A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.

An analgesic and antipyretic compound; inhibits COX-2 activity by more than 80%, albeit at relatively high doses, while it is less effective against COX-1.

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.

An inhibitor of HDAC, including HDAC1 (IC₅₀ = 0.1-0.2 μM); induces growth suppression and cell death of certain types of cancer cells in culture.

A pyrazine derivative that is used as a flavoring agent in the food and tobacco industry; has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC₅₀ = ~1.25 mM).

A flavone that modulates xenobiotic metabolism; antagonizes AhR at nanomolar concentrations, although it agonizes AhR at higher concentrations (10 µM); inhibits CYP19, CYP1A1, CYP1A2, and CYP1B1 (IC₅₀s = 500, 60, 6, and 5 nM, respectively), whereas it activates CYP3A4 (Kd = 7.4 µM).

A natural oxidative metabolic product of the mycotoxin aflatoxin B2.

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 cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC₅₀ values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS. The IC₅₀ values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively. Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.

Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of sPLA2. The IC₅₀ value for thioetheramide-PC is 2 µM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, thioetheramide-PC…

A major metabolite of sulforaphane that has been shown induce ARE-driven gene expression with roughly 8-fold less potency than sulforaphane.

(±)11-HDHA is an autoxidation product of DHA in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. DHA is metabolized to 11(S)-HDHA by human platelets and canine retina. In addition to 11(S)-HDHA, 14(S)-HDHA is also produced by platelets.…

An inhibitor of RIP1 kinase that prevents the death of TNF-α-treated FADD-deficient Jurkat cells with an EC50 value of 490 nM.

Caffeic acid is an inhibitor of 5-LO with an IC₅₀ value of 3.7-72 µM and 12-LO with an IC₅₀ value of 5.1-30 µM.

An analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.

(±)15-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid. The biological activity of (±)15-HETE is similar to that of its constituent enantiomers (Item Nos. 34720 and 34710).

A cyclic hexapeptide mycotoxin that binds β-tubulin in a vinca domain; blocks microtubule growth, modulates the dynamics of microtubules, and interferes with mitosis.

A potential metabolite of 8-iso PGF2β via the 15-hydroxy PGDH pathway.

Enzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings…

A glycopeptide antibiotic identified for its utility in the treatment of gram-positive bacteria, including penicillin-resistant staphylococci; binds to bacterial cell wall precursors, interfering with their synthesis.

A selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC₅₀ = 26.4 nM; Ki = 5 nM).

A reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC₅₀ = 26 nM).

Formal Name: N-?[[(4-?aminophenyl)?amino]?thioxomethyl]?-?4-?(1,?1-?dimethylethyl)?-benzamide CAS Number: 1011301-27-1 Molecular Formula: C₁₈H₂₁N₃OS

A polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM); acts as a non-specific competitor of…

A thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides.

A potent, competitive inhibitor of HMG-CoA reductase (Ki = 0.12 nM).

A cardiotonic steroid that inhibits theNa+/K+-ATPase transporter (Kds = 42, 45, and 40 nM for the α1, α2, and α3 subunits, respectively); inhibits SRC-1 and SRC-3 at doses as low as 5 nM, promotes the degradation of SRC-3 protein, and inhibits cancer cell growth both in vitro and…

A selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding (IC50 = 31 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation, which reduces cell viability and induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).

A first generation tyrosine kinase inhibitor that is used in the treatment of CML, GIST, and other cancers; selectively targets certain tyrosine kinases, including c-ABL, PDGFR, KIT, and the oncoprotein BCR-ABL.

A potent and selective G9a HMTase inhibitor (IC50 = 6 nM; Ki = 63 pM); more than 40,000-fold selective for G9a over SET7/9, SET8, PRMT3, and JMJD2E.