Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC₅₀ = 460 nM).

A potent cell-permeable antagonist of calmodulin that inhibits Ca2+/calmodulin cyclic nucleotide phosphodiesterase more potently than W-7 (IC₅₀ = 3.2 and 26 µM, respectively).

A 2' deoxy analog of 5-azacytidine which is incorporated into DNA and causes hypomethylation by inhibiting DNA methyltransferases in a concentration-dependent manner; useful in conditions characterized by DNA hypermethylation, as is found in myelodysplastic syndromes.

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…

C-6 ceramide is a cell-permeable analog of naturally occurring ceramides. With a longer carbon chain than C-2 ceramide, it is somewhat more hydrophobic, and may more closely mimic the effects of natural ceramides. C-6 ceramide mediates many diverse biological activities including apoptosis,…

A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.

A dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC₅₀s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively); improves glucose homeostasis in diet-induced insulin resistant mice.

An oxidizing reagent that reacts with nitric oxide to form nitric dioxide and corresponding imino nitroxides.

A fluorescent probe which is commonly used to stain DNA and chromosomes for fluorescent microscopy and flow cytometry applications; characterized by ultraviolet (max 358 nm) excitation and blue (max 461 nm) emission wavelengths.

A selective agonist of S1P3 (EC₅₀ = 72-132 nM); less effectively activates S1P1 (EC₅₀ = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.

A natural product with anti-inflammatory and cytotoxic activity; inhibits production of TNFα, IL-1β, IL-6, NO, INFγ, and expression of iNOS, and IL-12; blocks human aortic smooth muscle cell migration, inhibits MMP-9 activity, and interferes with PI3K/Akt and ERK1/2 signaling pathways.

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.

An agonist for mCAR (EC₅₀ = 20 nM) that is effective for the mouse receptor but not for human or rat CAR receptors; potently induces cytochrome P450 monooxygenases and multidrug resistance and xenobiotic efflux proteins.

A flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, antioxidant, antitumor, and neuroprotective activities at concentrations from 5-75 μM.

A potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of PRC2; blocks trimethylation of the PRC2 target H3K27 (IC₅₀ = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

An inhibitor of SRPK1 (Ki = 0.89 µM); suppresses the propagation of viruses in mammalian cells; modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.

A cell-permeable selective PDE4 inhibitor.

A broad-spectrum tetracycline antibiotic which has a particularly long half-life in serum; commonly used in the treatment of acne in older patients; also has both anti-inflammatory and neuroprotective actions.

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…

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

An HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in vitro (IC50 = 930 nM).

A small molecule inducer of adult neural stem cell differentiation; 2.5-20 µM triggers neurogenesis and blocks gliogenesis in HCN cells through a neurotransmitter-mediated calcium signal and myocyte-enhancer factor 2-dependent gene expression pathway.

A potent, reversible, ATP-competitive, thiazolidinedione inhibitor of PI3Kα (IC50 = 2 nM) and the common activating mutants of p100α (E542K, E545K, and H1047R) found in cancer; prevents proliferation in BT474 tumor xenografts and reduces MAPK signaling with twice daily dosing at 25 mg/kg.

A derivative of halopemide which potently inhibits both PLD1 (IC₅₀ = 25 nM) and PLD2 (IC₅₀ = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.

Molecular Formula: C₁₃H₁₅IN₂O₂

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

Docosatrienoic acid is a rare ω-3 fatty acid not readily detected in normal phospholipid PUFA pools. It inhibits [3H]-LTB4 binding to pig neutrophils at a concentration of 5 µM.

A potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC₅₀ = 70 nM), compared to PI3Kα (IC₅₀ = 240 nM), PI3Kβ (IC₅₀ = 1.45 μM), and PI3Kδ (IC₅₀ =1.70 μM); shows little or no activity against 38 other…