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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC79456 Yoda2
Yoda2 (KC289) is the potassium salt of Yoda1. Yoda2 is an agonist of PIEZO1 with an EC50 of 150 nM. Yoda2 evokes Ca2+ elevation in HeLa cells. Yoda2 can cause concentration-dependent and NO-dependent relaxation in mouse portal vein (EC50 = 1.2 μM). Yoda2 can stimulate NOS3 and NO production.
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DC79455 E-3709
E3709 is an antibacterial agent. E3709 exhibits significant inhibitory activity against Gram-positive bacteria, including Staphylococcus aureus (MRSA), Enterococcus faecalis, streptococci, Clostridia, and diphtheroids. E3709 can be used for research related to Gram-positive bacterial infections.
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DC79454 CKD-731
CKD-731 is a Fumagillin analogue. CKD-731 inhibits the proliferation of calf pulmonary artery endothelial cells (CPAE), lymphoma EL-4 cells and murine leukemia P388D1 cells. CKD-731 exerts the effect of inhibiting MetAP-2 activity and blocking angiogenesis. CKD-731 can be used for the research of anti-angiogenesis-related cancer.
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DC79453 UCM-05194 ammonium
UCM-05194 (ammonium) is a lysophosphatidic acid receptor 1 (LPA1) agonist. UCM-05194 (ammonium) induces calcium mobilization in LPA1-expressing RH7777 cells (EC50 = 0.24 µM). UCM-05194 (ammonium) induces neurite retraction and migration in LPA1-overexpressing B103 rat neuroblastoma cells. UCM-05194 (ammonium) attenuates acetic acid-induced writhing and hind paw mechanical hypersensitivity in mice.
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DC79452 ST-899
ST-899 is a novel platelet-activating factor (PAF) receptor antagonist. ST-899 can significantly reduce the mortality of mice with endotoxin (LPS)-induced shock. ST-899 can significantly inhibit the increase in serum tumor necrosis factor (TNF) levels induced by LPS, but has no effect on interleukin-6 (IL-6). The regulatory mechanism of ST-899 is to block the positive feedback loop between PAF and TNF, thereby reducing the inflammatory response. ST-899 can be used to study inflammatory diseases such as septic shock.
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DC79451 ent-Rhizocarpic acid
ent-Rhizocarpic acid is an enantiomer of Rhizocarpic acid. ent-Rhizocarpic acid has more potent antibacterial and antiparasitic activity against Staphylococcus aureus (ATCC 25923) and Giardiaduodenalis 713 compared to Rhizocarpic acid. ent-Rhizocarpic acid also has a weak but selective antitumor activity against NS-1 cells.
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DC79449 L-163007
L-163007 is an orally active AT1/2 receptor antagonist. L-163007 can be used for the research of cardiovascular disease, such as hypertension.
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DC79446 OSBP ligand-Linker Conjugate 1
OSBP ligand-Linker Conjugate 1 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for OSBP and a PROTAC linker, which recruits E3 ligases. OSBP ligand-Linker Conjugate 1 can be used for synthesis of PROTAC OSBP Degrader-1.
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DC79444 CP-114271
CP-114271 is a potent selective β3-adrenergic receptor agonist. CP-114271 possesses an in vivo efficacy in rodent models. CP-114271 can be used for obesity research.
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DC79442 RIPK1-ligand-2
RIPK1-ligand-2 is a RIPK1 inhibitor. RIPK1-ligand-2 can be used for synthesis of PROTAC RIPK1 Degrader-1.
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DC79440 AT-1459
AT-1459 is a selective and orally active direct Thrombin inhibitor with a Ki value of 4.9 nM. AT-1459 exhibits excellent antithrombotic activity in both rat models of venous and arterial thrombosis. AT-1459 can be used for research on thrombosis-related diseases.
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DC79438 N-Descyclopropanecarbaldehyde Olaparib suberic acid
N-Descyclopropanecarbaldehyde Olaparib suberic acid is a ligand-linker conjugate that can be used for the synthesis of DDO3602.
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DC79436 CP-664511
CP-664511 is an orally active and potent α4β1 integrin antagonist with anti-inflammatory effects (IC50=0.52 nM). CP-664511 inhibits the interaction between α4β1 and vascular cell adhesion molecule-1 (VCAM-1), significantly reducing eosinophil infiltration into lung tissue. CP-664511 is promising for research of asthma and allergic airway diseases.
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DC79435 CP-331684
CP-331684 is an orally active agonist of β3-Adrenergic receptor. CP-331684 can be studied in research on obesity.
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DC79434 AM-461
AM-461 is a DP2 receptor (Prostaglandin Receptor) antagonist. AM-461 can be used for the researches of inflammation and immunology, such as asthma.
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DC79433 PSMA ligand 1
PSMA ligand 1 (Compound 1c) is a PSMA ligand with an IC50 of 26.74 nM. The [18F]-labeled PSMA ligand 1 can serve as a PSMA PET tracer and is used in research on the diagnosis of prostate cancer.
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DC79432 CB 3705
CB 3705 is a dihydrofolate reductase (DHFR) and thymidylate synthetase (TS) inhibitor. CB 3705 inhibits L1210 cells and mutant L1210 cell line (L1210:C15) with ID50s of 4.77 μM and 408 μM, respectively.
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DC79431 EMD527040 hydrochloride
EMD527040 (hydrochloride) is a highly potent and selective αvβ6 antagonist with anti-fibrotic activity. EMD527040 (hydrochloride) is used in the research of liver cancer and liver fibrosis.
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DC79430 DS21412020
DS21412020 is a fluoroquinolone antibacterial agent. DS21412020 inhibits bacterial DNA gyrase (GyrA) and topoisomerase IV, leading to DNA breaks. DS21412020 exhibits significant activity against Gram-positive bacteria such as Staphylococcus aureus (MIC = 0.006 μg/mL), Streptococcus pneumoniae (MIC = 0.05 μg/mL), and Methicillin)-resistant Staphylococcus aureus (MIC = 0.2 μg/mL), and Gram-negative bacteria such as Escherichia coli (MIC = 0.006 μg/mL) and Pseudomonas aeruginosa (MIC = 0.78 μg/mL). DS21412020 significantly reduces bacterial load in mouse pneumonia and MRSA infection models. DS21412020 can be used in the development of next-generation quinolone antibiotics.
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DC79429 APL-5125
APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC50 of 0.348 nM and a Ki of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer.
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DC79427 GA-0056
GA-0056 is an angiotensin II receptor blocker. GA-0056 can be used in the research of heart disease.
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DC79426 UK-356202
UK-356202 is a urokinase-type plasminogen activator (uPA) with a Ki value of 0.037 μM. UK-356202 can be used in research related to the topical treatment of chronic ulcerous wounds.
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DC79423 ABT-255 hydrochloride
ABT-255 hydrochloride is an orally active anti-bacterial agent. ABT-255 hydrochloride exhibits potent in vitro potency (MIC = 0.016-0.031 μg/mL) against drug-susceptible and Rifampin- or Ethambutol-resistant Mycobacterium tuberculosis. ABT-255 hydrochloride shows efficacy against S. aureus, S. pneumoniae and E. coli and reduces viable counts of drug-resistant Mycobacterium tuberculosis in CF-1 mice. ABT-255 hydrochloride can be used for the study of pulmonary tuberculosis.
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DC79422 MRS4917
MRS4917 is an orally active, potent selective P2Y14 receptor (hP2Y14R) antagonist (IC50 = 2.88 nM, Ki = 1.67 nM) that shows >18,000 fold selectivity against P2Y6R (IC50 = 54 μM). MRS4917 demonstrates oral efficacy in reversing established mechanoallodynia in the chronic constriction injury (CCI) mouse model, while having no effect on thermoregulation. MRS4917 can be used for neurological diseases research.
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DC79421 AJI-9561
AJI-9561 is a benzoxazole derivative produced by Streptomyces sp. AJI-9561 exhibits cytotoxicity and antibacterial activity. AJI-9561 inhibits the proliferation of Jurkat T cells and mouse P388 leukemia cells, with its IC50 being 0.88 and 1.63 μM respectively. AJI-9561 can be used for research on anti-cancer and antibacterial properties.
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DC79420 FR-158999
FR-158999 is a potent orally active fibrinogen inhibitor. FR-158999 exhibits potent anti-platelet activities with a pIC50 of 7.50. FR-158999 can be used for antithrombotic research.
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DC79419 BMS-180431
BMS-180431 is an inhibitor of HMG-CoA reductase (IC50: 43 nM).
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DC79418 ZD 2486
ZD 2486 is a glycoprotein IIb/IIIa (GP IIb/IIIa) antagonist. ZD 2486 inhibits platelet aggregation by blocking the binding of fibrinogen to the GP IIb/IIIa receptor on platelets. ZD 2486 can be used for the study of conditions related to unwanted platelet aggregation, such as acute coronary syndrome, unstable angina pectoris, acute myocardial infarction, and complications from cardiovascular interventional procedures[1]
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DC79417 HCV-371
HCV-371 is a highly selective, potent, and low cytotoxicity HCV NSSB (EC50 = 4.8-6.1 μM) polymerase allosteric inhibitor. HCV-371 can be used for research on hepatitis C virus infection.
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DC79416 (R,R)-dWIZ-1 TFA
(R,R)-dWIZ-1 TFA is the the (R,R)-enantiomer of dWIZ-1. dWIZ-1 is a potent WIZ molecular glue degrader. dWIZ-1 has the potential for the research of sickle cell disease (SCD).
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