A sensitive fluorogenic elastase substrate that is selectively cleaved by elastase to yield Rhodamine 110, which can be analyzed with an excitation wavelength of 485 nm and emission wavelength of 525 nm.

An analog of ceramide that inhibits alkaline ceramidase (IC50 ~5 µM); suppresses growth of HL-60 cancer cells in culture.

Formal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C₁₂H₁₅Cl₂NO

5-trans PGE2 occurs naturally in some gorgonian corals and is a common impurity in commercial lots of PGE1. It is 18 times more potent than PGE2 in activating adenylate cyclase in NCB-20 cell homogenates. 5-trans PGE2 accelerates fibrinolysis by enhancing plasminogen activation mediated by…

Unoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…

A selective, cell permeable inhibitor of MLCK (IC₅₀ = 50 nM).

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

A 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).

Modified with a carboxylic acid group terminating the C-16 alkyl chain, providing a convenient site for chemical crosslinking.

A potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53); has been used in cells and in animals.

A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.

8-hydroxy Guanine is produced by oxidative damage of DNA or RNA by reactive oxygen and nitrogen species, including hydroxyl radical and peroxynitrite. It serves as a measure of oxidative stress in biological systems.

An indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).

A “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…

A potent inhibitor of several CDKs with selectivity for Cdk2 (IC₅₀s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.

3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.

A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.

A form of polymyxin B which terminates with 6-methyloctanamide; comparable to other B polymyxins in its ability to kill P. aeruginosa, A. baumannii, and K. pneumoniae isolates.

Citrinin is a mycotoxin initially produced by Penicillum, Aspergillus, and Monascus. Citrinin exhibits cytotoxic, cardiotoxic, nephrotoxic, and pro-oxidative activities. In leydig cells, citrinin inhibits testosterone production and induces caspase-mediated apoptosis. In embryos, citrinin alters…

The four tocopherols (α, β, .delta., and γ) and four tocotrienols (α, β, .delta., and γ) are forms of vitamin E, which is known for its antioxidant activity. Tocotrienols are found at high concentrations in palm oil and rice bran. Recent studies show tocotrienols…

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5

A bioactive sterol that can affect cholesterol homeostasis, membrane properties and cell survival; inhibits CYP7A1 with an IC₅₀ = ~ 1 µM; can be used as a standard in the determination of cholesterol derivatives by GC-MS or HPLC.

A naturally occurring agonist for the nuclear receptor Nur77 (IC₅₀ = 0.278 nM); induces apoptosis in cancer cells and retards xenograft tumor growth; induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat/high cholesterol diet.

A 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.

RD162 is a second-generation androgen receptor (AR) antagonist. It inhibits binding of 18 F-FDHT to AR in human prostate cancer cells with an IC₅₀ value of 30.9 nM. RD162 completely suppresses VCaP cell proliferation at 1 µM and induces apoptosis of VCaP cells at 10 µM.…

An intermediary prodrug of fluorouracil, the pyrimidine analog that inhibits thymidylate synthase selectively in tumor cells, interfering with DNA synthesis; one of two intermediary metabolites formed during metabolic conversion of the chemotherapeutic prodrug, capecitabine, to fluorouracil.

A potent and selective PPARγ antagonist with an apparent IC50 value of 1 nM for the human receptor.

A corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.

The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR family of proteins, is coordinated by synthesis of diffusible acylhomoserine lactone (AHL) molecules. C6-HSL is a small diffusible signaling molecule involved in quorum sensing, controlling gene…

CAY10499 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.

A potent, stable, and selective agonist analog of AEA with a Ki value of 2.2 nM at the isolated rat CB1 receptor; 325 times more potent at the CB1 receptor compared with the CB2 receptor; induces hypothermia in mice with the same efficacy as AEA, in spite of its much higher affinity for the CB1…