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.

Epoxyeicosatrienoic acid (EpETrE; EET) metabolites of arachidonic acid such as 11(12)-EET and 14(15)-EET have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EETs to the corresponding dihydroxy…

An inhibitor of the initiation of translation that blocks the interaction of eIF4G with eIF4E (KD = 25 μM); prevents the expression of oncogenic proteins in mammalian cancer cells, leading to apoptosis; blocks translation in some viruses that do not require eIF4E or a cap structure for initiation.

A potent, reversible, and cell permeable proteasome inhibitor; a more effective inhibitor of chymotrypsin-like, trypsin-like, and peptidylglutamyl peptide hydrolyzing proteasome activities compared to (S)-MG132 (IC₅₀s = 0.22 versus 0.89 µM (ChTL); 34.4 versus 104.43 µM (TL);…

CAS Number: 444932-31-4 Molecular Formula: C₂₀H₁₉N₃O₄ Formula Weight: 365.4

A potent, cell-permeable inhibitor of all JAK isoforms (IC50 = 6.1, 12, and 8.0 nM for JAK1, JAK2, and JAK3, respectively); useful in ameliorating inflammatory or autoimmune components of a host of diseases.

An antifungal agent that acts as an inverse agonist to disrupt Hh signaling (IC₅₀ = 0.8 μM); treatment at 100 mg/kg twice per day has been shown to suppress the growth of medulloblastomas from a Ptch+/-p53-/- mouse allograft model.

A small molecule pan activator of Ras-related GTPases, activating cdc42, Ras, and Rac1 with EC₅₀ values of 102, 109, and 151 nM, respectively.

An endocannabinoid analog that does not bind to CB1, CB2, or TRPV1; at 5 mg/kg antagonizes the hypotensive effects of a 10 mg/kg IV bolus of abnormal cannabidiol (Abn-CBD) in an anesthetized rat blood pressure model; relaxes isolated rat mesenteric arteries and abdominal aorta, and increases the…

A thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.

CAS Number: 1000998-59-3 Molecular Formula: C₂₂H₂₁ClN₂O₆ Formula Weight: 444.9

A selective inhibitor of PFKFB3 (IC₅₀ = 207 nM); rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.

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 potent cell-permeable inhibitor of ERK1 and ERK2 (Ki = 310 and 140 nM, respectively); much less effective against p38α (IC₅₀ = 10 µM) and does not inhibit a range of other serine/threonine or tyrosine kinases; blocks ERK-mediated signaling from TGF-β to AP-1…

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 cell-permeable selective PDE4 inhibitor.

A cell-permeable compound that maintains long-term mouse ESC pluripotency; allows ESCs to form embryoid bodies that continue to express markers of pluripotency when used at 4 µg/ml with Wnt3a; blocks the interaction of Nkd with a subunit of PP2A.

A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

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…

An allosteric, reversible inhibitor of PAR1 on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC₅₀ value of 0.26 µM; also blocks platelet activation induced by thrombin but not by PMA, U-46619, or collagen.

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

An immunosuppressant used to prevent transplant rejection; potent inhibitor of IL-2 activation of lymphocytes (IC50 = 5 pM); specifically interacts with FKBP12 to form a complex which inhibits mTORC1.

An unsaturated fatty acid found in royal jelly produced from honeybees; demonstrates longevity-promoting effects in C. elegans, down regulates matrix metalloproteinases (MMPs) in rheumatoid arthritis, inhibits VEGF-induced angiogenesis in HUVECs, facilitates differentiation of neurons from neural…

An irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases; at 20-200 µM arrests human epidermoid carcinoma A431 cells at mitotic metaphase; inhibits protease-resistant protein accumulation in scrapie-infected neuroblastoma cells (IC₅₀ = 0.5 µM).

A benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.

An intermediate in several metabolic pathways, including glycolysis and gluconeogenesis.

Molecular Formula: C₁₃H₉ClFNO₂

A potent inhibitor of calcium release-activated calcium channels in lymphocytes (IC₅₀ = 100 nM); also inhibits lung IL-4 and CysLT generation in animal models of asthma.

An inhibitor of SRE activation in PC3 cells (IC₅₀ = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC₅₀ = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay.

A small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.

A fatty acid amide from T. titanicus that at 0.1 μg/ml protects against ER stress-dependent cell death in Neuro2a cells induced by tunicamycin.

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.