An inhibitor of Cdc7 kinase (IC₅₀ = 10 nM) as well as Cdk9, (IC₅₀ = 34 nM); induces apoptotic cell death in multiple cancer cell types at 10 µM.

A natural anthocyanin that has neuroprotective effects, reducing amyloid β-induced cytotoxicity in Neuro-2A cells; stimulates autophagy in U2OS cells.

A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

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.

A stable, cell-permeable molecule that generates free α-ketoglutarate upon hydrolysis by cytoplasmic esterases; used in experiments to increase levels of intracellular α-ketoglutarate and modulate a variety of enzymes, particularly in the context of glycolysis, hypoxia, and cancer.

A physiologically active metabolite of losartan; a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.

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.

A hybrid molecule patterned after N-arachidonoyl serotonin; inhibits capsaicin-induced TRPV1 channel activation (IC₅₀ = 2.57 μM) without blocking FAAH-mediated hydrolysis of arachidonoyl ethanolamine (IC₅₀ > 50 μM).

A highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC₅₀ = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.

A glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively); reversibly inhibits γ-glutamyl transpeptidase.

A cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

A biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.

A selective, ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC₅₀ = 104 nM); demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC₅₀ = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably…

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…

A small molecule inhibitor of human cytomegalovirus viral replication (EC₅₀ = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.

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.

A high-affinity ligand for retinoid X receptors (RXRs)(EC50 = 28, 25, and 20 nM for RXRα, β, and γ, respectively); inhibits cell cycle progression, induces apoptosis, and blocks angiogenesis and metastasis; stimulates clearance of soluble Aβ, reduces plaque area, and reverses…

A small molecule, multi-targeted receptor tyrosine kinase inhibitor; potently inhibits signaling through PDGFR, VEGFR, KIT, and FLT3; inhibits both tumor cell growth and angiogenesis; approved by the FDA for the treatment of gastrointestinal stromal tumor and metastatic renal cell carcinoma.

CAS Number: 883986-34-3 Molecular Formula: C₂₄H₂₅N₅O₄ Formula Weight: 447.5

Butaprost is a structural analog of PGE2 with good selectivity for the EP2 receptor subtype. Butaprost has frequently been used to pharmacologically define the EP receptor expression profile of various human and animal tissues and cells. Serious confusion as to the structure of Butaprost was…

A nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins (IC₅₀ = 7 nM); 60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally has been shown to restore…

An irreversible inhibitor of BMX (IC₅₀ = 8 nM) and BTK (IC₅₀ = 10.4 nM); inhibits the proliferation of Tel-BMX-transformed Ba/F3 prostate cancer cells (GI₅₀ = 25 nM), as well as RV-1, DU-145, PC-3, and VCAP prostate cancer cell lines (GI₅₀s = 2.54, 4.38,…

An inhibitor of PAD4 deimination activity (IC50 = 5.9 μM) that also inhibits PAD1 and PAD3 (IC50 = 0.8 and 6.2 μM, respectively); dose dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies in a CIA mouse model of inflammatory arthritis.

A selective inhibitor of cFMS kinase (IC₅₀ = 0.03 μM) that prevents CSF-1-induced monocyte growth with an IC₅₀ value of 0.14 μM; at 75-100 mg/kg, inhibits joint connective tissue and bone degradation in mouse models of arthritis.

A potent, orally available inhibitor of CDKs, blocking the Cdk9 activity of P-TEFb (IC50 = 8 nM) as well as all other CDK isoforms (IC50 = 100-300 nM); less effectively inhibits EGFR and PKA (IC50 = 21 and 122 μM, respectively); has potential applications in cancer therapy.

A small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

A mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.

A cell-permeable ACL inhibitor (IC₅₀ = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.

A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

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.