A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 4 nM), p59fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM).

A synthetic prodrug which is converted to the vitamin D receptor agonist 1,25-dihydroxy vitamin D3 in vivo; suppresses the synthesis and secretion of parathyroid hormone in secondary hyperparathyroidism; supports bone growth; provides renal and cardiovascular protection during chronic kidney disease.

=98% (HPLC), synthetic Synonym: (11a,13E,15S)-11,15-Dihydroxy-9-oxoprost-13-enoic acid, Alprostadil, PGE CAS Number: 745-65-3 Empirical Formula (Hill Notation): C20H34O5 Molecular Weight: 354.48 Beilstein Registry Number: 5294062 EC Number: 212-017-2 MDL number: …

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 type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.

An alkaloid that inhibits the growth of mouse leukemia P388 cells (IC₅₀ = 1.8 μg/ml); binds to and stabilizes the topoisomerase I-DNA binary complex, leading to DNA breakage and cell death (IC₅₀ = 5.07-12.6 μM); selectively inhibits CYP1A1 and CYP1A2 (IC50 = ~6 μM for…

A cyclic polypeptide-containing anticancer antibiotic that binds to DNA and blocks transcription by interfering with RNA synthesis; ~10 nM promotes cell death in a variety of tumors.

PGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC₅₀ of PGE1 for the inhibition of ADP-induced human platelet…

An analog of 1,24-dihydroxy vitamin D3 which, when used in a 4 μg/g ointment, suppresses psoriasis; inhibits the growth of both normal and psoriatic human keratinocytes (IC50 ~ 10 nM) via the vitamin D receptor; suppresses the production of RANTES and IL-8 by human dermal fibroblasts.

A 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.

An analog of wortmannin; irreversibly binds PI3K; inhibits recombinant PI3K and mTOR (IC₅₀ = 2.7 and 193 nM, respectively) and prevents the growth of LNCap cells (IC₅₀ = 1.46 μM).

Empirical Formula: C₁₈H₂₅NO₅ Linear Formula: C₁₈H₂₅NO₅ Formula Weight: 335.39 MDL Number: MFCD00221720 Purity: ≥95.0% (GC) Melting Point: 236 °C(lit.) Storage: −20°C Beilstein Registry…

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…

A potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC₅₀ values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A CYP2C9 metabolite of the NSAID diclofenac that demonstrates anti-inflammatory and analgesic properties by inhibiting COX and suppressing PGE2 synthesis.

An intermediate produced from vitamin D2 by cytochrome P450 isoforms in vertebrates; subsequently metabolized to 1,25-dihydroxy vitamin D2, which is an agonist for the vitamin D receptor.

Calcitriol is synthesized from 7-dehydrocholesterol in humans via a non-enzymatic photochemical reaction with 290-310 nm UV light in the skin. Hydroxylation of the resulting cholecalciferol in the liver produces 25-hydroxy Vitamin D3, the principal circulating form of Vitamin D. A second, tightly…

A 4-demethoxy analog of daunorubicin which intercalates in DNA and inhibits topoisomerase II, resulting in cancer cell cytotoxicity at low concentrations (IC₅₀ = 20-120 nM); effective in combination therapy for the treatment of different types of leukemia.

A potent, cell-permeable, and irreversible inhibitor of PI3K enzymes (IC50 = 1-10 nM).

An anti-coagulant; differs from (−)-warfarin by being five times less potent as a vitamin K antagonist; has a longer terminal elimination half-life (35-58 hours) than (−)-warfarin (24-33 hours).

An esterified form of the free acid which may be more amenable for certain applications.

A mycotoxin that specifically and reversibly inhibits sarco-endoplasmic reticulum Ca2+-ATPases (SERCA; IC50 = 0.6 μM); effectively inhibits SERCA in intact tissue, in smooth muscle and endothelium, as well as in isolated cells.

A natural chemical found in fresh ginger that activates TRPV1 (EC50 = 3.3 µM) as well as the TRP ankyrin receptor TRPA1 (EC50 = 10.4 µM).

A minor component of the oligomycin complex that acts as an inhibitor of the mitochondrial F1FO-ATP synthase, which leads to cell death.

A natural dithiol that reversibly inhibits bacterial and yeast RNA polymerases (IC50 = 3 μg/ml); used for the analysis of mRNA stability; inhibits endothelial cell adhesion (IC50 induced angiogenesis in mice by inhibiting Hsp27 interactions with cytoskeletal elements.

A mycotoxin produced from F. moniliforme, a prevalent fungus of corn and other grains that causes food poisoning in livestock and humans.

A selective EP1 antagonist that displays analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in rats; inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo; attenuates neuronal cell death in response to oxidative stress.

A water-soluble analog of forskolin which has both inotropic and vasodilator effects when administered intravenously; stimulates cardiac (type V) adenylyl cyclase more potently than other isoforms; relaxes guinea pig tracheal smooth muscle precontracted with histamine with an EC50 value of 32.6 nM.