A tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2 (both EC₅₀s = 1 nM in vitro).

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.

3-acetyl-11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense). It selectively inhibits 5-lipoxygenase (IC₅₀ = 1.5 µM) in an enzyme-directed, nonredox, and noncompetitive…

Beraprost is an analog of prostacyclin in which the unstable enol-ether has been replaced by a benzofuran ether function. This modification increases the plasma half-life from 30 seconds to several hours, and permits the compound to be taken orally. Doses of 20-100 µg in humans, given 1 to 3…

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…

A potent, selective inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM); bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model; decreases hepatic necrosis and apoptosis after orthotopic liver transplantation in rats.

A selective, cell permeable inhibitor of MLCK (IC₅₀ = 50 nM).

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.

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 synthetic version of the endogenous antidiuretic hormone arginine vasopressin; acts as an agonist at human vasopressin V1a, V1b, and V2 receptors with Ki values of 62.4, 5.8, and 23.3 nM, respectively.

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.

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

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

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (K_is = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively). It also inhibits mTOR in both mTORC1 and mTORC2 (K_is = 180 and 300 nM, respectively), as well as several common…

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.

An inactive metabolite of PGE2 formed by 15-hydroxy PGDH PGs inactive.

A substrate for β-galactosidase, the lactose repressor, the galactose-binding protein, the β-methylgalactoside transport system, and thiogalactoside transacetylase.

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 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 natural chalcone that has anti-inflammatory actions, supporting its use as a skin lightening agent, particularly for rosacea and atopic dermatitis; induces apoptosis and suppresses migration and invasion of cancer cells in vitro; has antibacterial and anti-parasitic actions.

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 selective inhibitor of PAD4 (IC₅₀ = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils.

A pan inhibitor PKD (IC₅₀s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively); blocks cell proliferation, induces apoptosis, and reduces the viability of pancreatic cancer cells both in vitro and in vivo.

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).

An analytical reference standard categorized as an oxidative quinone product of CBGA; intended for research and forensic applications

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…