Bottle, Glass, Clear, 25 mg, Cayman Chemical
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ML-204
Cayman ChemicalML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…
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Luzindole
Cayman ChemicalA melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values = 10-27 and 158-513 nM, respectively); used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways.
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A-77-01
Cayman ChemicalA-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC50 = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks…
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5-fluoro 203
Cayman ChemicalA cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…
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Cyclic Pifithrin-a (hydrobromide)
Cayman ChemicalA stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC50 = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…
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CAY10499
Cayman ChemicalCAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme. The in vivo pharmacological efficacy of CAY10499 has not been reported.
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Eltrombopag
Cayman ChemicalEltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase…
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ON-01910 (sodium salt)
Cayman ChemicalA potent, non-ATP-competitive inhibitor of Plk1 (IC50 = 9 nM); induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM); active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents.
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3-Methyladenine
Cayman ChemicalA specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.
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ß-Nicotyrine
Cayman ChemicalAn alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.
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GW 2580
Cayman ChemicalA selective inhibitor of cFMS kinase (IC50 = 0.03 μM) that prevents CSF-1-induced monocyte growth with an IC50 value of 0.14 μM; at 75-100 mg/kg, inhibits joint connective tissue and bone degradation in mouse models of arthritis.
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MS37452
Cayman ChemicalA competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM); derepresses transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells at 250 µM.
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1-Palmitoyl Lysophosphatidic Acid
Cayman ChemicalAn LPA analog containing palmitic acid at the sn-1 position.
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HA-155
Cayman ChemicalA selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.
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Hexanolamino PAF C-16
Cayman ChemicalHexanolamino PAF C-16 is a PAF analog with mixed PAF receptor agonist/antagonist properties. In human monocyte-derived macrophages, it is an antagonist which inhibits the production of reactive oxygen species in response to PAF C-16. On the other hand, in rabbit platelets and guinea pig…
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Kanosamine (hydrochloride)
Cayman ChemicalAn antibiotic that can inhibit cell wall synthesis in plant-pathogenic oomycetes (MIC = 25 µg/ml for P. medicaginis M2913) and certain fungi as well as some bacterial species (MIC = 400 µg/ml for S. aureus).
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5-(N-ethyl-N-isopropyl)-Amiloride
Cayman ChemicalA potent inhibitor of several NHE isoforms, inhibiting NHE1, NHE2, NHE3, and NHE5 with Ki values of 0.02, 0.5, 2.4, and 0.42 μM, respectively; less effectively inhibits NHE4 (IC50 ≥10 μM).
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L-Canaline
Cayman ChemicalAn aminooxy analog of ornithine that irreversibly inhibits aminotransferases, including ornithine aminotransferase (Ki = 2 µM); cytotoxic to a range of organisms.
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SC-19220
Cayman ChemicalA dibenzoxazepine which acts as a selective antagonist of PGE2 at the human EP1 receptor (IC50 = 6.7 µM); at doses between 0.3-300 µM, is a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach and trachea.
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BAZ2-ICR
Cayman ChemicalA selective inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains.
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Atorvastatin (calcium salt)
Cayman ChemicalAn HMG-CoA reductase inhibitor that is effective in treating hypercholesterolemia and certain dyslipidemias; reduces the production of LDL as well as inhibiting cholesterol synthesis; metabolized by CYP3A4, prodrug several metabolites that are important in the therapeutic actions attributed to atorvastatin.
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N-Arachidonoyl-L-Serine
Cayman ChemicalAn endocannabinoid analog that does not bind to CB1, CB2, or TRPV1; at 5 mg/kg antagonizes the hypotensive effects of a 10 mg/kg IV bolus of abnormal cannabidiol (Abn-CBD) in an anesthetized rat blood pressure model; relaxes isolated rat mesenteric arteries and abdominal aorta, and increases the…
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Genipin
Cayman ChemicalA protein cross-linking agent isolated from G. jasminoides Ellis; inhibits UCP2 activity; 5 µM genipin increases glucose-stimulated insulin secretion in isolated pancreatic islets chronically exposed to high levels of glucose; induces apoptosis in FaO rat hepatoma cells and human…
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N1-Acetylspermine (hydrochloride)
Cayman ChemicalA monoacetylated derivative of spermine (Item No. 18041), an endogenous polyamine synthesized from spermidine (Item No. 14918), that displays lower Km and higher Vmax values than spermine, making it a better substrate of polyamine oxidase than the non-acetylated polyamine.
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Calindol (hydrochloride)
Cayman ChemicalA phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling; stimulates PI hydrolysis and proliferation through human CaSR (pEC50 values are 6.9 and 7.4, respectively) in the presence of calcium.
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a-Hydroxyglutaric Acid (sodium salt)
Cayman ChemicalAn α-hydroxy acid, overproduced in 2-hydroxyglutaric aciduria; mutations in IDH1 and IDH2 cause these enzymes to convert isocitrate to 2-hydroxyglutarate; competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.
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ß-Elemene
Cayman ChemicalA natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.
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A-23187
Cayman ChemicalA divalent cation ionophore, commonly used to facilitate the movement of Ca2+ into cells, triggering the activation of intracellular calcium-dependent pathways; also used to produce apoptosis through calcium overload, as occurs during hypoxic or oxidative stress.
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4EGI-1
Cayman ChemicalAn inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (KD = 25 μM); prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis; blocks translation in some viruses that do not require eIF4E or a cap structure for initiation.
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3,4',5-Trismethoxybenzophenone
Cayman ChemicalAn analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol