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 (1352)
Related Products (1352)
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Antibodies (1)
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PROTACs Isoform Comparison
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MS108
0 ImagesCat. No.: HY-183555MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC50 of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog AF9, which shares a highly conserved YEATS domain with ENL. MS108 suppresses proliferation of cancer cells.
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PROTAC AR Degrader-7
0 ImagesCat. No.: HY-160221CAS No.: 2505495-83-8PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC50 value of 3 nM.
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(S)-dHTC1
0 ImagesCat. No.: HY-173631CAS No.: 3081383-46-9(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC50 value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC50 value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study.
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PROTAC BRD4 Degrader-23
0 ImagesCat. No.: HY-161093PROTAC BRD4 Degrader-23 is a visible light-regulated BRD4 PROTAC degrader, with DC50 values of 6871 nM and < 30 nM in the dark and under light exposure, respectively; its IC50 values are 1172 nM and 140 nM under the corresponding conditions. PROTAC BRD4 Degrader-23 shows inhibited activity in dark environments, and recovers BRD4 degradation ability upon irradiation with 405 nm visible light. PROTAC BRD4 Degrader-23 inhibits tumor cell proliferation in a visible light-dependent manner. PROTAC BRD4 Degrader-23 can be used in studies of BRD4-dependent B-cell lymphoma.
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PROTAC EGFR degrader 10
0 ImagesCat. No.: HY-161632CAS No.: 3034244-56-6PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM.
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PROTAC SARS-CoV-2 RdRp Degrader-1
0 ImagesCat. No.: HY-179283PROTAC SARS-CoV-2 RdRp Degrader-1 (PROTAC 10) is a SARS-CoV-2 RdRp PROTAC degrader, with a DC50 of 1.97 μM (in infected cells). PROTAC SARS-CoV-2 RdRp Degrader-1 promotes the ubiquitination and degradation of SARS-CoV-2 RdRp. PROTAC SARS-CoV-2 RdRp Degrader-1 can be used in the research of SARS-CoV-2 infection.
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BCPyr
0 ImagesCat. No.: HY-142621CAS No.: 2669844-82-8BCPyr is a PROTAC degrader targeting cIAP1 and BTK, with a Kd of 262 nM for human cIAP1, and Kd values of 262 nM and 692 nM for human BTK. BCPyr binds to the Bir3 domain of cIAP1, recruits BTK to cIAP1, and mediates the ubiquitination and degradation of BTK. BCPyr acts as a degrader, ternary complex stabilizer, cooperative binder, and higher-order assembly inducer. BCPyr can be used in studies related to leukemia and lymphoma.
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SA-VA
0 ImagesCat. No.: HY-155685CAS No.: 3058085-77-8SA-VA is an intracellular self-assembled PROTAC based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase.
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UNC8209
0 ImagesCat. No.: HY-183098UNC8209 is a selective PROTAC-based TANK-binding kinase 1 (TBK1) degrader. UNC8209 recruits cereblon (CRBN) to mediate ubiquitin-proteasome pathway-dependent TBK1 degradation and reduces AAK1, GAK, and AURKA abundance. UNC8209 suppresses tumor cell proliferation, impairs in vivo tumor growth, inhibits colony and clonogenic growth and enhances tumor cell sensitivity to TNFα or IFN-γ. UNC8209 modulates cell cycle and induces mild apoptosis. UNC8209 can be used for the research of clear cell renal cell carcinoma, non-small cell lung cancer, pancreatic ductal adenocarcinoma.
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PROTAC BRD4 Degrader-27
0 ImagesCat. No.: HY-162875CAS No.: 2407163-44-2PROTAC BRD4 Degrader-27 is a selective cereblon-mediated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-27 exhibits anticancer activity, induces G1 phase arrest, and inhibits DNA synthesis and colony formation. PROTAC BRD4 Degrader-27 suppresses HCC1806 tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-27 can be used in breast cancer-related research.
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GMB-805
0 ImagesCat. No.: HY-180968CAS No.: 2489876-41-5
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PROTAC SOS1 degrader-6
0 ImagesCat. No.: HY-162281CAS No.: 3032282-51-9PROTAC SOS1 degrader-6 is a selective SOS1 PROTAC degrader with a DC50 of 43-130 nM. PROTAC SOS1 degrader-6 induces ubiquitination and degradation of SOS1 via the ubiquitin-proteasome system by recruiting the E3 ligase VHL. PROTAC SOS1 degrader-6 reduces the levels of phosphorylated MEK and ERK. PROTAC SOS1 degrader-6 exerts antiproliferative effects in KRAS-driven cancer cells. PROTAC SOS1 degrader-6 can be used in research related to KRASG12C-mutant cancers and chronic myeloid leukemia.
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PROTAC Hemagglutinin Degrader-1
0 ImagesCat. No.: HY-147654CAS No.: 3031330-66-9PROTAC Hemagglutinin Degrader-1 (Compound V3) is a potent PROTAC influenza hemagglutinin (HA) degrader with a median degradation concentration of 1.44 μM. PROTAC Hemagglutinin Degrader-1 shows broad-spectrum anti-influenza virus activity.
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PROTAC ALK degrader-2
0 ImagesCat. No.: HY-161750PROTAC ALK degrader-2 (B1-PEG) is an ALK degrader based on PROTACs, with the DC50 of 45 nM in H3122 EML4-ALK DC50 (GSH+). PROTAC ALK degrader-2, through PEGylation, is engineered to self-organize into micelles in water and releases its active form in response to the tumor-specific high GSH environment.
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TD-802
0 ImagesCat. No.: HY-146397CAS No.: 2760703-21-5TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models.
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LGF308
0 ImagesCat. No.: HY-181756CAS No.: 3061406-69-4LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer.
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PROTAC SMARCA2/4 degrader-35
0 ImagesCat. No.: HY-168225CAS No.: 2933253-85-9PROTAC SMARCA2/4-degrader-35 (Ex.43) is a SMARCA2/4 degrader with a DC50 <2.5 nM
