Biologically Active Small Molecules, 1.0 mg
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Zearalenone
Cayman ChemicalA mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.
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17-phenyl trinor Prostaglandin A2
Cayman Chemical17-phenyl trinor PGA2 is a synthetic prostaglandin analog designed for increased half-life and greater potency. There are no published reports of the biological activity of 17-phenyl trinor PGA2 in the literature at this time.
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N-(2-phenylethyl)-Indomethacin amide
Cayman ChemicalN-2PIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-2PIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.06 and 0.125 µM, respectively. It is over 400 times less potent as an inhibitor of…
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a,ß-methylene Adenosine 5'-triphosphate (sodium salt)
Cayman ChemicalA phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.
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PF-477736
Cayman ChemicalAn ATP-competitive Chk1 inhibitor (Ki = 0.49 nM) that demonstrates 100-fold selectivity over Chk2; abrogates DNA damage-induced cell cycle arrest in tumor cell lines and xenografts, potentiating the antiproliferative effects of various chemotherapeutics.
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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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11ß-Prostaglandin E2
Cayman Chemical11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…
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Darifenacin (hydrobromide)
Cayman ChemicalA receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively); effective in treating problems related to the lower urinary tract.
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SMER3
Cayman ChemicalA selective inhibitor of SCFMET30 ubiquitin ligase, an E3 ligase that regulates transcription, cell-cycle control, and immune response; at 5 μM, upregulates a set of methionine biosynthesis genes by altering the SCFMET30 complex, preventing ubiquitination of target proteins, including Met4.
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DL-Glyceraldehyde-3-phosphate
Cayman ChemicalAn intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.
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Piriprost (potassium salt)
Cayman ChemicalPiriprost is a structural analog of PGI2 with low IP receptor-mediated activity. Piriprost inhibits 5-LO with an IC50 value around 100 µM, as measured by the release of 5-HETE from cultured myometrial cells. Piriprost inhibits the release of histamine and leukotrienes from isolated…
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BCTC
Cayman ChemicalA potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.
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(+)-Cloprostenol methyl amide
Cayman ChemicalA more lipid soluble form of (+)-cloprostenol, possibly serving as a prodrug for the bioactive free acid.
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Pexidartinib
Cayman ChemicalA brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively); blocks macrophage recruitment in mammary tumor-bearing mice and blocks glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.
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Bortezomib
Cayman ChemicalA dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM); drives cell cycle arrest and apoptosis in cancer cell lines and has applications in multiple myeloma and certain lymphomas, as well as other types of cancer.
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VPC 23019
Cayman ChemicalA competitive antagonist of S1P1 and S1P3 receptors (pKis = 7.86 and 5.93, respectively); inhibits S1P-induced migration of thyroid cancer cells, ovarian cancer cells, and neural stem cells.
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Arbidol (hydrochloride)
Cayman ChemicalA broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells; effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC50s range from 3-12.5 µg/ml).
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Biotin-XX hydrazide
Cayman ChemicalA biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.
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D-AP5
Cayman ChemicalA selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.
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CL 316,243
Cayman ChemicalA β3-adrenoceptor agonist (EC50 = 3 nM) that is >10,000-fold selective over β1 and β2; causes a rapid decrease in blood glucose level in mice and has been used to study the induction of brown adipocytes and to increase thermogenesis in a mouse model of dietary obesity.
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Doripenem
Cayman ChemicalA broad spectrum antibiotic that is in the β-lactam subclass known as carbapenems; effective against many Gram-negative and Gram-positive bacteria and is more effective against P. aeruginosa than other carbapenems; not effective against MSRA.
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ZLN005 (hydrochloride)
Cayman ChemicalA small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…
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15(R)-17-phenyl trinor Prostaglandin F2a
Cayman ChemicalAn isomer of 17-phenyl trinor PGF2α, characterized by an inverted (β) hydroxyl group at C-15.
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Biocytin
Cayman ChemicalA conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.
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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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RVX-208
Cayman ChemicalA selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 µM) over BD1 (IC50 = 1.8-3.1 µM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces…
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Tivantinib
Cayman ChemicalA staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM).
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trans-ISRIB
Cayman ChemicalA symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC50 = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.
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CYT387
Cayman ChemicalAn ATP-competitive inhibitor of JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.
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MK-2206 (hydrochloride)
Cayman ChemicalAn orally active, allosteric Akt inhibitor (IC50s = 5, 12, and 65 nM for Akt1, 2, and 3, respectively); inhibits cell proliferation of human cancer cell lines synergistically in combination with other topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth…