PROTAC SGK3 degrader-2
0 ImagesCat. No.: HY-176823CAS No.: 2381196-78-5PROTAC SGK3 degrader-2 is the cis epimer of PROTAC SGK3 degrader-1 (SGK3-PROTAC1) (HY-125878), with a cis hydroxyl group in its VH032 moiety, which is incapable of binding to the VHL E3 ligase. PROTAC SGK3 degrader-2 exhibits inhibitory activity against SGK3, SGK1, and S6K1 with IC50 values of 0.6 μM, 1.4 μM, and 1.7 μM, respectively, but shows no SGK3 degradation efficiency. PROTAC SGK3 degrader-2 can be used as a control compound to study the specific effects of SGK3-PROTAC1-mediated SGK3 degradation.
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PCC16 chloride
0 ImagesCat. No.: HY-169232PCC16 chloride is a dual PROTAC degrader targeting DHHC3 and PD-L1, with a DC50 of 0.103 μM for PD-L1 degradation. PCC16 chloride induces DHHC3 degradation via the ubiquitin-proteasome pathway by recruiting the CRBN E3 ubiquitin ligase (E3 ubiquitin ligase). By targeting DHHC3-which is essential for PD-L1 palmitoylation and membrane stability-PCC16 chloride reduces PD-L1 levels, decreases PD-L1 membrane retention time, and impairs its immunosuppressive function. PCC16 chloride enhances anti-tumor immunity by disrupting PD-L1-mediated immunosuppression. PCC16 chloride can be used in the research of immune checkpoint blockade-resistant cancers.
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XZ8078
0 ImagesCat. No.: HY-184967XZ8078 is a potent, selective dual-target PROTAC degrader against PARP1 and IKZF3. In Capan-1 cells, XZ8078 exhibits a DC50 of 23.01 nM for PARP1 degradation and a DC50 of 23.20 nM for IKZF3 degradation. XZ8078 upregulates DNA damage markers in a concentration-dependent manner, induces cell cycle arrest, upregulates activated caspases and triggers apoptosis. XZ8078 inhibits tumor growth in both AZD5305-sensitive and AZD5305-resistant xenograft models. XZ8078 can be used for cancer-related research.
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PROTAC MLKL Degrader-2
0 ImagesCat. No.: HY-169072CAS No.: 3103327-20-1PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research.
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PROTAC VEGFR-2 degrader-2
0 ImagesCat. No.: HY-146369CAS No.: 2353417-85-1
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PROTAC FSP1 degrader 1
0 ImagesCat. No.: HY-179384CAS No.: 3096510-51-6PROTAC FSP1 degrader 1 is a highly efficient and selective PROTAC degrader targeting FSP1. PROTAC FSP1 degrader 1 significantly induces the accumulation of intracellular lipid peroxides. PROTAC FSP1 degrader 1 exhibits synergistic induction of ferroptosis with GPX4 inhibitors. PROTAC FSP1 degrader 1 can induce ROS production. PROTAC FSP1 degrader 1 upregulates the mRNA expression of ferroptosis-related proteins (GPX4, FTH1, ACSL4, TfR1, FSP1). PROTAC FSP1 degrader 1 can be used for the study of triple-negative breast cancer.
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PROTAC CDK2-pRb degrader-1
0 ImagesCat. No.: HY-186132CAS No.: 3030276-48-0PROTAC CDK2-pRb degrader-1 is an orally active PROTAC-class degrader of CDK2. PROTAC CDK2-pRb degrader-1 effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811 by inducing ubiquitination and proteasomal degradation of CDK2. PROTAC CDK2-pRb degrader-1 exhibits significant activity against human cells (with EC50 values of 12 nM and 125 nM, respectively). In xenograft models, PROTAC CDK2-pRb degrader-1 effectively inhibits tumor growth and induces tumor stasis, making it suitable for research related to CCNE1-amplified cancers (such as ovarian cancer, gastric cancer, and breast cancer).
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PROTAC Bcl-xL degrader-4
0 ImagesCat. No.: HY-176740CAS No.: 2930759-37-6PROTAC Bcl-xL degrader-4 (Compound 2-38-III) is a Bcl-xL PROTAC degrader. PROTAC Bcl-xL degrader-4 has strong anti-tumor activity against HepG2 cells and HUVEC cells. PROTAC Bcl-xL degrader-4 induces cells apoptosis by decreasing mitochondrial membrane potential and activating the MAPK signaling pathway. PROTAC Bcl-xL degrader-4 significantly inhibits tumor growth in xenograft tumor mouse models.
