A monoacetylated derivative of spermine (Item No. 18041), an endogenous polyamine synthesized from spermidine (Item No. 14918), that displays lower Km and higher Vmax values than spermine, making it a better substrate of polyamine oxidase than the non-acetylated polyamine.

A potent, selective, and competitive inhibitor of ATGL (IC₅₀ = 0.7 μM); does not inhibit hormone-sensitive lipase, monoglyceride lipase, pancreatic lipase, lipoprotein lipase, or other lysophospholipases; blocks lipolysis by ATGL in vitro, in white adipose tissue organ cultures, and…

A LPA analog containing stearyl alcohol at the sn-1 position; exhibits platelet aggregating activity with an EC50 value of 9 nM versus an EC50 value of 177 nM for 1-octadecanoyl LPA.

A natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes; also a weak inhibitor of the related zinc metalloprotease ECE (Ki = 3.5 µM); has little or no effect on a variety of other proteases.

DuP-697 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK-966 (rofecoxib), SC-58125, and celecoxib. DuP-697 is a potent and time-dependent inhibitor of COX-2. When tested on isolated recombinant enzymes, DuP-697 is at least 50 times more potent in the…

A selective inhibitor of MEK1 and MEK2 (IC₅₀s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2; rapidly passes the blood-brain barrier and has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.2 and 5 nM, respectively); studied in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors.

A specific and potent inhibitor of MPC carrier activity; potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC₅₀ = 50 nM).

A potent and selective inhibitor of reticulocyte 15-LO-1.

A triazolothiadiazine that inhibits PDE4 (EC₅₀ = 18.7 nM in a cell-based assay); selectively inhibits PDE4A (IC₅₀ = 6.7 nM) over PDE4B1, PDE4B2, PDE4C1, and PDE4D2 (IC₅₀ = 48.2, 37.2, 452, and 49.2 nM, respectively).

A inhibitor of Epac1 and Epac2 (IC₅₀s = 3.2 and 1.4 µM, respectively); blocks Akt phosphorylation and insulin secretion in pancreatic β cells and inhibits the migration of AsPC-1 and PANC-1 pancreatic cancer cells in vitro.

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

A cyclododecadepsipeptide potassium-selective ionophore antibotic; induces apoptosis in several cell tyes, including CHO cells, by stimulating potassium efflux.

A RARβ agonist, RARα/γ antagonist that inhibit the proliferation of normal breast cells via the induction of TGF-β activity, causing G1 arrest; used to trigger the differentiation of mouse embryonic stem cells.

An inhibitor NF-κB activation in vitro and in vivo (IC₅₀ = 5 µM).

A non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

A dual inhibitor of IGF1R kinase and IR (IC₅₀s = 100 and 73 nM, respectively); blocks IFG1R autophosphorylation and signaling through MEK1/2 and Akt, leading to G1 arrest and apoptosis in ML-1 cells; reverses EMT in MCF10A cells overexpressing constitutively activated IGF1R.

A divalent cation ionophore, commonly used to facilitate the movement of Ca2+ into cells, triggering the activation of intracellular calcium-dependent pathways; also used to produce apoptosis through calcium overload, as occurs during hypoxic or oxidative stress.

A noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC₅₀ = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC₅₀s range from 1-7 μM).

A compound used to increase the levels of H₂S within mitochondria; stimulates mitochondrial electron transport and improves cellular bioenergetic function at lower concentrations (30-100 nM), while having an inhibitory effect at 300 nM; is effective in vivo.

An inhibitor of EGF receptor kinase with an IC50 value of 1 µM in HT-22 cells.

MAHMA NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 1 minute and 3 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

One of four major analogs in the enniatin complex that has been shown to moderately inhibit ACAT activity in rat liver microsomes (IC₅₀ = 22 µM); demonstrates anthelmintic properties against N. brasiliensis, T. spiralis, and H. spumosa.

A polymethoxylated flavone that has been shown to enhance adipogenesis and lipolysis, to inhibit α-glucosidase and α-amylase activity, and to suppress the expression of genes associated with inflammation by regulating IκBα.

A dual inhibitor of DNA-PK and PI3K.

A selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor); used to induce hyperemia, particularly in the context of myocardial perfusion imaging.

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…

An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

An inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC₅₀ = 2.0 µM) over a control (mammary epithelial) cell line (EC₅₀ = 64 µM).

A fluorescent substrate for calpain and papain (excitation max: 360 nm; emission max: 460 nm) that is used for measuring the chymotrypsin-like peptidase activity of the 20S proteasome.

A selective antagonist of S1P binding to the S1P3 receptor; blocks calcium increase in HeLa cells by about 40% at 10 µM.

A small molecule that binds to CBFβ and inhibits its association with Runx1 (IC₅₀ = 3.2 µM); blocks CBFβ-Runx1 interactions in ME-1 cells, acute myeloid leukemia cells harboring dysfunctional CBF, reducing proliferation without toxicity.