An N-cyanosulphonamide that selectively blocks the sodium/bicarbonate cotransporter (NBC, also known as SLC4A7) with a Ki value of 1.7 µM, with full inhibition occurring at ~30 µM in myocytes; prevents changes in pH associated with depolarization and hyperpolarization of ventricular myocytes.

An inhibitor of HDAC, including HDAC1 (IC₅₀ = 0.1-0.2 μM); induces growth suppression and cell death of certain types of cancer cells in culture.

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

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…

CAS Number: 1228817-38-6 Molecular Formula: C₂₆H₃₆N₆O₃ Formula Weight: 480.6

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 cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

A competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.

An intermediate in the biosynthesis of NAD+ that has been used to enhance NAD biosynthesis and glucose-stimulated insulin secretion in Nampt+/- mice and high-fat diet-induced type 2 diabetes mice.

A competitive inhibitor of heme oxygenase that also inhibits soluble guanylyl cyclase and inactivates the NOS isoforms nNOS, iNOS, and eNOS (IC₅₀s = 0.8, 4, and 5 μM, respectively); used to assess iron status and to diagnose iron disorders and has shown therapeutic potential in hyperbilirubinemia.

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 cell-permeable inhibitor of SIRT1 (IC₅₀ = 56 µM) and SIRT2 (IC₅₀ = 59 µM); less effectively inhibits SIRT5 (IC₅₀ >300 µM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a…

ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC₅₀s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

A membrane-permeable cationic dye that is a substrate for P-gp and is rapidly exported from cells with functional P-gp; also accumulates within mitochondria and can be used to both localize mitochondria and study their properties.

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.

A natural isoflavone which promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.

A pan-caspase inhibitor that blocks apoptosis, prevents the production of cytokines, and inhibits T cell proliferation dose-dependently at 1-100 μM.

A cell permeable analog of BAPTA that binds calcium only after the AM group is removed by cytoplasmic esterases; commonly used at 10-100 μM to evaluate the role of intracellular calcium in cell signaling; also inhibits Kv channels, including Kv1.3, Kv1.5, and Kv11.1 (Ki = 1.45, 1.23, and 1.30…

An EPA-containing MAG amide analog that inhibits the growth of human lung carcinoma A549 cells, producing 98.4% growth inhibition when applied at 3 µM; an analog of EPEA, a natural N-acylethanolamide that impacts aging and inflammation.

A cell-permeable, reversible inhibitor of a mitochrondrial glutaminase splice variant, glutaminase C (IC₅₀ = ~2.5 µM), which is commonly found in cancer cells; blocks transformation induced by Rho GTPases and inhibits the proliferation of cancer cell lines without affecting normal cells.

An anthracycline antitumor antibiotic agent that inhibits DNA topoisomerase II by inducing double-stranded DNA breaks; inhibits nucleic acid synthesis and induces apoptosis by intercalating within DNA.

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.

A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC₅₀ = 80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.

A selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay (pA2 = 8.1); demonstrates analgesic activity in a mouse writhing assay (ED50 = 0.9 mg/kg); potentiates the vasorelaxation of human pulmonary vein induced by PGE2 (EC50 = 7.75 µM).

A cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC₅₀ = 15 μM); inhibits clathrin-dependent vesicle formation and endocytosis; can also augment the release of neurotransmitters and secreted cytokines.

A cell-permeable green fluorescent dye (excitation and emission maxima are 494 and 520 nm, respectively); used to analyze cell proliferation and track cell migration in vivo.

A first generation tyrosine kinase inhibitor that is used in the treatment of CML, GIST, and other cancers; selectively targets certain tyrosine kinases, including c-ABL, PDGFR, KIT, and the oncoprotein BCR-ABL.

Endogenous ligand of the APJ receptor, with an EC50 of 0.37 nM; acts primarily in the periphery and CNS, playing important roles in regulating cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity.

An aminooxy analog of ornithine that irreversibly inhibits aminotransferases, including ornithine aminotransferase (Ki = 2 µM); cytotoxic to a range of organisms.

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.

A non-symmetrically substituted indolylmaleimide that increases β-catenin levels by inhibiting GSK3β (IC₅₀ = 53 nM); reduces proliferation and increases differentiation of a ReNCell VM cell line derived from human ventral midbrain.