An indole-based, time-dependent inhibitor of Icmt (IC₅₀ = i = 0.14 µM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells.

A chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21); potent in cells, with an IC₅₀ value of 250 nM.

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

A major oxysterol formed from cholesterol by CYP3A4/5; used as a marker for CYP3A4/5 activity.

An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.

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, potent, and cell-permeable inhibitor of mTOR (IC₅₀ = 4.3 nM) which blocks signaling through both mTORC1 and mTORC2; induces G1 cell cycle arrest in both rapamycin-sensitive and rapamycin-resistant cancer cell lines and reduces tumor growth in nude mice with PTEN-null tumors.

A natural adenosine analog that prevents IRE1α-induced mRNA cleavage (IC₅₀ = 80 nM) and inhibits constitutive activation of XBP1 in multiple myeloma cell lines; used to study IRE1α action in the endoplasmic reticulum stress response.

A selective non-peptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC₅₀ = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor; effectively activates µ/δ receptor heteromers (EC₅₀ = 52.8 nM) but not κ/δ or μ/κ heteromers.

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

A non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

PGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC₅₀ of PGE1 for the inhibition of ADP-induced human platelet…

An inactive analog of U-73122; can be used as a negative control.

A small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism in bacteria; activates NF-κβ in RAW 264.7 macrophages, increasing the expression of TNF-α, IL-1β, and IL-8; alters cell cycling and…

A non-cholestatic regioisomer of E217G that acts as a substrate for MRP2, competing with E217G for MRP2-mediated transport (IC₅₀ = 14.2 µM).

A reactive disulfide-containing, fluorescent probe designed to detect H2S in biological samples and cells.

A reversible, competitive thrombin inhibitor (Ki = 5 nM) that shows selectivity for thrombin over other clotting pathway enzymes.

A synthetic analog of PGF2β.

CZC-54252 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀s = 1.28 and 1.85 nM for wild-type and G2019S mutant forms of LRRK2, respectively). It has been shown to protect against neuronal injury induced by Parkinson’s disease-related LRRK2-G2019S mutant activity in…

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 5 nM), p59fynT (IC₅₀ = 6 nM), Hck (IC₅₀ = 20 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 non-ionic, water-soluble X-ray contrast agent for intravascular administration; can cause acute kidney injury and is used in animal models of contrast-induced nephropathy.

A selective inhibitor of mutant B-RafV600E (IC₅₀ = 0.8 nM), with 4- and 6-fold reduced potency against wild type B-Raf and c-Raf (IC₅₀s = 3.2 and 5 nM, respectively); studied in clinical trials in patients with B-RafV600E metastatic melanoma and other solid tumors.

A natural kavalactone that enhances the binding of bicuculline methochloride at the GABAA receptor at 0.1 µM.

A selective, cell permeable inhibitor of CaMKII (IC₅₀ = 900 nM).

A cell permeable analog of cAMP that activates PKA with a Ka value of 0.05 μM; more stable to hydrolysis and has increased membrane permeability compared to unmodified cAMP.

One of the phenolic antioxidants present in extracts of rosemary; inhibits the formation of tumors derived using irritants such as TPA and DMBA.

8-iso PGF2β is an isomer of PGF2α with a non-enzymatic, non-cyclooxygenase origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and…

A non-reducing inhibitor of 5-LO that shows selectivity for 5-LO over 12-LO or COX; inhibits topoisomerase II activity and arrests cell cycling or induces apoptosis in cancer cells.

8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.

Inhibits several isoforms of protein kinase C (PKC; IC₅₀ = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.