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PROTAC

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Cat. No. Product Name Field of Application Chemical Structure
DC70723 QC-01–175 Featured
QC-01-175 is a hetero-bifunctional molecule designed to engage both tau and Cereblon (CRBN) to trigger tau ubiquitination and proteasomal degradation (tau PROTAC).QC-01–175 effected clearance of tau in frontotemporal dementia (FTD) patient-derived neuronal cell models, with minimal effect on tau from neurons of healthy controls.QC-01–175 also rescued stress vulnerability in FTD neurons, phenocopying CRISPR-mediated MAPT-knockout.
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DC21351 MS4078 Featured
MS4078 is a novel PROTAC (degrader) of ALK, potently decreases cellular levels of oncogenic active ALK fusion proteins in a concentration- and time-dependent manner in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells (DC50=11 nM).
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DC21360 MZ1 Featured
MZ1 is a PROTAC that tethers JQ1 to a ligand for the E3 ubiquitin ligase VHL, triggers, induces degradation of the BET bromodomain BRD4.
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DC74495 HDAC3 PROTAC P7 Featured
HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).
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DC28539 SIAIS178 Featured
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
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DC28688 UNC6852 Featured
UNC6852 is a selective rolycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a VHL ligand, with an IC50 of 247 nM for EED.
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DC50038 PROTAC SGK3 degrader-1 Featured
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
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DC28556 XY028-133 Featured
XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, extracted from patent WO2018106870A1.
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DC79828 Aurora kinase ligand-1
Aurora kinase ligand-1 (Compound I-4) is an Aurora kinase B (AURKB) PROTAC ligand. Aurora kinase ligand-1 can be conjugated with E3 ligase Ligand and linker to synthesize AURKB PROTAC degrader MS44. MS44 can be used for cancer research.
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DC79824 IRAK4 ligand-14
IRAK4 ligand-14 is a ligand for IRAK4. IRAK4 ligand-14 can be used for synthesizing PROTACs such as APH02174.
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DC79777 SMARCA2/4-ligand-6
SMARCA2/4-ligand-6 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). SMARCA2/4-ligand-6 can be used for the synthesis of SMARCA2/4-ligand-6.
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DC79734 PDE4 ligand 2
PDE4 ligand 2 is a CRBN E3 ligase ligand. PDE4 ligand 2 can be used to synthesize PROTAC such as PDE4 degrader-1. PDE4 ligand 2 can be studied in research for autoimmune and anti-inflammatory diseases.
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DC79565 KRASG12C ligand-1
KRASG12C ligand-1 is a PROTAC target protein ligand that can be used to synthesize the PROTAC YN14-H. YN14-H is a PROTAC degrader targeting KRASG12C and has antitumor activity.
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DC79483 Oxide-DFHBI-demethyl
Oxide-DFHBI-demethyl is a target aptamer ligand (Ligand for Target Protein for PROTAC). Oxide-DFHBI-demethyl can be used for synthesis of RNA aptamer-based PROTAC Dth.
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DC79445 DOT1L ligand-1
DOT1L ligand-1 is a DOT1L ligand. DOT1L ligand-1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as MS2133.
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DC79428 PROTAC BRD4 ligand-4
PROTAC BRD4 ligand-4 is a BRD4 ligand, which can be used to synthesize PROTAC BRD4 Degrader-37.
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DC79425 FAK ligand-5
FAK ligand-5 (BI-4464) is a FAK inhibitor, with an IC50 of 25 nM. FAK ligand-5 can serve as a ligand for target protein for PROTAC, used in the development and design of degraders for PROTAC FAK. FAK ligand-5 can be used in the synthesis of PROTAC FAK degrader 4. FAK ligand-5 can be used in cancer research.
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DC79403 BCL-xL ligand 2
BCL-xL ligand 2 is a ligand for BCL-xL. BCL-xL ligand 2 can be conjugated with E3 ligase Ligand and linker to synthesize Bcl-xL PROTAC degrader PZ671.
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DC79397 HDAC6 ligand-5
HDAC6 ligand-5 is a binding ligand of HDAC6 and can be used to synthesize PROTACs such as PROTAC HDAC6 degrader 5.
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DC79369 sEH-H ligand 2
sEH-H ligand 2 is an sEH inhibitor and a ligand for the target protein for PROTAC (sEH). sEH-H ligand 2 can be used to synthesize PROTAC sEH-degrader-4.
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DC79354 sEH-H ligand 1
sEH-H ligand 1 is a PROTAC target protein ligand that can be used to synthesize PROTAC sEH degrader-2.
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DC79339 MNK1 ligand 1
MNK1 ligand 1 (Compound 5) is a MNK1 ligand. MNK1 ligand 1 can be used for synthesis of PROTAC MNK1 degrader-1.
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DC79336 ASK1 ligand 1
ASK1 ligand 1 is a binding ligand for ASK1 and can be used to synthesize PROTACs such as dASK1-VHL.
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DC79305 PRMT5 ligand 2
PRMT5 ligand 2 (Compound 38) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PRMT5 ligand 2 can be used for synthesis MS115.
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DC79273 NASA-linker-VH032-PEG3 ligand
NASA-linker-VH032-PEG3 ligand is a ligand that can be used to synthesize PROTACs.
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DC79228 HPK1 ligand 4
HPK1 ligand 4 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-5. PROTAC HPK1 Degrader-5 is a potent and orally active HPK1 PROTAC degrader with anti-tumor activity.
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DC79143 TBK1 ligand 2
TBK1 ligand 2 (Compound 1b) is a TBK1 inhibitor. TBK1 ligand 2 can be used for synthesis of PROTAC TBK1 degrader-2.
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DC79133 Rimonabant carboxylic acid
Rimonabant carboxylic acid is a Ligand for Target Protein for PROTAC. Rimonabant carboxylic acid can be used to synthesize PROTAC CB1R Degrader-1.
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DC79114 STAT6 ligand-1
STAT6 ligand-1 is a ligand for STAT6. STAT6 ligand-1 can be used for synthesizing PROTACs such as STAT6 degrader-2.
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DC79033 BRAF ligand-1
BRAF ligand-1 is the ligand of BRAF. BRAF ligand-1 can be used to synthesize CST905.
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