A mycotoxin produced from F. moniliforme that functions as an inhibitor of ceramide synthase (sphingosine N-acyltransferase).

A potent and selective agonist for both LXRα and LXRβ (EC₅₀ = 50 nM).

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.

A potent, selective inhibitor of ATR (IC₅₀ = 5 nM); inhibits the growth of LoVo colorectal adenocarcinoma cells in vitro and significantly reduces the growth of LoVo xenografts in mice.

Mn(III)TMPyP is a cell-permeable SOD mimic and peroxynitrite decomposition catalyst. The rate constants for superoxide dismutation and peroxynitrite decomposition are 3.9 x 107 M−1s−1 and ~2 x 106 M−1s−1, respectively.

An orally bioavailable, specific, broad spectrum JAK inhibitor (IC₅₀s = 10, 18, 99, and 84 nM for JAK1, JAK2, JAK3, and JAK4, respectively); blocks cell-based JAK signaling induced by IL-2, IL-4, IL-6, IL-13, or IL-31 with IC₅₀ values ranging from 36 to 249 nM.

Clodronate is a first-generation non-nitrogen-containing bisphosphonate that is used clinically for its anti-resorptive activity. Clodronate generates formation of a non-hydrolysable ß-? ATP analog that inhibits mitochondrial ADP/ATP translocase and prevents mitochondrial oxygen consumption…

A synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1; phosphorylated by Cdk5 with a Km value of 5 µM.

A mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…

A synthetic progestin that acts as a prodrug to norelgestromin and levonorgestrel; selectively binds the progesterone receptor and is androgenically neutral.

A thiophene carboximide derivative proposed to inhibit IKK2; likely to be useful in the treatment of inflammatory diseases and cancer.

An orally available, selective inhibitor of both free and prothrombinase-bound factor Xa (Ki = 0.8 nM); effective anticoagulant in both preclinical and clinical models of venous and arterial thrombosis.

A potent inhibitor of specific IAPs that binds baculovirus IAP repeat (BIR) domains (Kis = 28, 14, 17, and 43 nM for XIAP BIR3, NL-IAP BIR, BIRC2 (c-IAP1) BIR3, and BIRC3 (c-IAP2) BIR3, respectively); induces activation of caspases, decreasing the viability of cancer cells without affecting normal cells.

Can be formed by the dimerization of two molecules of α-trans-cinnamic acid; significantly blocks inflammatory pain while having little effect on neurogenic pain, as indicated by the formalin test in mice.

The CysLTs, LTC4 and LTD4, are potent mediators of asthma and hypersensitivity. They induce bronchoconstriction, increase microvascular permeability, and are vasoconstrictors of coronary arteries. Their biological effects are transduced by a pair of GPCRs, CysLT1 and CysLT2. Montelukast (sodium…

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 prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.

N-Oleoyl glycine is a putative substrate for peptidyl glycine α-amidating enzyme in the biosynthesis of oleoyl amide.

A potent, selective, and cell-permeable inhibitor of Raf-1 (IC₅₀ = 9 nM); blocks phosphorylation of ERK1/2 by 90% in cells stimulated with EGF when given at 5 µM; shows more than 100-fold selectivity for Raf-1 versus several related kinases.

A selective, nonpeptide antagonist of the vasopressin V1a receptor (Ki = 1.1-6.3 nM in human); inhibits arginine vasopressin-induced human platelet aggregation with an IC₅₀ value of 3.7 nM.

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…

A selective SIP1 agonist (EC₅₀ = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC₅₀ = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.

A potent, orally available inhibitor of CDKs, blocking the Cdk9 activity of P-TEFb (IC50 = 8 nM) as well as all other CDK isoforms (IC50 = 100-300 nM); less effectively inhibits EGFR and PKA (IC50 = 21 and 122 μM, respectively); has potential applications in cancer therapy.

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…

A selective inhibitor of TAF1 bromodomain 2 (Kd = 1.8 µM; IC₅₀ = 0.9 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

A homoserine lactone member that possesses a rare odd-numbered acyl carbon chain and may be a minor quorum-sensing signaling molecule in P. aeruginosa strains.

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.

11-deoxy PGF1α is a synthetic analog of PGF1α. In whole animal studies, a dose of 32 mg/kg inhibited gastric acid secretion by 35%. 11-deoxy PGF1α is also known to cause rat uterine contractions at a dose 0.3 times that of PGF1α. It also exhibits vasopressor and…

An aminooxy analog of ornithine that irreversibly inhibits aminotransferases, including ornithine aminotransferase (Ki = 2 µM); cytotoxic to a range of organisms.

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.

(+)-15(R)-Fluprostenol isopropyl ester is a prodrug (Travoprost) which is converted by esterase enzymatic activity in the cornea to yield the corresponding free acid. The free acid, (+)-15(R)-fluprostenol, is a potent FP receptor agonist. The 15(R)-epimers of most PGs are about 100 times less…

An antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC₅₀ values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways.