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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC80710 Glucagon receptor antagonist-10
Glucagon receptor antagonist-10 (Compound 11) is a glucagon receptor antagonist with a pIC50 of 7.154. Glucagon receptor antagonist-10 can be used in studies of glucose homeostasis.
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DC80701 Gentamicin B
Gentamicin B (SCH-14342) is an aminoglycoside antibiotic that can be isolated from Micromonospora echinospora. Gentamicin B can be used for the research of ataxia potential and renal toxicity.
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DC80699 Gd-PCTA-Ach
Gd-PCTA-Ach is a macrocyclic gadolinium-based MRI contrast agent with high kinetic inertness and moderate albumin affinity. The albumin-binding property of Gd-PCTA-Ach effectively prolongs its blood circulation time. Gd-PCTA-Ach is mainly cleared via the kidneys, while approximately 10% of the dose is excreted through the hepatobiliary pathway, exhibiting a unique dual-channel excretion profile. Gd-PCTA-Ach enables high-quality imaging of brain and liver tumor lesions, and has important application value in diagnostic studies of liver cancer and glioma.
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DC80696 GAT100
GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases.
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DC80691 Gallamine
Gallamine is an allosteric, selective muscarinic M2 acetylcholine receptor antagonist (EC50: 130 nM for [3H]NMS dissociation from porcine muscarinic M2 receptors). Gallamine is also an acetylcholinesterase inhibitor (IC50s : 1070 μM, 1480 μM, 235  μM for EeAChE, hAChE, hBChE, respectively (in the absence of MeCN)). Gallamine increases free norepinephrine levels. Gallamine can be used as a muscle relaxant.
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DC80686 FXR DUBTAC IN-1
FXR DUBTAC IN-1 (compound D11) is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC IN-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC IN-1 can be used in the research of cholestatic liver injury.
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DC80678 Frenlosirsen sodium
Frenlosirsen sodium is an antisense oligonucleotide targeted to IRF4. It is used for study of relapsed/refractory multiple myeloma (RRMM).
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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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