A selective, irreversible inhibitor of BTK (IC₅₀ = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481; inhibits osteoclast function and reduces osteoclast-stimulated proliferation of multiple myeloma cells in animal models of…

A nutlin-3 analog; inhibits the growth of HCT116 cells at high concentrations (IC50 = ~8 µM); promotes the growth of HCT116 cells ~40% at concentrations between 5-100 nM.

A natural nitroaryl-substituted polyketide that exhibits antitumor, antifungal, and insecticidal activities; non-competitive inhibitor NADH:ubiquinone oxidoreductase of bovine heart, N. crassa, and E. coli (IC₅₀s = 0.07, 0.08, and 22 nmol/mg protein, respectively).

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

11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.

A steroidal saponin that displays cytotoxicity against a range of cancer cells in vitro, including leukemia, colon cancer, and prostate cancer cells (GI50 ≤ 2 µM).

A selective inhibitor of 15-hydroxy PGDH (IC₅₀ = ~10 µM).

A grasshopper neuropeptide from a family of arthropod hormones and neuroregulators, found in Locusta migratoria.

Hexanolamino PAF C-16 is a PAF analog with mixed PAF receptor agonist/antagonist properties. In human monocyte-derived macrophages, it is an antagonist which inhibits the production of reactive oxygen species in response to PAF C-16. On the other hand, in rabbit platelets and guinea pig…

A small molecule inhibitor of human cytomegalovirus viral replication (EC₅₀ = ~5 nM with a selectivity index >15,000) that targets viral DNA cleavage and packaging.

A synthetic analog of natural PtdIns containing C6:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.

A tumor-promoting teleocidin compound that activates PKC (Ki = 3.4 nM and 1 μM for PKCη and PKCγ, respectively); induces differentiation of human embryonic stem cells into pancreatic progenitors.

8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the…

An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

Specifically inhibits the histone acetyltransferase Gcn5 (IC₅₀ = 100 μM) and can inhibit pre-RNA splicing with an IC₅₀ value of 0.5 mM.

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity. At a 25 µM concentration, PGA2 blocks the cell…

PGB1 is a non-enzymatic dehydration product of PGE1 resulting from treatment with strong base. Oligomers of PGB1 are known to exhibit antioxidant and ionophoric activity.

A specific and potent inhibitor of MPC carrier activity; potently inhibits pyruvate-dependent oxygen consumption by rat heart mitochondria (IC₅₀ = 50 nM).

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A hydrophobic diterpene ester that rapidly induces cell death in proliferating keratinocytes through plasma membrane and mitochondrial disruption; causes inflammation due, at least in part, to activation of PKC, leading to antibody-dependent cellular cytotoxicity.

A homolog of LOEA, characterized by the addition of an (S)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.

A potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50 = 2, 8, 20, 26 nM for DNA-PK, p110α, mTORC1, and PI3-KC2β, respectively).

A dipeptide boronic acid derivative that reversibly inhibits the 20S proteasome (Ki = 0.6 nM); drives cell cycle arrest and apoptosis in cancer cell lines and has applications in multiple myeloma and certain lymphomas, as well as other types of cancer.

A selective inhibitor of the Src family of non-receptor tyrosine kinases (IC₅₀s = 2 and 6 nM for Lck and Src, respectively); used in combination with PD 0325901, CHIR99021, and SB-590885 to support self-renewal of naïve human embryonic stem cells.

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

An analog of geldanamycin which has potent in vivo activity and reduced toxicity; has diverse anti-tumor actions; promotes the degradation of HER2 and induces growth arrest and apoptosis in breast cancer cells overexpressing HER2 (IC50 = 4-72 nM).

Bicyclo PGE2 is a stable, base-catalyzed transformation product of 13,14-dihydro-15-keto PGE2. 13,14-dihydro-15-keto PGE2 itself is a metabolite of PGE2 found in human plasma at a median level of 20-25 pg/ml. Due to the inherent instability of 13,14-dihydro-15-keto PGE2, it is advisable to quantify…

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

A phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of…