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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC71973 TSPO ligand-1
TSPO ligand-1 is the ligand of AUTAC4 that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.
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DC71972 PROTAC BRD9-binding moiety 5
PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells.
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DC71952 Pomalidomide-C12-NH2 hydrochloride
Pomalidomide-C12-NH2 hydrochloride is the E3 ligase ligand-linker conjugate of PROTAC KRAS G12C degrader-1. PROTAC KRAS G12C degrader-1 is a Cereblon-based KRASG12C degrader.
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DC71927 XF067-68
XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5) (extracted from patent WO2019246570A1).
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DC71926 MS9449
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer.
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DC71925 MS159
MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease.
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DC71924 DA-PROTAC
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research.
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DC71678 (S,R,S)-AHPC-O-PEG1-propargyl
(S,R,S)-AHPC-O-PEG1-propargyl (Compound 10b) is an E3 ligand for the synthesis of PROTAC.
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DC71636 MS9427
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer.
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DC71635 HD-TAC7
HD-TAC7 is a PROTAC HDAC3 degrader with a DC50 value of 0.32 μM. HD-TAC7 inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 3.6, 4.2, and 1.1 μM, respectively. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
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DC71634 SIAIS164018
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, which is designed from Brigatinib, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib.
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DC71633 dTAG-47-NEG
dTAG-47-NEG is an analog of dTAG-47 that cannot bind and recruit cereblon (CRBN). dTAG-47-NEG can be used as a heterobifunctional negative control of dTAG-47.
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DC71632 PP-C8
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
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DC71631 dTAG-47
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12F36V). FKBP12F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC).
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DC71630 (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine has a multi-path anti-fibrosis function and a renal protection function for research of renal anemia.
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DC71629 SS47
SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell treatment. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies.
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DC46369 GSK215 Featured
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
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DC71244 YF135
YF135 is an efficient and reversible-covalent KRASG12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRASG12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
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DC71237 SIAIS117
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer.
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DC71233 Azido-PEG2-VHL
Azido-PEG2-VHL is a multikinase degrader which can be used in the synthesis of PROTACs.
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DC71175 PROTAC TTK degrader-2
PROTAC TTK degrader-2 is a potent TTK (threonine tyrosine kinase) PROTAC degrader, with DC50 values of 3.1 and 12.4 nM in COLO-205 and HCT-116 cell, respectively. PROTAC TTK degrader-2 exhibits target degradation and anticancer efficacy in a xenograft mouse model of COLO-205 human colorectal cancer cells.
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DC71174 PROTAC SOS1 degrader-1
PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 agonist with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
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DC71142 Dimethyl-F-OICR-9429-COOH
Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs.
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DC71088 MS5033
MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC50 of 430 nM in PC3 cells.
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DC50270 TCO-PEG2-Sulfo-NHS ester sodium
TCO-PEG2-Sulfo-NHS ester sodium is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC50269 DBCO-PEG6-amine TFA
DBCO-PEG6-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC50247 Cereblon inhibitor 1
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research.
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DC50219 NJH-2-030
NJH-2-030 can be used as a covalent recruiter for FEM1B in targeted protein degradation applications.
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DC50142 DB-0646
DB-0646, a PROTAC, is a multi-kinase degrader.
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DC50141 SB1-G-187
SB1-G-187, a PROTAC, is a multi-kinase degrader.
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