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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC80670 Fmoc-C-PEG3-C3-Succinamic acid
Fmoc-C-PEG3-C3-Succinamic acid is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC80667 Fluorofelbamate
Fluorofelbamate, a Felbamate analog, is a potent NMDA receptor antagonist. Fluorofelbamate exhibits anticonvulsant and antiepileptogenic effects in an experimental rat model of self-sustaining status epilepticus (SSSE). Fluorofelbamate can be used for epilepsy research.
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DC80645 FCH-2296413
FCH-2296413 is a potent and selective hydroxycarboxylic acid receptor (HCAR) agonist with an EC50 of 4.4-8.6 nM. FCH-2296413 exhibits analgesic activity and can be used for the research of peripheral pain-related diseases.
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DC80641 Farabursen sodium
Farabursen sodium (RGLS8429 sodium; RG1015 sodium) is a miR-17 inhibitor. Farabursen sodium inhibits the function of the miR-17 family, relieves the inhibitory effect on miR-17 target genes including PKD1 and PKD2, and increases the level of PC1/2. Farabursen sodium slows the growth of renal cysts, reduces the ratio of kidney weight to body weight, and decreases the cyst index and proliferation index. Farabursen sodium is applicable to research related to autosomal dominant polycystic kidney disease.
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DC80636 FAK activator-1
FAK activator-1 is a FAK activator and mucosal healing inducer.FAK activator-1 increases FAK phosphorylation at Tyr-397, promoting FAK activation.FAK activator-1 promotes mucosal healing.FAK activator-1 can be used for the research of nsaid-associated gastrointestinal mucosal injury.
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DC80634 FABP4/5-IN-6
FABP4/5-IN-6 is an orally active, potent FABP4/5 inhibitor (Ki = 0.41/2.53 μM), showing low selectivity over FABP3 (Ki = 59.72 μM). FABP4/5-IN-6 inhibits the secretion of MCP-1 and IL-6 in Lipopolysaccharides (LPS)-induced THP-1 macrophage. FABP4/5-IN-6 exhibits significant anti-inflammatory effects and attenuates LPS-induced liver injury. FABP4/5-IN-6 has low hERG inhibition (LD50 > 2000 mg/kg). FABP4/5-IN-6 can be used for the study of Inflammation-related diseases.
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DC80631 EVs inducer-1
EVs inducer-1 is a release inducer of immunostimulatory extracellular vesicles (EVs). EVs inducer-1 inhibits tubulin polymerization. EVs inducer-1 enhances the release of immunostimulatory EVs by antigen-presenting cells, increases the release of EV particles from dendritic cells, and elevates CD63 reporter gene activity. EVs inducer-1 inhibits the viability of proliferating cells. EVs inducer-1 is applicable for research related to immune regulation.
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DC80626 Ethyl 4-(piperazin-1-yl)benzoate
Ethyl 4-(piperazin-1-yl)benzoate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC80622 ERX-208
ERX-208 is an anticancer agent that induces endoplasmic reticulum stress by targeting lysosomal acid lipase A (LIPA), ultimately leading to cancer cell apoptosis. ERX-208 can be used in ovarian cancer research.
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DC80620 ERG-IN-4
ERG-IN-4 (Compound 12) is an orally active, selective ERG inhibitor with an IC50 of 5.2 μM for hERG. ERG-IN-4 activates PXR. ERG-IN-4 exhibits anticancer activity against MTAP-deleted non-small cell lung cancer.
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DC80617 EphB4-IN-1
EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC50 values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.
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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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