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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC80500 Cyclohexane-1,2,3,4,5,6-hexaone octahydrate
Cyclohexane-1,2,3,4,5,6-hexaone octahydrate(Triquinoyl octahydrate) is a metal-organic framework (MOF).
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DC80499 Cyclobenzaprine
Cyclobenzaprine (MK130) is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Cyclobenzaprine also possesses antiparasitic activity. Cyclobenzaprine holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases.
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DC80498 CXL 017
CXL 017 is a sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) inhibitor. CXL 017 can inhibit the ATPase activity of SERCA by competing with ATP for binding. CXL 017 exhibits selective cytotoxicity against multidrug-resistant acute myeloid leukemia cells HL60/MX2. CXL 017 can be used in the research of tumors such as multidrug-resistant acute myeloid leukemia.
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DC80497 CXCR6 antagonist 1
CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma.
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DC80495 Cx43 HC-IN-1
Cx43 HC-IN-1 (Compound D4) is a selective and orally active inhibitor of connexin hemichannels (Cx43 HC). Cx43 HC-IN-1 effectively inhibits the hemichannel activity mediated by Cx43/Cx45 in denervated skeletal muscle fibers, significantly increasing the reinnervation rate of muscle fibers by neurons. Cx43 HC-IN-1 reduces neuroinflammation and neuronal overexcitation by inhibiting hemichannels in glial cells in the brain, and alleviates epilepsy in mice. Cx43 HC-IN-1 can be used for research on epilepsy and muscle diseases.
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DC80494 CV-6504
CV-6504 is a dual inhibitor of TXA2 synthase and 5-lipoxygenase. CV-6504 can scavenge ROS and exhibit antitumor activity. CV-6504 can be used for the researches of cancer, inflammation and cardiovascular disease.
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DC80493 CuET
CuET, a metabolite of Disulfiram, is a cuproptosis and ferroptosis inducer with anti-tumor activity. CuET interacts directly with polyunsaturated phospholipids to generate free radicals, leading to lipid peroxidation. CuET induces cuproptosis via excessive copper accumulation, leading to lipoylated protein aggregation and iron-sulfur cluster protein loss. CuET induces ferroptosis via a copper-triggered, radical-dependent pathway with limited dependence on iron accumulation, and alters lipid composition to sensitize cells to peroxidative damage. CuET increases intracellular ROS and MDA levels in cancer cells. CuET exhibits anti-tumor activity against non-small cell lung cancer in vitro and in vivo. CuET can be used for the research of cancer, such as non-small cell lung cancer.
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DC80492 CTR/AMYR modulator-2
CTR/AMYR modulator-2 (Example 107) is a receptor 3 for pancreatic amyloid peptide (bAMY3R) agonist, and its EC50 for stimulating cAMP production in cells is <500 nM. CTR/AMYR modulator-2 is also a receptor for calcitonin (bCTR) agonist, with its EC50 being <5000 nM. CTR/AMYR modulator-2 can be used for research on type 2 diabetes and obesity.
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DC80491 CTR/AMYR modulator-1
CTR/AMYR modulator-1 is a calcitonin receptor/amylin receptor modulator. CTR/AMYR modulator-1 can be used for the research of metabolic disease.
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DC80490 CTR/AMYR agonist-1 enantiomer
CTR/AMYR agonist-1 enantiomer is a CTR/AMYR agonist with EC50 values of 0.56-6.9 nM. CTR/AMYR agonist-1 enantiomer can be used for the research of metabolic disease.
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DC80489 CTR/AMYR agonist-1
CTR/AMYR agonist-1 is a CTR/AMYR agonist with EC50 values of 0.56-6.9 nM. CTR/AMYR agonist-1 can be used for the research of metabolic disease.
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DC80488 CSP-2503
CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.
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DC80487 CSN5-IN-3
CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.
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DC80486 Cryptophycin 52
Cryptophycin 52 (LY355703) is a synthesized 16-membered cyclic ester peptide compound and is a derivative of marine natural product cryptophycin 1 with antitumor activity. Cryptophycin 52 can induce cells G2/M phase arrest. Cryptophycin 52 is also effective for solid tumors that are resistant to Paclitaxel and Doxorubicin. Cryptophycin 52 can be used for the research of cancer, such as multidrug-resistant tumor.
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DC80485 CRBN ligand-895
CRBN ligand-895 (Compound 14) is an E3 ubiquitin ligase ligand for cereblon (CRBN), which is used to recruit the cereblon protein. CRBN ligand-895 can be used for the synthesis of PROTACs, such as PROTAC HDAC8 Degrader-4.
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DC80484 CRBN ligand-222
CRBN ligand-222 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-222 can be linked to a target protein ligand via a linker to form a PROTAC.
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DC80483 CQ80
CQ80 is a PEPD/XPNPEP1 inhibitor and selective CARD8 inflammasome activator. CQ80 has IC50 values of 0.91 μM for PEPD, 43 μM for XPNPEP1. CQ80 promotes the accumulation of Xaa-Pro peptides by inhibiting PEPD and XPNPEP1, releases the fragment of CARD8 for inflammasome formation, and induces pyroptosis via GSDMD cleavage. CQ80 can be used for research on inflammasome, CARD8-expressing cancer cells, HIV-1-infected cell clearance, acute myeloid leukemia (AML).
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DC80482 CPU-228
CPU-228 is a complex class III antiarrhythmic agent. CPU-228 concentration-dependently blocks the activities of the rapid component 50 of the delayed rectifier potassium channel (IKr) and the L-type calcium channel (ICa,L), with an IC50 value of 0.909 μM for ICa,L current. CPU-228 produces negative inotropic effects and induces mild, non-frequency-dependent prolongation of the effective refractory period (ERP) in isolated left atria. CPU-228 reduces the incidence of torsades de pointes (TDP) in anesthetized rabbits and inhibits ischemia/reperfusion-induced arrhythmias in rats. CPU-228 can be used in studies related to torsades de pointes.
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DC80480 CP8754
CP8754 is an orally active, selective human progesterone receptor (hPR) antagonist that blocks progesterone-mediated signaling pathways. CP8754 competitively inhibits the binding of [3H]-progesterone to hPR. And in vitro, CP8754 inhibits progesterone-dependent exogenous luciferase and endogenous alkaline phosphatase expression; while in vivo, CP8754 inhibits rabbit endometrial transformation. CP8754 does not significantly bind to human glucocorticoid receptors (hGR), estrogen receptors (hER), or rat androgen receptors (rAR). CP8754 can be used in the study of progesterone-related diseases such as breast cancer, endometriosis, uterine fibroids, and meningioma, as well as hormone-dependent tumors.
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DC80479 CP-85958
CP-85958 is a specific leukotriene D4 (LTD4) receptor antagonist. CP-85958 can be used in the research of inflammatory diseases such as asthma.
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DC80478 CP-470711
CP-470711 is an orally active and potent and selective sorbitol dehydrogenase (SDH) inhibitor with an IC50=10 nM for human SDH and IC50=17 nM for rat SDH. CP-470711 is promising for research of chronic complications related to type 2 diabetes mellitus, such as neuropathy and nephropathy.
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DC80477 CP-467688
CP-467688 is a retinal toxicant with a basic pKa=8.1 and lipophilic clogP=5.0. CP-467688 is promising for research of drug-induced retinopathy.
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DC80476 CP-457493
CP-457493 is an Erlotinib metabolite. CP-457493 can be detected in plasma.
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DC80475 CP 71362
CP 71362 is a renin inhibitor, a highly potent substrate-analog transition state mimic with antihypertensive properties. CP 71362 exhibits significant inhibitory activity against plasma renin from rats, dogs, and humans (IC50 values are 3 nM, 0.0033 nM, and 20 nM, respectively). CP 71362 reduces the mean arterial pressure of anesthetized and conscious sodium-depleted animals in a dose-dependent manner, and has pharmacokinetic characteristics of rapid elimination and short duration of action. CP 71362 can be used in research related to hypertension and congestive heart failure.
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DC80474 COX-2-IN-65
COX-2-IN-65 is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 10.24 μM. COX-2-IN-65 inhibits Staphylococcus aureus and Escherichia coli growth. COX-2-IN-65 scavenges reactive oxygen species (ROS). COX-2-IN-65 can be used for the researches of bacterial infections and inflammation.
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DC80473 COX-2/CaV2.2-IN-1
COX-2/CaV2.2-IN-1 is an orally active and selective dual COX-2/CaV2.2 inhibitor, exhibiting a COX-2 IC50 of 0.26 μM and a CaV2.2 IC50 of 0.29 μM. COX-2/CaV2.2-IN-1 suppresses inflammatory responses and inflammatory mediator (IL-6, TNF-α, NO) production. COX-2/CaV2.2-IN-1 produces pronounced analgesic effects in diverse models of inflammatory, neuropathic, and visceral pain. COX-2/CaV2.2-IN-1 can be used for the research of chronic pain.
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DC80472 COX-2/Aromatase-IN-2
COX-2/Aromatase-IN-2 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-2 can simultaneously inhibit COX-2 and aromatase, suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-2 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-2 can be used for the study of inflammation and breast cancer.
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DC80471 COX-2/15-LOX-IN-7
COX-2/15-LOX-IN-7 is a potent, selective and orally active dual inhibitor of COX-2 and 15-LOX with IC50 values of 0.022 and 1.19 μM. COX-2/15-LOX-IN-7 also inhibits COX-1 with an IC50 value of 28.081μM. COX-2/15-LOX-IN-7 has low cytotoxicity against human colorectal cancer HT-29 and HCT116 cell lines (IC50 >100 μM for both). COX-2/15-LOX-IN-7 exhibits non-ulcerogenic performance. COX-2/15-LOX-IN-7 can be used for the research of cancer.
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DC80468 Corthrombin
Corthrombin (CVS 995) is a potent alpha-keto-amide thrombin inhibitor with Ki of 1 pM. Corthrombin can be used for the research of cardiovascular disease.
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DC80467 Copanlisib-NH
Copanlisib-NH is a PI3Kα/δ ligand. Copanlisib-NH can be used as a ligand for target protein for PROTAC to develop and design degraders of PROTAC PI3Kα/δ, such as PROTAC PI3Kα/δ degrader-1. Copanlisib-NH can be used in breast cancer research.
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