Biologically Active Small Molecules, 25 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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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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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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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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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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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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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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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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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…
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AZ 20
Cayman ChemicalA potent, selective inhibitor of ATR (IC50 = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.
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Flumazenil
Cayman ChemicalAn imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC50 = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.
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(R)-Equol
Cayman ChemicalAn ER agonist that binds to ERα and ERβ with Ki values of 27.4 and 15.4 nM, respectively; demonstrates higher ER agonist activity at ERα compared to ERβ (EC50 = 66 and 330 nM, respectively).
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KT195
Cayman ChemicalA selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.
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ß-Nicotinamide Mononucleotide
Cayman ChemicalAn intermediate in the biosynthesis of NAD+ that has been used to enhance NAD biosynthesis and glucose-stimulated insulin secretion in Nampt+/- mice and high-fat diet-induced type 2 diabetes mice.
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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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ML-097
Cayman ChemicalA small molecule pan activator of Ras-related GTPases, activating cdc42, Ras, and Rac1 with EC50 values of 102, 109, and 151 nM, respectively.
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PD 153035
Cayman ChemicalA potent, selective, reversible inhibitor of epidermal growth factor receptor (EGFR) kinase (Ki = 5.2 pM; IC50 = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.
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HEPC
Cayman ChemicalThioester analogs of glycerophospholipids, in combination with Ellman’s reagent, are convenient colorimetric substrates for the measurement of phospholipase activity. HEPC is a truncated analog of phosphatidylcholine with the entire sn-1 substituent deleted, and with a hexadecylthioester in…
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Bromosporine
Cayman ChemicalA non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.
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BI 6727
Cayman ChemicalA dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC50s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis; inhibits proliferation of multiple cancer cell lines (EC50s = 11-37 nM) and prevents the growth of various human carcinoma xenografts in mice.
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Garcinol
Cayman ChemicalAn inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.
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Solifenacin (succinate)
Cayman ChemicalA competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.
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C-8 Ceramide
Cayman ChemicalC-8 ceramide is a cell-permeable analog of naturally occurring ceramides. Unlike C-2 ceramide, it is metabolized within cells to generate natural ceramides, often causing a dramatic increase in cellular ceramide levels. For this reason, treatment of cells with C-8 ceramide may more closely mimic…
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8-bromo-Cyclic AMP (sodium salt)
Cayman ChemicalA cell permeable analog of cAMP that activates PKA with a Ka value of 0.05 μM; more stable to hydrolysis and has increased membrane permeability compared to unmodified cAMP.
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JNJ-26854165
Cayman ChemicalAn antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways.