Biologically Active Small Molecules, 50 mg
-
L-(+)-Ergothioneine
Cayman ChemicalA naturally-occurring amino acid which is a stable antioxidant; scavenges free radicals and oxidants, controls NF-κB activation, and inhibits inflammatory gene expression; blocks oxidative DNA damage and cell death.
-
Coumarin Boronic Acid pinacolate ester
Cayman ChemicalA fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.
-
Erbstatin Analog
Cayman ChemicalA stable, potent analog of erbstatin; inhibits EGFR tyrosine kinase in vitro with an IC50 of 0.14 µg/ml; inhibits EGF-stimulated growth in NIH3T3 cells with an IC50 value of 0.5 µg/ml; delays onset of EGF-induced DNA synthesis.
-
Glufosinate (ammonium salt)
Cayman ChemicalA racemic mixture of D- and L-phosphinothricin, used as the active ingredient in broad spectrum herbicides; also used, with the bar gene, which encodes phosphinothricin acetyltransferase, for selection during genetic engineering in plants.
-
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…
-
Zileuton
Cayman ChemicalZileuton (Zyflo™) is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. It is a…
-
SB-743921 (hydrochloride)
Cayman ChemicalCAS Number: 940929-33-9 Molecular Formula: C31H33ClN2O3 • HCl Formula Weight: 553.5
-
Vitexin
Cayman ChemicalAn apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.
-
-
Obatoclax (mesylate)
Cayman ChemicalAn antagonist of Bcl-2 family members containing four Bcl-2 homology domains, including Bcl-2, Bcl-W, Bcl-xL, and Mcl-1 (Kd ~500 nM); prevents interaction of these pro-survival proteins with Bax or Bak, inducing apoptosis; also induces autophagy in mouse embryo fibroblasts and in HeLa cell.
-
-
WYE-354
Cayman ChemicalA selective, potent, and cell-permeable inhibitor of mTOR (IC50 = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.
-
2,4-DPD
Cayman ChemicalA cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.
-
2-hydroxy Flutamide
Cayman ChemicalThe major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC50 = ~300-900), blocking the expression of AR target genes.
-
Estradiol 17-(ß-D-Glucuronide) (sodium salt)
Cayman ChemicalAn estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.
-
N-(ß-ketocaproyl)-L-Homoserine lactone
Cayman ChemicalA HSL compound produced in the marine bioluminescence bacterium V. fischeri.
-
Cilostazol
LKT LabsCilostazol is a quinolone inhibitor of phosphodiesterase 3B (PDE 3B) that exhibits vasodilatory, antiplatelet, anti-inflammatory, anti-diabetic, antidepressant, anxiolytic, and pro-angiogenic activities. Cilostazol is clinically used to treat intermittent claudication associated with peripheral…
-
1,2-Diphytanoyl-sn-glycero-3-PE
Cayman ChemicalA phospholipid containing the tetramethylated long-chain (16:0) diphytanic acid inserted at the sn-1 and sn-2 positions.
-
Rivaroxaban
Cayman ChemicalAn orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM) that inhibits thrombin formation without prolonging bleeding time; approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.
-
Mn(III)TMPyP
Cayman ChemicalMn(III)TMPyP is a cell-permeable SOD mimic and peroxynitrite decomposition catalyst. The rate constants for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M−1s−1 and ~2 x 106 M−1s−1, respectively.
-
Saracatinib
Cayman ChemicalA dual inhibitor of c-Src and Abl (IC50 = 2.7 and 30 nM, respectively); less effectively inhibits other kinases; blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival; reduces osteoclast bone resorption.
-
8-bromo-Cyclic GMP (sodium salt)
Cayman ChemicalA cell-permeable analog of cGMP that preferentially activates cGMP-dependent protein kinase; 1 µM-0.1 mM inhibits acetylcholine-induced increases in intracellular calcium concentrations.
-
Ganciclovir
Cayman ChemicalA synthetic analog of 2'-deoxy-guanosine which is used to treat or prevent cytomegalovirus (CMV) infections; inhibits the replication of human CMV with an IC50 value of 0.01 μM and is effective against strains of CMV from human, monkey, mouse, and guinea pig.
-
Bufalin
Cayman ChemicalA cardiotonic steroid that inhibits theNa+/K+-ATPase transporter (Kds = 42, 45, and 40 nM for the α1, α2, and α3 subunits, respectively); inhibits SRC-1 and SRC-3 at doses as low as 5 nM, promotes the degradation of SRC-3 protein, and inhibits cancer cell growth both in vitro and…
-
Isoxanthopterin
Cayman ChemicalA natural intermediate in the pteridine pathway that can be produced naturally from 7-oxobiopterin or in vitro by the oxidation of pterin by xanthine oxidase.
-
Olvanil
Cayman ChemicalA structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum genus, and the amide of vanillylamine and oleic acid; acts as an agonist at TRPV1, inducing desensitization analgesia in rat and mouse models of pain; potentiates the agonist activity of…
-
Docosahexaenoic Acid
Cayman ChemicalAn essential fatty acid and the most abundant ω-3 fatty acid in neural tissues, especially in the retina and brain; constitutes as much as 40% of the total PUFA pool in retinal and neuronal membranes; dietary supplementation via fish oil inhibits the progression of atherosclerosis and delays…
-
BAY 41-2272
Cayman ChemicalAn activator of sGC, stimulating activity at concentrations as low as 10-100 nM; inhibits platelet aggregation (IC50 = 36 nM), induces relaxation of preconstricted aorta rings (IC50 = 304 nM); effective in vivo, decreasing mean arterial blood pressure in hypertensive rats.
-
Phortress
Cayman ChemicalA lysyl amide prodrug of the benzothiazole 5-fluoro 203, a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1, which leads to the formation of DNA adducts and cell cycle arrest.
-
Aprotinin
Cayman ChemicalA reversible inhibitor of serine proteases such as trypsin (Ki = 0.06 pM), chymotrypsin (Ki = 9.5 nM), and kallikrein (Ki = 0.8 nM); widely used as a protein purification tool to prevent proteases present in tissue samples from degrading the protein of interest.
-
-
Dihomo-y-Linolenic Acid
Cayman ChemicalAn elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.