An analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM, respectively); significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2.

A verapamil derivative that dose-dependently blocks calcium uptake via Na+/Ca2+ exchange in diverse types of cells (Ki = 28 µM); also prevents calcium release from mitochondria induced by Ruthenium Red but not by uncouplers, respiratory inhibitors, or a chelating agent.

A potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM); avidly binds the serotonin receptors 5-HT1A and 5-HT1D (Ki = 12.9 and 10.7 nM, respectively), as well as α and β adrenoreceptors.

A second generation analog of amiloride that inhibits TRPP3-mediated Ca2+-activated (IC₅₀ = 0.14 μM) and ENaC (IC₅₀ = 10 nM); inhibits active sodium transport of human and ovine bronchial epithelial cells (IC₅₀s = 75 and 116 nM, respectively).

A natural anthocyanidin.

A fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.

An inhibitor of STAT3 transcription factor activation, dimerization, and gene transcription; suppresses IL-6-induced phosphorylation of STAT3 in T cells (IC₅₀ = 38 μM) and is protective against angiotensin II-induced vascular dysfunction.

A fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

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 TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

Keystone essential fatty acid that is converted by COX, LO, and epoxygenase enzymes into more than 150 potent metabolites in species ranging from fungi to plants to mammals.

A metabolite of dimetridazole, the nitroimidazole-based antibacterial and anticoccidial agent suspected to be carcinogenic and mutagenic to humans.

The main saponin constituent of C. asiatica that has been shown to improve wound healing including increasing collagen synthesis and elevating antioxidant levels in various normal and diabetic wound models.

The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR family of proteins, is coordinated by synthesis of diffusible acylhomoserine lactone (AHL) molecules. C6-HSL is a small diffusible signaling molecule involved in quorum sensing, controlling gene…

Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1)…

A selective slow off-rate inhibitor of Raf kinases (IC₅₀s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively); shows significant antiproliferative activity against mutated BRAF or mutated NRAS cancer cell lines and xenograft models.

An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…

AMT is a potent, relatively selective inhibitor of iNOS with a Ki of 4.2 nM in mouse macrophages. It inhibits other isoforms of NOS, but at higher concentrations; the IC₅₀ values for rat nNOS and bovine eNOS are 34 and 150 nM, respectively.

PGB1 is a non-enzymatic dehydration product of PGE1 resulting from treatment with strong base. Oligomers of PGB1 are known to exhibit antioxidant and ionophoric activity.

An intermediate in the interconversion of glucose and galactose.

A selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 µM.

A potent and selective CB1 receptor inverse agonist (Ki = 243 nM; EC50 = 195 nM); a 10 µM concentration results in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and CB2 receptors, respectively.

A post-synaptic α1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia; displays high-affinity with non-selectivity for the three known human α1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for α1A, α1B,…

3-Tert-butyl-5-methoxy-catechol exhibits anticancer activity, inhibiting proliferation of leukemia cells. This compound may also induce cellular differentiation in vitro.

A potent and selective AhR antagonist (Ki = 1.2 nM).

A plant lectin that selectively cross-links cell-surface glycoproteins and affects the initiation of cell agglutination, mitogenesis, and apoptosis; widely used in affinity chromatography purifications of various glycoproteins and cellular structures; also used to induce liver injury in…

An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.

A high-affinity ligand for retinoid X receptors (RXRs)(EC50 = 28, 25, and 20 nM for RXRα, β, and γ, respectively); inhibits cell cycle progression, induces apoptosis, and blocks angiogenesis and metastasis; stimulates clearance of soluble Aβ, reduces plaque area, and reverses…

A highly potent, reversible inhibitor of the EGFR (Ki = 5.2 pM; IC₅₀ = 29 pM); rapidly suppresses autophosphorylation of EGFR in ?broblasts and human epidermoid carcinoma cells.

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC₅₀ = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type…

A cell-permeable, cGMP analog that activates cGMP-dependent protein kinase.