Phytochemical from cruciferous vegetables that demonstrates anticancer and chemopreventative effects (10-30 µM) involving the induction of Phase 2 enzymes, promotion of apoptosis, induction of cell cycle arrest, inhibition of cell proliferation, and inhibition of histone deacetylases and DNA…

Inhibits CKII (IC50 range of 4-10 µM), Cdk7 (IC50 = ~20 µM), Cdk8 (IC50 = ~20 µM), and Cdk9 (IC50 = 3 µM); inhibits elongation during RNA polymerase II transcription; triggers p53-dependent apoptosis of human colon adenocarcinoma cells; inhibits trans-activated transcription…

A thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.

A dual inhibitor of DNA-PK and PI3K.

An antimycotic prodrug that is converted by cytosine deaminase to 5-fluorouracil, a cytotoxic drug that inhibits viral infections and has cytotoxic effects on cancer cells.

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

13(S)-HpODE is produced by the oxidation of linoleic acid by LO-1 in many plants including soybean, flaxseed, apples, and tea leaves, and by 15-LO in mammals. In plants, 13(S)-HpODE is the preferred substrate for the garlic bulb divinyl ether synthase. In mammalian tissues, 13(S)-HpODE is generally…

A selective, cell-permeable EZH2 inhibitor (IC₅₀ = 2 nM) that has been shown to inhibit H3K27methylation in MCF10A cells with an IC₅₀ value of 124 nM.

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

An active metabolite of proguanil, produced by CYP2C19; an inhibitor of dihydrofolate reductase (Kis = 0.3 and 1.5 nM for Plasmodium and human forms, respectively).

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3

An anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.

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)…

An aminonucleoside antibiotic that blocks protein synthesis in both prokaryotes and eukaryotes by causing premature termination of nascent polypeptide chains; used in assays for peptide-bond formation and elongation and also often used as selective agent in cell culture systems.

A selective inhibitor of ABHD6 (IC₅₀ = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ; used both as a probe to study ABHD6 and as a negative control for studies of DAGLβ.

A potent inhibitor of LSD1 (IC₅₀ = 0.02 µM) that less effectively inhibits MAO-A and MAO-B (IC₅₀s = 1.38 and 0.72 µM); blocks the expression of IE genes of HSV and hCMV in mammalian cells; represses HSV primary infection in mice and blocks HSV reactivation from…

Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin M1 is the hydroxylated metabolite of aflatoxin B1; it inhibits DNA synthesis and induces cell cycle arrest.

A glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively); reversibly inhibits γ-glutamyl transpeptidase.

A broad-spectrum, indole-based antiviral compound that blocks viral fusion with target membranes, prohibiting viral entry into cells; effective against numerous viruses, including influenza A, B, and C and hepatitis B and C (IC₅₀s range from 3-12.5 µg/ml).

Bromosporine is an inhibitor of BET bromodomains (BRDs) BRD2, BRD4, BRD9, and CECR2; it may exhibit anticancer potential.

An analog of 1,24-dihydroxy vitamin D3 which, when used in a 4 μg/g ointment, suppresses psoriasis; inhibits the growth of both normal and psoriatic human keratinocytes (IC50 ~ 10 nM) via the vitamin D receptor; suppresses the production of RANTES and IL-8 by human dermal fibroblasts.

An inhibitor of SRE activation in PC3 cells (IC₅₀ = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM; inhibits PC3 cell migration (IC₅₀ = 4.2 μM), as determined by a scratch wound assay; causes no cytotoxicity when evaluated by WST-1 assay.

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC₅₀ = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC₅₀ = 0.6 µM); shows good in vivo potency and duration of action.

An inactive control for the selective PAD4 inhibitors, GSK484 and GSK199 (IC₅₀s >100 µM).

A flavonoid compound that acts as a powerful antioxidant; inhibits TBARS formation with an IC50 value of 6.34 µM; blocks oxLDL uptake by U937-derived macrophages at 20 µM; demonstrates potent chemopreventative potential by binding JAK1/STAT3 to inhibit neoplastic transformation of…

A cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively; does not alter HDAC1 activity.

This product is used to measure apoptosis in vitro.

A small diffusible signaling molecule produced by wild-type E. carotovora strain SCC 3193 involved in quorum sensing, controlling gene expression, and affecting cellular metabolism.

A toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.

A potent inhibitor of autotaxin (IC50 = 2.8 nM in an in vitro enzyme assay); at 30 mg/kg, reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).

A synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist; inhibits androstenediol-dependent LNCaP cell tumor growth both in vitro (IC₅₀ = 6 nM) and in vivo.

n-Triacontanol is a plant growth regulator found in the plant cuticle waxes and in beeswax as the palmitate ester. n-Triacontanol has been reported to have growth enhancing properties when applied to the leaves of growing plants.