A potent antagonist of dopamine receptors (IC₅₀s = 1.0 and 0.9 nM for D2 and D3, respectively);,also avidly binds α1- and α2-adrenergic receptors, histamine H1 receptor, and serotonin (5-HT) receptors 5-HT1D and 5-HT2A (Kis = 10, 80, 3.4, 19, 1.2 nM, respectively).

The major bioactive constituent of T. wilfordii Hook F., with known antiproliferative, immunosuppressive, anti-inflammatory, antifertility, and antipolycystic kidney disease effects; inhibits human DCTPP1 (Ki = 168 μM; IC50 = 7-10 nM) and COX-2 (IC50 = 0.04 μM).

An endogenous agonist of the CB1 and CB2 receptors; it is the most abundant molecular species of monoacylglycerol found in rat brain.

An 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…

A membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis; changes fluorescence characteristics with alteration in mitochondrial transmembrane potential, a very early event in apoptosis.

A small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.

A metabolite of the natural purine base that is generated by DNA methylation and has been used as a probe of protein-DNA interactions and for DNA sequencing methods; carcinogenic biomarker for cigarette smoking that is detectable in urine.

Spectral Characteristics: Visible absorption maximum = 545 nm, Emission maximum = 572 nm; This streptavidin with a SureLight® B-Phycoerythrin probe, binds biotinylated targets.

A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC₅₀ = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

An ATP/GTP-competitive inhibitor of CK2 (IC₅₀ = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC₅₀ = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

A natural pyrazinone produced by certain fungi and by Staphylococcus spp. that inhibits calpain in a casein hydrolysis assay (IC₅₀ = 1.3 µM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

A 4-azasteroid analog of testosterone that competitively blocks type II 5α-reductase activity (IC₅₀ = 4.2 nM) with 100-fold greater affinity than for the type I enzyme; used in the treatment of benign prostatic hyperplasia, decreasing human prostatic dihydrotestosterone levels by…

Bicyclo Prostaglandin E1 (bicyclo PGE1) is a stable, base-catalyzed transformation product of the PGE1 metabolite 13,14-dihydro-15-keto PGE1. Bicyclo PGE1 is a stable, base-catalyzed transformation product of the PGE1 metabolite 13,14-dihydro-15-keto PGE1. 13,14-dihydro-15-keto PGE1 itself is a…

A prodrug of a potent FP receptor agonist.

FK-409 is a NO donor. It liberates NO in a time-dependent manner with a half-life of approximately 40 minutes in phosphate buffer (pH 7.4) at 37°C. The IC₅₀ for the inhibition of platelet aggregation is 4.9 µM.

A potent inhibitor of iNOS (IC₅₀ = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC₅₀ = 350 μM).

A purine analog that inhibits mTOR (IC₅₀ = 37 nM) and PI3K (IC₅₀s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively); demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.

Dihomo-γ-linolenoyl PAF C-16 is a PAF analog which contains dihomo-γ-linolenoate at the sn-2 position rather than the acetate moiety found in PAF C-16. The biological activities of dihomo-γ-linolenoyl PAF C-16 are not known at present, but may be similar to arachidonoyl PAF C-16…

A bactericidal thioamide effective against M. tuberculosis (MIC = ~0.5 µg/ml), M. leprae (MIC = 0.8-1.6 mg/L), and M. avium; inhibits mycolic acid biosynthesis (Ki = 2 nM).

A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC₅₀ values between 10 and 30 µM; blocks the proliferation of erythroleukemia cells and human hematopoietic progenitor cells expressing JAK2-V617F.

A diterpene acid isolated from the bark of P. kaempferi, a traditional Chinese medicinal plant; has anti-fungal activities and diverse effects that are relevant to cancer therapy.

A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor (nm IC₅₀) that inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth; reduces…

A selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively; at 10 μM, has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).

A potent, cell-permeable inhibitor of PARP-1 (Ki = 5.5 μM); arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors.

A cell-permeable cAMP analog with improved lipophilicity compared to the PKA activators, 8-bromo-cAMP and Sp-cyclic AMPS; not readily degraded by PDE.

An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.

A polyunsaturated fatty alcohol produced by the reduction of linoleic acid.

A fluorogenic, sensitive substrate for human sEH which displays good aqueous stability and solubility making it ideal for high throughput screening programs.

Capsaicin is an agonist of transient receptor potential vanilloid (TRPV) channels that was originally found in peppers of the Capsicum genus. Capsaicin exhibits analgesic, anti-inflammatory, anti-obesity, and anticancer chemotherapeutic activity. Capsaicin also displays bronchoconstrictive activity…

A cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC₅₀ = 1.2-5.9 μM).

A potent, selective inhibitor of TrkA (IC₅₀ = 2 nM); used to clarify the role of TrkA in regulating cell function.

A rotenoid that exhibits antineoplastic and piscicidal activities; inhibits the NADH:ubiquinone oxidoreductase (IC₅₀ = 98 nM) and induces ornithine decarboxylase activity (IC₅₀ = 147 nM).