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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC80610 EL244
EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.
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DC80608 EGFR-IN-77
EGFR-IN-77 (Compound 4a) is a selective EGFRT790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 functionally inhibits the kinase activities of EGFRT790M/L858R, EGFRL858R and wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer cells. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer.
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DC80606 EGFR-IN-204
EGFR-IN-204 (Example 1) is a HER2 exon 20 mutation inhibitor with selectivity for wild-type EGFR. EGFR-IN-204 exerts antiproliferative effects on cells dependent on HER2 exon 20 YVMA insertion mutation and wild-type HER2, and shows strong selectivity over cells dependent on wild-type EGFR. EGFR-IN-204 is applicable to non-small cell lung cancer research.
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DC80603 EGFR-IN-200
EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, which potently targets human EGFR (IC50=0.03 μM), TNF-α (IC50=3.1 μM), and the IL-6/GP130 complex (IC50=1.6 μM). EGFR-IN-200 binds to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, induces G2/M cell cycle arrest, apoptosis, and antiproliferative activity. EGFR-IN-200 exhibits high gastrointestinal absorbability, low BBB permeability, and complies with the Lipinski's rule. EGFR-IN-200 can be used for the research of lung cancer and breast adenocarcinoma.
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DC80595 EGFR/BRAFV600E-IN-7
EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAFV600E kinase inhibitor with human IC50 values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAFV600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAFV600E, including hydrogen bonding with EGFR Met769 and BRAFV600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer.
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DC80593 EG36
EG36 is a selective E. coli DnaK inhibitor that inhibits DnaK ATPase activity at a concentration of 100 μM. EG36 directly binds to the nucleotide-binding domain (NBD) of E. coli DnaK by disrupting the DnaK-DnaJ interaction. EG36 can be used for research on bacterial infectious diseases.
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DC80588 E5700
E5700 is an orally active squalene synthase inhibitor, antimalarial agent and antifungal agent with an IC50 of 0.49 nM (without PPi) against squalene synthase from T. cruzi epimastigotes. E5700 shows antiparasitic activities against Trypanosoma cruzi. E5700 inhibits the growth and alters the lipid prolife and the ultrastructure of a multiple agent-resistant C. tropicalis strain. E5700 is a potent and selective inhibitor of the growth of Leishmania amazonensis.
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DC80586 E3 Ligase Ligand-linker Conjugate 225
E3 Ligase Ligand-linker Conjugate 225 is an E3 ligase ligand-linker conjugate used for the synthesis of PROTACs; it consists of the PEG-based linker Bis-Tos-PEG3 and the VHL-type E3 ubiquitin ligase ligand VH 101 thiol. E3 Ligase Ligand-linker Conjugate 225 can be further coupled with a target protein ligand—such as MT-4—to synthesize the PROTAC TG2 Degrader-3.
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DC80584 E3 Ligase Ligand-linker Conjugate 215
E3 Ligase Ligand-linker Conjugate 215 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 215 can be used to synthesize STAT3 PROTAC Degrader S3D5.
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DC80580 E 047/1
MW-436 (E 0471) hydrochloride is a benzofuran compound with antiarrhythmic effects. MW-436 hydrochloride can be used for the research of cardiovascular disease.
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DC80572 DU172
DU172 is a ligand for the adenosine A1 receptor (Adenosine A1 Receptor), with an IC50 of 24.9 nM against A1AR and an IC50 of 0.42 μM against A2AAR.
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DC80565 DPP-4-IN-18
DPP-4-IN-18 (Sitagliptin impurity 3) (Compound 4) impurity 3 is a potent, selective and orally active DPP-4 inhibitor with an IC50 of 27 nM. DPP-4-IN-18 can effectively prevent DPP-4 from degrading glucagon-like peptide 1 (GLP-1), thereby increasing the level of active GLP-1. DPP-4-IN-18 can be used for the research of type 2 diabetes.
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DC80560 DOT1L705
DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia. (Pink: DOT1L ligand ; Blue: VHL E3 ligase ligand; Black: linker).
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DC80547 Discodermolide
Discodermolide (NVP-XAA-296) is a potent microtubule-stabilizing agent with a Ki of 0.4 μM. Discodermolide stabilizes microtubules, induces G2 or M phase cell cycle arrest and apoptosis, leading to inhibition of cancer cell proliferation. Discodermolide competitively inhibits the binding of Paclitaxel to tubulin polymers, and inhibits the growth of Paclitaxel-resistant cells. Discodermolide can be used for breast and colon cancer research.
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DC80535 Dichlorobenzamil hydrochloride
Dichlorobenzamil (3',4'-Dichlorobenzamil; L-594881) hydrochloride is a Na+-Ca2+ Exchanger inhibitor. Dichlorobenzamil (hydrochloride) attenuates the Na+-Ca2+ exchanger-mediated inward current induced by activation of type I metabotropic glutamate receptors in second-order baroreceptor neurons of the rat nucleus tractus solitarius.
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DC80525 DFCI-002-06
DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor, inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies. (Pink: Src and Btk ligand ; Blue: Cereblon ligand ; Black: linker).
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DC80518 Desamino lenalidomide-5-F
Desamino lenalidomide-5-F is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-5-F can be linked to a target protein ligand via a linker to form a PROTAC.
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DC80517 Dehatrine
Dehatrine is a dibenzylisoquinoline alkaloid with antiplasmodial activity. Dehatrine can be found in the Indonesian medicinal plant Beilschmiedia madang. Dehatrine is applicable to malaria-related research.
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DC80516 Decyl phosphate
Decyl phosphate is a selective LPA2 agonist (EC50: 1.8 μM) and LPA1/LPA3 antagonist. Decyl phosphate can be used in the research of blood disorders.
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DC80513 D-DT/MIF-1-IN-1
D-DT/MIF-1-IN-1 (Compound 4h) is a non-competitive, non-covalent inhibitor of MIF-1 and D-DT, with IC50 values of 2.4 μM and 4.0 μM against D-DT, and an IC50 value of 9.8 μM against MIF-1. D-DT/MIF-1-IN-1 inhibits D-DT-induced phosphorylation of ERK and exerts antiproliferative activity in non-small cell lung cancer cells.
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DC80509 ddATP
ddATP (2',3'-Dideoxyadenosine 5'-triphosphate), an active metabolite of 2',3'-dideoxyinosine, is a chain-elongating inhibitor of DNA polymerase. ddATP can be used for Sanger method for DNA sequencing and research of virus infection.
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DC80506 Danitracen
Danitracen (NSC 170955) is an orally active, CNS penetrant serotonin antagonist with antidepressant activity. Danitracen reduces serotonin levels in the cerebrum, cerebellum, medulla and the whole brain. Danitracen exhibits anticataleptic effects in rat catalepsy models. Danitracen can be used for catalepsy and depression research.
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DC80504 D-Alanine-13C3
D-Alanine-13C3 ((R)-Alanine-13C3) is the 13C-labeled D-Alanine. D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.
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DC80502 CYP51-IN-32
CYP51-IN-32 is an antifungal agent with an IC50 of 0.331 μM against CYP51 of Candida albicans. CYP51-IN-32 releases hydrogen sulfide (H2S) and inhibits hyphal formation and biofilm development of Candida albicans. CYP51-IN-32 can be formulated into PEG-based nanovesicles. CYP51-IN-32 is applicable to the research of Candida albicans infection.
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DC80496 CX-5279
CX-5279 is an efficient and selective CK2 inhibitor with IC50 values for nCK2 and CK2α of 2.73 and 0.91 nM, respectively. CX-5279 is sensitive to mutations at Val66, Ile174, and V66I174AA, with IC50 values of 13.8, 12.5, and 23.35 nM, respectively. CX-5279's inhibitory activity against PIM1 is very weak, with a IC50 value of 8.52 μM. CX-5279 exhibits anti-proliferative activity in various cancer cell lines. CX-5279 can be used for research on cancers such as pancreatic cancer and leukemia.
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DC80481 CppA-IN-1
CppA-IN-1 is a CppA inhibitor specific to Chlamydia trachomatis, which inhibits the growth of Chlamydia trachomatis. CppA-IN-1 shows no activity against recombinant CppA in vitro. CppA-IN-1 can be used in studies related to Chlamydia trachomatis infection.
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DC80470 COX-1-IN-5
COX-1-IN-5 (example 13, compound PS13) is a potent and selective COX-1 inhibitor (COX-1 IC50 = 1 nM, COX-2 IC50 > 0.1 μM) exhibiting >1000-fold selectivity over COX-2. COX-1-IN-5 possesses strong anti-inflammatory, antipyretic, analgesic, antithrombotic, anti-cancer activities. COX-1-IN-5 can be used for COX-mediated diseases research, such as inflammatory conditions and pain. COX-1-IN-5 radiolabeled with 11C can be used as a selective PET tracer for whole‑body imaging of COX‑1 distribution and target engagement in vivo.
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DC80469 Cot-IN-4
Cot-IN-4 (compound 32) is a potent cancer osaka thyroid (COT) kinase inhibitor with an IC50 of 6 nM. Cot-IN-4 inhibits the phosphorylation of ERK (IC50: 60 nM) and inhibits TNFα release (IC50: 60 nM). Cot-IN-4 also inhibits the formation of the pro-inflammatory cytokine IL-1β (IC50: 0.2 μM) in Uric acid-stimulated macrophages. Cot-IN-4 can be used for the study of inflammatory diseases.
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DC80465 CN-716 dihydrochloride
CN-716 dihydrochloride is a reversible covalent flavivirus NS2B·NS3 protease inhibitor with antiviral activity. CN-716 dihydrochloride effectively inhibits the replication of dengue virus (DENV2), West Nile virus (WNV) and Zika virus (ZIKV). The IC50 values of CN-716 dihydrochloride against the proteases of the above three viruses are 0.066 μM, 0.11 μM and 0.25 μM, respectively, while the Ki values against the same proteases are 0.051 μM, 0.082 μM and 0.04 μM, respectively. CN-716 dihydrochloride can be used to study the infection mechanisms of dengue fever, West Nile fever and Zika virus infection.
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DC80462 CM304 free base
CM304 free base (FTC-146) is a potent S1R antagonist. CM304 free base enhances the antinociceptive effects of the cannabinoid receptor agonists. CM304 free base inhibits convulsions in rats.
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