Biologically Active Small Molecules, UN3077, 25 mg
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Dynasore
Cayman ChemicalA cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC50 = 15 μM); inhibits clathrin-dependent vesicle formation and endocytosis; can also augment the release of neurotransmitters and secreted cytokines.
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ICI 192605
Cayman ChemicalICI 192605 is a potent antagonist of the thromboxane A2 receptor (TP) that blocks contraction of isolated guinea pig trachea induced by U-46619 (Item No. 16450; Kd = 0.398 nM). It is used to study the role of TP signaling in tissues and animals.
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Cobimetinib
Cayman ChemicalA selective, orally available inhibitor of MEK1 (IC50 = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.
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Magnolol
Cayman ChemicalA partial CB receptor agonist isolated from the bark of M. officinalis that has been used in Asian traditional medicine for the treatment of anxiety, sleep disorders, and allergic diseases; demonstrates selectivity for the peripheral CB2 receptor subtype (EC50 = 3.28 μM; Ki = 1.44…
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Efavirenz
Cayman ChemicalAn non-nucleoside reverse transcriptase inhibitor that prevents RNA plus-strand initiation (IC50 = 17 nM); also inhibits the late stages of HIV-1 replication by interfering with HIV-1 Gag-Pol polyprotein processing.
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Oxyphenbutazone
Cayman ChemicalAn NSAID that reduces edema in certain types of acute inflammation in animal models; a poor inhibitor of prostaglandin synthesis, but, like other NSAIDs, it inhibits OAT1 (Ki = 32 µM).
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G-1
Cayman ChemicalG-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM. Competitive binding studies in endoplasmic reticulum α- (ERα-) and ERβ-expressing cells yielded Ki values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial…
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Honokiol
Cayman ChemicalA natural product with diverse therapeutic effects, including acting as an anxiolytic in mice; inhibits NF-κB and PI3K/Akt signaling, preventing inflammation; interferes with angiogenesis while preventing tumor growth in vivo; scavenges superoxide and peroxyl radicals.
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2-Methoxyestradiol
Cayman ChemicalA natural metabolite formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol; has anticancer agent activity as an angiogenesis inhibitor via the HIF-1α pathway; levels are significantly lower in women with severe pre-eclampsia.