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

15(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…

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).

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.

Anoninvasive, intracellular calcium indicator that is UV light-excitable; spectral properties in the presence of low calcium concentrations (excitation max = 362 nm, emission max = 512 nm) differ from those during high calcium conditions (excitation ma

An internal standard for the quantification of PGA2 by GC- or LC-MS.

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 natural oxidative metabolic product of the mycotoxin aflatoxin B2.

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.

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.

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…

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

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 plant growth regulator with anticancer activity.

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.…

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.

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 specific Akt inhibitor that has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells (IC₅₀ = 30-60 nM in vitro); inhibits Akt, PDK1, and FLT3 in acute myelogenous leukemia cells, decreasing the colony-forming ability of these cells (IC₅₀…

An intermediate in the HMG-CoA reductase pathway derived directly from farnesyl pyrophosphate and used in the biosynthesis of terpenes and terpenoids; also serves as a substrate in the prenylation of a variety of critical intracellular proteins including small GTPases.

The first identified small molecule inhibitor of BLM helicase (IC₅₀ = 1.8 μM) that is 28-fold selective against the related helicases RECQ1, RECQ5, and E. coli UvrD (IC₅₀s ≥ 50 μM); 25-50 μM dose-dependently inhibits the proliferation of BLM-expressing PSNF5…

PGB1 is a non-enzymatic dehydration product of PGE1 resulting from treatment with strong base. Oligomers of PGB1 are known to exhibit antioxidant and ionophoric activity.

A peptide antagonist of PAR2 which blocks activation by trypsin (IC₅₀ = ~50 μM) but not by the synthetic agonist SLIGRL-NH2; does not affect thrombin-induced activation of PAR1 or trypsin-mediated proteolysis of casein; used to study PAR2 action in cells and in animals.

A potent, semi-synthetic LXR agonist derived from extracts of the mayapple; induces the expression of the ABCA1 reverse cholesterol transporter to increase the efflux of cholesterol from enterocytes and thus inhibits the overall absorption of cholesterol (ED50 = 1 nM).

An inhibitor of both CDK1 and CDK2 (IC₅₀s =2.9 and 2.2 µM, respectively); inhibits cellular ataxia telangiectasia mutated and Rad3-realted kinase activity (IC₅₀ = 6.7 µM) and impairs G2/M arrest in various human cancer cells, potentiating the cytotoxic effects of…