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
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PROTACs Related Products (1386)
Related Products (1386)
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Antibodies (1)
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PROTACs Isoform Comparison
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ZJK-807
0 ImagesCat. No.: HY-178497ZJK-807 is a highly efficient and selective KRASG12D PROTAC degrader (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 promotes KRASG12D ubiquitination and degradation. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer.
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MS243
0 ImagesCat. No.: HY-181728MS243 is a potent KRASG12D PROTAC degrader with a DC50 of 4.2 nM. MS243 promotes the proximity between KRASG12D and the VHL E3 ubiquitin ligase, drives the ubiquitination and proteasomal degradation of KRASG12D, and inhibits the proliferation of cancer cells harboring KRASG12D. MS243 can be used in the research of KRASG12D-carrying cancers, such as colon cancer and pancreatic cancer.
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JPS016
0 ImagesCat. No.: HY-145816CAS No.: 2669785-77-5JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 reduces the viability of colon cancer cells and induces Apoptosis. JPS016 activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 is applicable to research related to colon cancer and sepsis cardiomyopathy.
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PROTAC KAT6 Degrader-2
0 ImagesCat. No.: HY-187357PROTAC KAT6 Degrader-2 is a KAT6A PROTAC degrader. PROTAC KAT6 Degrader-2 induces ubiquitination and proteasomal degradation of KAT6A. PROTAC KAT6 Degrader-2 exhibits high maximum fold activity in ternary complex formation assays. PROTAC KAT6 Degrader-2 can be used in studies related to breast cancer.
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XYD190
0 ImagesCat. No.: HY-161494CAS No.: 3040121-23-8XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia.
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PROTAC FLT3/JAK2/BRD4 Degrader-1
0 ImagesCat. No.: HY-175610CAS No.: 3067695-20-6PROTAC FLT3/JAK2/BRD4 Degrader-1 is a FLT3/JAK2/BRD4 PROTAC degrader with DC50 values of 5.23, 0.68, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces cereblon- and proteasome-dependent degradation of FLT3, JAK2, and BRD4 via the ubiquitin-proteasome system. PROTAC FLT3/JAK2/BRD4 Degrader-1 is used in studies related to FLT3 inhibitor-resistant leukemia and acute myeloid leukemia.
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PROTAC EZH2 Degrader-30
0 ImagesCat. No.: HY-181359CAS No.: 3093642-31-7PROTAC EZH2 Degrader-30 (compound 67) is ais a PROTAC protein degrader targeting EZH2 with an IC50 of 6.22 μM against SU-DHL-6 cells. PROTAC EZH2 Degrader-30 can be used for the research of diffuse large B-cell lymphoma.
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PROTAC SMARCA2/4 degrader-18
0 ImagesCat. No.: HY-163871CAS No.: 2568276-91-3
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PROTAC BRD4 Degrader-26
0 ImagesCat. No.: HY-161650CAS No.: 3050769-37-1PROTAC BRD4 Degrader-26 is a light-regulated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-26 induces targeted degradation of BRD4 via the ubiquitin-proteasome system. PROTAC BRD4 Degrader-26 is a degrader that can be inactivated in response to ultraviolet light. PROTAC BRD4 Degrader-26 can be used in breast cancer-related research.
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phoBET1
0 ImagesCat. No.: HY-149328CAS No.: 3033545-34-2phoBET1 is a photolabile PROTAC molecule that, upon photoactivation, functions as a BRD4 PROTAC degrader to trigger BRD4 degradation via the ubiquitin-proteasome system. Activated phoBET1 induces cancer cell apoptosis and inhibits tumor growth in xenograft mouse models. In its inactive caged state, phoBET1 exhibits only extremely low antiproliferative activity against cancer cells. phoBET1 can be applied in studies related to acute myeloid leukemia.
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PROTAC NAMPT Degrader-31
0 ImagesCat. No.: HY-187347PROTAC NAMPT Degrader-31 is a PROTAC degrader that targets and degrades NAMPT by recruiting cereblon. It exhibits DC50 values of 9.31 nM and 12.54 nM against NAMPT in MDA-MB-231 and 4T1 cells, respectively, and an IC50 value of 15.05 nM for NAMPT enzymatic activity. PROTAC NAMPT Degrader-31 induces NAMPT degradation via the ubiquitin-proteasome system, inhibits NAMPT enzymatic activity, and reduces NAD+ levels through the NAD+ salvage pathway. It can be used in research related to triple-negative breast cancer.
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dTAG-TRIMTAC
0 ImagesCat. No.: HY-185652CAS No.: 3070832-72-0dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.
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THNAN69
0 ImagesCat. No.: HY-178122THNAN69 is a PROTAC degrader targeting LIMK2, which efficiently degrades ectopically expressed EGFP-LIMK2 in live HuCCT1 cells with a DC50 of 1 nM. THNAN69 induces isoform-specific ubiquitin-mediated degradation of LIMK2 by recruiting the CRBN E3 ligase, forming a stable ternary complex with LIMK2 and CRBN; this degradation process depends on the activity of cullin-RING ligase. THNAN69 does not reduce phosphorylated cofilin levels, as LIMK1 can compensate for the loss of LIMK2; it also stimulates compensatory activation of the Rho signaling pathway including PAK1/2 and ROCK1/2. THNAN69 serves as a selective chemical probe for dissecting the LIMK2 isoform-dependent biological mechanisms. THNAN69 can be used in the research of cholangiocellular carcinoma and acute lymphoblastic leukemia.
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PROTAC BRD4 Degrader-17
0 ImagesCat. No.: HY-143328CAS No.: 2585561-49-3PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
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PROTAC TTK degrader-2
0 ImagesCat. No.: HY-143905CAS No.: 2953426-48-5PROTAC TTK degrader-2 is a threonine tyrosine kinase (TTK) PROTAC degrader with a DC50 of 3.1 nM in COLO-205 cells. PROTAC TTK degrader-2 induces proteasome-mediated degradation of TTK. It inhibits the proliferation of colorectal cancer cells. In colorectal cancer xenograft mouse models, PROTAC TTK degrader-2 mediates target degradation and exerts anticancer activity. PROTAC TTK degrader-2 can be used in colorectal cancer-related research.
