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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC81417 PU-11
PU-11 is a Hsp90α/Hsp90β inhibitor with IC50 values of 18.6 μM and 89.8 μM and Kd values of 2 and 4.2 μM. PU-11 binds to the ATP-binding pocket of Hsp90α and Hsp90β and displays selective binding preference for Hsp90α over Hsp90β, mediated by the nonconserved Hsp90α Ser52 residue. PU-11 can be used for the research of neurodegenerative disorders.
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DC81416 PTPN2-IN-3
PTPN2-IN-3 (example 52) is a PTPN2 inhibitor that can be used in tumor research.
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DC81415 PTPN2-IN-2
PTPN2-IN-2 is a potent and orally active PTPN2 inhibitor (IC50 = 7.05 nM) that enhances the IFN-γ signaling pathway. PTPN2-IN-2 inhibits PTP1B with an IC50 of 9.88 nM. PTPN2-IN-2 inhibits tumor growth, promotes the activation and infiltration of tumor immune cells in a B16-OVA mouse model. PTPN2-IN-2 can be used for the research of melanoma.
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DC81414 PTP1B-IN-33
PTP1B-IN-33 is a PTP1B inhibitor with a human IC50 of 2.45 μM and over 20-fold selectivity for PTP1B over SHP2. PTP1B-IN-33 enhances π-Alkyl interaction with PTP1B to increase WPD loop closure degree. PTP1B-IN-33 can be used for the research of cancer, diabetes, autoimmune deficiency diseases.
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DC81413 p-Toluenesulfonamide-15N
p-Toluenesulfonamide-15N is the 15N-labeled p-Toluenesulfonamide. p-Toluenesulfonamide is an intermediate and plasticizer. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum.
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DC81412 PTH1R agonist 4
PTH1R agonist 4 (Example 63) is a parathyroid hormone 1 receptor (PTH1R) agonist with a pEC50 value greater than 7. PTH1R agonist 4 can be used for the study of bone diseases, such as osteoporosis.
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DC81411 PTH1R agonist 1
PTH1R agonist 1 (Example 2) is a parathyroid hormone 1 receptor (PTH1R) agonist. PTH1R agonist 1 can be used for research of hypoparathyroidism and osteoporosis.
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DC81410 PTERi
PTERi is a selective inhibitor of PTER with selectivity towards HDACs. PTERi increases the level of N-acetyltaurine in both lean and obese mice, and reduces food intake in obese mice. PTERi can be used in the research of obesity.
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DC81409 PSMA ligand 3
PSMA ligand 3 is a PSMA-targeting ligand of Psa-AR. Psa-AR can be used for cancer research.
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DC81408 P-SCN-Bn-NOTA
P-SCN-Bn-NOTA is a metal chelator and molecular imaging probe precursor that allows radiolabeling with Ga-68. P-SCN-Bn-NOTA can be conjugated to CD70-specific molecules B3, B6, ABDB3 and ABDB6 to form NOTA-labeled derivatives. P-SCN-Bn-NOTA is applicable for preclinical PET/CT imaging of CD70-expressing tumors in NCG mouse PDX models. P-SCN-Bn-NOTA can be used in studies related to CD70-positive tumors.
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DC81407 PS1097
PS1097 is a broad-spectrum antiviral inhibitor with a BVDV RdRp IC50 of 0.64 μM. PS1097 selectively reduces RTN3 protein levels, causes partial RTN3 mRNA reduction, and leaves other endoplasmic reticulum-resident proteins unaffected. PS1097 inhibits replication of Zika virus and multiple viruses that use the endoplasmic reticulum as a replication hub. PS1097 inhibits BVDV RdRp enzymatic activity and exerts activity against Bovine Viral Diarrhea Virus. PS1097 can be used for the research of zika virus infection, usutu virus infection, west nile virus infection, COVID-19, coxsackie b virus 5 infection, chikungunya virus infection, vaccinia virus infection.
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DC81406 PRT-060318 dihydrochloride
PRT-060318 (PRT318) dihydrochloride is a potent, selective and orally active tyrosine kinase Syk inhibitor with an IC50 of 3 nM. PRT-060318 dihydrochloride suppresses chronic lymphocytic leukemia (CLL) B cell activation and migration, and induces apoptosis. PRT-060318 dihydrochloride prevents Heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model. PRT-060318 dihydrochloride can be used for CLL and thrombus research.
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DC81405 ProX1-(SS)-DOTAGA_R
ProX1-(SS)-DOTAGA_R (Compound 25a) is the unbound radionuclide portion of the radiopharmaceutical and can be used for targeted delivery to diseases characterized by ACP3 expression.
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DC81404 ProX1-(SS)-DOTAGA
ProX1-(SS)-DOTAGA (Compound 12b) is the unbound portion of the radionuclide in the compound and can be used for targeted delivery to diseases characterized by ACP3 expression.
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DC81403 Proteasome-IN-8
Proteasome-IN-1 (Compound 130) is a proteasome inhibitor. Proteasome-IN-1 exhibits antiparasitic activity against P. faciparum 3D7.
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DC81402 PROTAC USP7 Degrader-2
PROTAC USP7 Degrader-2 (Compound D16) is an efficient and selective USP7 PROTAC degrader with a DC50 of 1.91 μM (in TE-12 cells). PROTAC USP7 Degrader-2 inhibits the migration of upper gastrointestinal tract (UGI) cancer cells and shows relatively weak anti-proliferative activity. PROTAC USP7 Degrader-2 can be used in the research of metastatic upper gastrointestinal cancer. (Pink: USP7 ligand ; Blue: Cereblon ligand ; Black: linker).
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DC81401 PROTAC TG2 Degrader-3
PROTAC TG2 Degrader-3 is a TG2 PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer. (Pink: Transglutaminase ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).
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DC81400 PROTAC TEAD degrader-2
PROTAC TEAD degrader-2 (Compound 31) is an efficient TEAD1 PROTAC degrader with a DC50 of 0.6 nM. PROTAC TEAD degrader-2 inhibits the YAP/TAZ-TEAD interaction, with a IC50 of 1.8 nM. PROTAC TEAD degrader-2 exhibits significant selective inhibitory activity against YAP-dependent cancer cells and effectively suppresses the transcriptional activity mediated by YAP. PROTAC TEAD degrader-2 can be used for research on mesothelioma and glioma. (Pink: TEAD1 ligand ; Blue: Cereblon ligand ; Black: linker ).
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DC81399 PROTAC STAT6 degrader-4
PROTAC STAT6 degrader-4 (Compound 3u247) is a STAT6 PROTAC degrader with a DC50 of 0.04 nM. PROTAC STAT6 degrader-4 promotes the ubiquitination and degradation of STAT6, and is applicable to the research of immune diseases.
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DC81398 PROTAC STAT6 degrader-3
PROTAC STAT6 degrader-3 is a potent STAT6 PROTAC degrader with a DC50 of less than 1 nM. PROTAC STAT6 degrader-3 can be used for research on allergic/inflammatory diseases and cancer.
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DC81397 PROTAC STAT6 degrader-2
PROTAC STAT6 degrader-2 is a highly efficient PROTAC degrader targeting STAT6. PROTAC STAT6 degrader-2 has a DC50 value of 1-10 nM for STAT6 in human PBMC cells and a DC50 value of less than 100 nM for STAT6 in HEK293-HIBiT-STAT6 cells. PROTAC STAT6 degrader-2 can be used for STAT6-mediated diseases.
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DC81396 PROTAC SMARCA2 degrader-36
PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers. (Pink: Epigenetic Reader Domain Target protein ligand; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker).
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DC81395 PROTAC SKP2 Degrader-1
PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research. (Pink: COX and NF-κB ligand ; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker ).
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DC81394 PROTAC SARS-CoV-2 Mpro degrader-8
PROTAC SARS-CoV-2 Mpro degrader-8 is an antiviral PROTAC degrader targeting the SARS-CoV-2 main protease (Mpro), with weak direct binding affinity to Mpro (Kd=80.5 μM). PROTAC SARS-CoV-2 Mpro degrader-8 exhibits broad-spectrum antiviral activity against SARS-CoV-2 and the human endemic coronavirus HCoV-OC43. It can be used for research on coronavirus infections. (Pink: SARS-CoV Target protein ligand; Blue: VHL ligand ; Black: ).
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DC81393 PROTAC SAMHD1 Degrader-1
PROTAC SAMHD1 Degrader-1 is an orally active targeted SAMHD1 PROTAC degrader, with an IC50 of 6.3 μM against the dNTP hydrolase activity of SAMHD1. PROTAC SAMHD1 Degrader-1 binds to SAMHD1 inside cells and mediates its degradation, with low off-target effects. PROTAC SAMHD1 Degrader-1 inhibits the production of pro-inflammatory cytokines and interferes with the cascade amplification process of inflammatory responses. PROTAC SAMHD1 Degrader-1 delays the progression of pulmonary fibrosis and exerts protective effects on lung tissues. PROTAC SAMHD1 Degrader-1 can be used in pulmonary fibrosis-related research. (Pink: Ligands for Target Protein for PROTAC and HIV ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker ).
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DC81392 PROTAC RET Degrader 1
PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand; Blue: CRBN ligand; Black: Linker).
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DC81391 PROTAC PLK1 Degrader-3
PROTAC PLK1 Degrader-3 (Compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway, with a Kd value of 2.2 μM. The cell penetration ability of PROTAC PLK1 Degrader-3 is limited and a higher concentration is required to achieve significant degradation effects. PROTAC PLK1 Degrader-3 can be used for research on non-small cell lung cancer. (Pink: PLK1 ligand ; Blue: Ligands for E3 Ligase ligand ; Black: linker).
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DC81390 PROTAC NTRK1 degrader-1
NTRK degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). NTRK degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1.NTRK degrader-1 can be used for the research of solid tumors. (Pink: NTRK1 Target protein ligand; Blue: Cereblon E3 ligase ligand; Black: linker).
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DC81389 PROTAC NAMPT Degrader-28
PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research. (Pink: NAMPT ligand ; Blue: VHL ligand ; Black: linker ).
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DC81388 PROTAC MLLT1 Degrader-1
PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML).
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