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 (1378)
Related Products (1378)
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Antibodies (1)
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PROTACs Isoform Comparison
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(4S)-PROTAC SOS1 degrader-1
0 ImagesCat. No.: HY-144657CAS No.: 2913176-81-3(4S)-PROTAC SOS1 degrader-1 is a stereoisomer of PROTAC SOS1 degrader-1 (HY-145737). PROTAC SOS1 degrader-1 (Compound 9d) is a degrader of SOS1 PROTAC, with a DC50 of 98.4 nM and a Kd value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers.
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PROTAC HIF-1α degrader-2
0 ImagesCat. No.: HY-179424CAS No.: 3095636-64-6PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex. PROTAC HIF-1α degrader-2 inhibits HeLa cell proliferation, migration, and colony formation, and induces apoptosis. PROTAC HIF-1α degrader-2 reduces p-MEK and p-AKT expression in the MAPK and PI3K/AKT pathways. PROTAC HIF-1α degrader-2 can be used for the study of cervical cancer.
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PROTAC Bcl-xL degrader-1
0 ImagesCat. No.: HY-131188CAS No.: 2450351-07-0PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
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(S)-GNE-987
0 ImagesCat. No.: HY-129937CAS No.: 2738533-33-8(S)-GNE-987 is an isomer of GNE-987 (HY-129937A), which loses VHL binding capacity and BRD4 protein degradation activity, but retains BRD4 inhibitory activity. (S)-GNE-987 is a BRD4/BET inhibitor that potently binds to the BD1 and BD2 bromodomains of BRD4, with a BRD4 BD1 IC50 of 4.0 nM and a BRD4 BD2 IC50 of 3.9 nM. (S)-GNE-987 inhibits MYC expression and exhibits inhibitory activity against acute myeloid leukemia cells, whereas its CLL1‑6 antibody-drug conjugate shows almost no in vivo antitumor efficacy in the HL‑60 xenograft tumor model. (S)-GNE-987 can be used in related research on acute myeloid leukemia.
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PROTAC ALK degrader-4
0 ImagesCat. No.: HY-179732PROTAC ALK degrader-4 is a ALK PROTAC degrader with a DC50 of 445.25 nM. PROTAC ALK degrader-4 induces concentration- and time-dependent degradation of EML4-ALK, as well as concentration-dependent degradation of ALKF1174L. PROTAC ALK degrader-4 downregulates 390 proteins in NCI-H3122 cells, including the targets of ceritinib (ALK, IGF-1R) and downstream molecules ERK1/2 and STAT3. PROTAC ALK degrader-4 exerts antiproliferative activity in ALK-positive cancer cells. ALK degrader-4 can be used in studies related to lung adenocarcinoma.
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UNC9036
0 ImagesCat. No.: HY-158048CAS No.: 3094059-54-5UNC9036 is a STING PROTAC degrader with a DC50 value of 227 nM. UNC9036 binds to and activates STING, recruits the VHL E3 ligase to target phosphorylated STING for ubiquitination and proteasomal degradation. UNC9036 inhibits downstream innate immune signaling events triggered by cytoplasmic DNA sensing, including IRF3 phosphorylation. UNC9036 reduces the antiviral response of cells infected with HSV-1. UNC9036 can be used in the research of renal cell carcinoma.
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PROTAC K-Ras Degrader-6
0 ImagesCat. No.: HY-168678CAS No.: 3052745-46-4PROTAC K-Ras Degrader-6 (compound 102) is a potent cereblon-based KRAS PROTAC degrader, with a DC50 of ≤100 nM. PROTAC K-Ras Degrader-6 shows anticancer effects.
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Truly-4
0 ImagesCat. No.: HY-187439Truly-4 is a bifunctional Rpn13 PROTAC and CRBN ByeTAC degrader. Degradation of Rpn13 relies on CRBN-mediated E3 ubiquitin ligase activity, while degradation of CRBN itself proceeds via a ByeTAC mechanism of action. Truly-4 induces selective cytotoxicity in hematological cancer cells and solid cancer cells, but not in healthy cells, despite comparable levels of Rpn13 depletion in both cell types. Truly-4 can be used in studies related to B-cell lymphoma and triple-negative breast cancer.
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PROTAC HPK1 Degrader-4
0 ImagesCat. No.: HY-174135PROTAC HPK1 Degrader-4 is an orally active HPK1 PROTAC degrader and immune activator, with DC50 values of 3.16 nM and 72.59 nM in Jurkat cells and PBMCs, respectively. PROTAC HPK1 Degrader-4 induces degradation via the ubiquitin-proteasome system, downregulates the HPK1-SLP76 signaling pathway, reduces the phosphorylation level of SLP76 (S376), and promotes immune activation. PROTAC HPK1 Degrader-4 can be used in the research of colorectal cancer and B-cell lymphoma.
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PROTAC BRD9 Degrader-8
0 ImagesCat. No.: HY-162651CAS No.: 3081180-48-2PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
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PROTAC BRD4-DCAF1 degrader-1
0 ImagesCat. No.: HY-169151CAS No.: 3036944-87-0
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PROTAC MLKL Degrader-3
0 ImagesCat. No.: HY-182343PROTAC MLKL Degrader-3 is a MLKL PROTAC degrader with DC50 values of 248.9 nM (Hepa1-6) and 271.3 nM (HepG2), respectively. PROTAC MLKL Degrader-3 induces proteasome- and cereblon-dependent MLKL degradation via ubiquitination. PROTAC MLKL Degrader-3 reduces intratumoral MLKL levels and inhibits tumor growth in mice. PROTAC MLKL Degrader-3 can be used in the research of hepatocellular carcinoma.
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PROTAC BRM degrader-1
0 ImagesCat. No.: HY-163152CAS No.: 2378051-80-8PROTAC BRM degrader-1 is a VHL-recruiting PROTAC degrader that exhibits higher selectivity for the degradation of SMARCA2 (BRM) over its highly homologous protein SMARCA4 (BRG1). The KD values of PROTAC BRM degrader-1 for BRM and BRG1 are 72 nM and 108 nM, respectively. PROTAC BRM degrader-1 can be used in studies related to selective SMARCA2 degradation, SWI/SNF function, and SMARCA4-mutant non-small cell lung cancer.
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TQ-3959
0 ImagesCat. No.: HY-175541CAS No.: 2926610-43-5
