Biologically Active Small Molecules
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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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LY2157299
Cayman ChemicalA small molecule inhibitor of the TGF-β receptor type 1 kinase (IC50 = 56 nM) that has been used to study the role of TGF-β signaling in triple negative breast cancer cells and hepatocellular carcinoma cells.
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Meclofenamate (sodium salt)
Cayman ChemicalA time-dependent, non-specific COX inhibitor with IC50 values of 1.5 and 9.7 µM for human recombinant COX-1 and COX-2, respectively.
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Pyridoxal isonicotinoyl hydrazone
Cayman ChemicalA lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and also in vivo in rats and mice.
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Azithromycin Dihydrate
LKT LabsAzithromycin is an azalide macrolide antibiotic derived from erythromycin. Azithromycin binds the bacterial 50S ribosomal subunit, inhibiting protein translation. Azithromycin displays antibacterial, anti-fibrotic, and anti-inflammatory activities. In epithelial cells, azithromycin inhibits the…
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L-161,982
Cayman ChemicalA potent and selective EP4 receptor antagonist (Ki = 24 nM); reverses the anti-inflammatory action of PGE2 in LPS - activated human macrophages at 100 nM.
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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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Licochalcone A
Cayman ChemicalA natural chalcone that has anti-inflammatory actions, supporting its use as a skin lightening agent, particularly for rosacea and atopic dermatitis; induces apoptosis and suppresses migration and invasion of cancer cells in vitro; has antibacterial and anti-parasitic actions.
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Prostaglandin E2 p-acetamidophenyl ester
Cayman ChemicalPGE2 p-acetamidophenyl ester is a crystalline derivative of PGE2. PGE2 is one of the primary COX products of arachidonic acid and one of the most widely investigated PGs. Its activity influences inflammation, fertility and parturition, gastric mucosal integrity, and immune modulation. The effects…
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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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Doxepin (hydrochloride)
Cayman ChemicalA tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.
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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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ARRY-162
LKT LabsARRY-162 is an orally bioavailable noncompetitive inhibitor of MEK1/2 and ERK that shows anticancer chemotherapeutic activity. Inhibition of MEK inhibits downstream signaling by IL-1, IL-6, and TNF. ARRY-162 inhibits proliferation in melanoma, non-small-cell lung cancer (NSCLC), head/neck cancer,…
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Acridine Orange
Cayman ChemicalA cell-permeable, fluorescent dye that accumulates in acidic organelles in a pH-dependent manner and is used for autophagy detection and cell cycle determination; emits green fluorescence (ex. max: 502 nm; ,em. max: 525 nm) at neutral pH or when bound to dsDNA and red fluorescence (ex. max: 460 nm;…
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Aztreonam
Cayman ChemicalA monobactam antibiotic that is effective against Gram-negative bacteria but inactive against Gram-positive bacteria.
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Fulvestrant
Cayman ChemicalA potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.
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Gö 6983
Cayman ChemicalInhibits several isoforms of protein kinase C (PKC; IC50 = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.
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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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AEBSF (hydrochloride)
Cayman ChemicalA water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.
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15(S)-15-methyl Prostaglandin F2a
Cayman Chemical15(S)-15-methyl PGF2α is a metabolically stable analog of PGF2α. It is a potent uterine stimulant and abortifacient which can be administered intramuscularly to induce labor. It induces luteolysis and reduces serum progesterone concentrations when given as an intramuscular injection in…
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CAY10678
Cayman ChemicalA benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment…
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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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Linolein Hydroperoxides
Cayman ChemicalLinolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…
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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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HDMAPP (ammonium salt)
Cayman ChemicalA microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.
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Streptozotocin
Cayman ChemicalA glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.
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Aflatoxin M1
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin M1 is the hydroxylated metabolite of aflatoxin B1; it inhibits DNA synthesis and induces cell cycle arrest.
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2,3-dinor-11ß-Prostaglandin F2a
Cayman ChemicalKey urinary metabolite of PGD2; represents approximately 1% and 4% of the infused radiolabeled dose in monkeys and humans, respectively.
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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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KB2115
Cayman ChemicalA synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.
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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.