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.

Formal Name: N-?[[(4-?aminophenyl)?amino]?thioxomethyl]?-?4-?(1,?1-?dimethylethyl)?-benzamide CAS Number: 1011301-27-1 Molecular Formula: C₁₈H₂₁N₃OS

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.

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 27 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation,…

A colorimetric substrate whose amino acids YVAD have been shown to be a preferred cleavage site for caspase-1 and -4.

A water soluble and metabolically stable curaxin that activates p53 with an EC₅₀ value of 0.37 µM and inhibits NF-κB with an EC₅₀ of 0.47 µM; has broad anticancer activity in mice when administered orally.

A non-nucleoside pyridopyrimidine compound that selectively blocks the action of adenosine kinase in an adenosine-competitive manner (IC₅₀ = 1.7 nM in cell-free assays); suppresses nociception in various rodent pain models.

A macrolide antibiotic with antifungal activity; also cytotoxic against trypanosomes (IC₅₀ = 120-540 ng/ml) while being more than 25,000 times less effective against mammalian cells; inhibits bacterial and mitochondrial ATP synthases.

A stable, monomethoxylated resveratrol derivative that at 0.1-10 μM reduces neurotoxicity in SH-SY5Y cells induced by the parkinsonian mimetic 6-OHDA and scavenges DPPH radicals (IC₅₀ = 47.1 μM).

Immediate precursor of 4-HNE formed from ω-6 hydroperoxides such as linoleic acid and arachidonic acid.

A small molecule inhibitor of nucleophosmin dimers that can prevent cell proliferation and induce apoptosis in various cancer cell lines (IC₅₀s = 1.4-4 µM).

A potent inhibitor of HCV infection (EC₅₀ = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC₅₀ = 21.3 µM); displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without…

A dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC₅₀s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis; inhibits proliferation of multiple cancer cell lines (EC₅₀s = 11-37 nM) and prevents the growth of various human carcinoma xenografts in mice.

An inhibitor of PD-1/PD-L1 interaction.

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5

A selective β₃-adrenergic receptor antagonist.

A potent, ATP-competitive inhibitor of ROCKs including p160ROCK (Ki = 140 nM) and ROCK-II (IC50 = 800 nM); also inhibits PRK2 with an IC50 value of 600 nM.

A cell-permeable mycotoxin which binds to the barbed end of actin, reversibly inhibiting the elongation and shortening of actin filaments; blocks diverse cellular functions, including cell division, migration, phagocytosis, exocytosis, chemotaxis, and glucose transport.

An inverse agonist of LRH-1 (IC₅₀ = 3.7 µM) with maximum efficacy of 64% repression; inactive at the related SF1 transcriptional activator; alters the expression of haptoglobin, SAA1, and SAA4, induces the death of ER negative MDA-MB-231 breast cancer cells, and inhibits the StAR…

A naturally occurring metabolite of bile acid that is produced by the conjugation of cholic acid and sulfate, predominantly in the liver and gut.

An angiotensin metabolite that functions as a type 1 angiotensin II receptor agonist whereupon it can control hydroelectrolyte balance and demonstrates vasodilatory and anti-inflammatory actions in opposition to various adverse effects of angiotensin II.

A DR5 agonist (Kd= 1.2 µM; IC₅₀ = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.

8-iso PGF2β is an isomer of PGF2α with a non-enzymatic, non-cyclooxygenase origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and…

DMABA-d4 NHS ester is intended for use in combination with DMABA NHS ester (Item No. 11216) as a derivatizing reagent for PE lipids in order to facilitate MS characterization and to quantify relative changes in their abundance.

Formal Name: 4-[6-methoxy-2-[(1E)-2-(3-nitrophenyl)ethenyl]-4-oxo-3(4H)-quinazolinyl]-benzoic acid CAS Number: 1237744-13-6 Molecular Formula: C₂₄H₁₇N₃O₆

Anoninvasive, intracellular calcium indicator that is UV light-excitable; spectral properties in the presence of low calcium concentrations (excitation max = 362 nm, emission max = 512 nm) differ from those during high calcium conditions (excitation ma

8-iso PGE2 is one of several isoprostanes produced from arachidonic acid during lipid peroxidation. It is a potent renal vasoconstrictor in the rat. 8-iso PGE2 inhibits U-46619 or I-BOP-induced platelet aggregation with IC₅₀ values of 0.5 and 5 µM, respectively. When infused into…

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 microbial metabolite isolated from Streptomyces that is widely used as a selective inhibitor of the 20S proteasome.

A potent LTB4 receptor antagonist that inhibits the specific binding of [3H]-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM; inhibits the LTB4-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.

A potent inhibitor of several CDKs with selectivity for Cdk2 (IC₅₀s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.