An antitumor antibiotic that crosslinks double stranded DNA and is widely used as a tool to selectively inhibit DNA synthesis and mutagenensis, to stimulate genetic recombination, chromosome breakage and sister chromatid exchange, and to induce DNA repair.

A selective L-type calcium channel blocker with long-acting antihypertensive activity; relaxes depolarization-induced contractions of rabbit aorta (EC₅₀ = 1.4 nM) and reduces the rate of spontaneously beating guinea pig right atria (EC₂₅ = 0.45 nM); attenuates β-amyloid…

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC₅₀ = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type…

An inhibitor of topoisomerase I that demonstrates less toxicity than its parent compound; demonstrates strong anti-tumor activity against a wide range of experimental tumors including L1210 leukemia cells (IC₅₀ = 1.15 μM).

A competitive antagonist of muscarinic (M) receptors (Ki = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1 through M5, respectively).

NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC₅₀ = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC₅₀ = 5 nM). It can also inhibit the insulin-like growth factor 1 receptor (IC₅₀ = 0.16 µM) as well as the activity of…

A potent inhibitor of PDE5 (IC50 = 1-5 nM) that also blocks the activity of PDE11 (IC50 = 10-33 nM); IC50 values against other isoforms of PDE are in the micromolar range; pharmacokinetics are highlighted by its prolonged duration of effect.

A plant alkaloid that demonstrates cytotoxicity against leukemia P-388 cells (IC₅₀ = 2.3 µM) through a mechanism that involves stabilizing the DNA topoisomerase I-DNA complex.

A cell-permeable inhibitor of Arp2/3 complex action that inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC₅₀s = 4, 32, and 24 µM, respectively); prevents the formation of actin filament comet tails by Listeria in infected SKOV3 cells…

An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…

A natural sesquiterpene lactone that reduces growth (EC₅₀ = 3-35 μM) and induces apoptosis in assorted cancer cell lines; inhibits the activation of Akt (15 μM) in endometriotic epithelial cells and STAT3 activation in THP-1 cells (EC₅₀ = 10 μM); inhibits telomerase…

A chromogenic substrate for N-acetyl-D-galactosaminidase that generates a yellow solution upon cleavage.

D-erythro-Sphinganine is a precursor of ceramide and sphingosine as well as a substrate of sphingosine kinases, which generate sphinganine-1-phosphate. Sphinganine levels increase significantly in response to certain mycotoxins, including fumonisins, as well as in some cancers. Sphinganine can…

A reversible inhibitor of the cis-Golgi ArfGEF, GBF1 (IC₅₀ = 3.3 µM); induces rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network, preventing bidirectional transport of endocytic cargo.

A lipophilic activator of PKA and PKG (Ka = 0.05 and 0.11 μM, respectively); inhibits PDE VA, PDE III, and PDE IV with IC50 values of 0.9, 24, and 25 μM, respectively.

A potent, bioavailable JAK inhibitor with preference for JAK2 (IC₅₀ = 2 nM) over JAK1 and JAK3 (IC₅₀s = 130 and 250 nM, respectively); effective against JAK2V617F as well as JAK2 and inhibits phosphorylation of STAT5 in vivo.

A synthetic quinine derivative commonly used as an anti-malarial drug; also useful in managing SLE, rheumatoid arthritis, and other diseases; inhibits autophagy and induces autophagic cell death (IC₅₀ = 30 µM).

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 15-hydroxy PGDH (IC₅₀ = ~10 µM).

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…

An inhibitor of EGFR and VEGFR tyrosine kinases (IC₅₀s = 2, 6, 77, and 59 nM for EGFR, ErbB2, KDR, and FLT1, respectively); demonstrates antitumor activity and anti-angiogenic activity in numerous in vitro and in vivo models.

A rotenoid compound with chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis; inhibits cell growth (IC50 = 8 M), blocks PI3K/Akt signaling, suppresses COX-2 expression, and induces apoptosis of premalignant and squamous HBE cells without affecting…

An orally available inhibitor of SGLT1 and SGLT2 (IC₅₀s = 36 and 1.8 nM, respectively, for human isoforms in vitro); improves glycemic control in nonobese diabetes prone mice with type 1 diabetes and in patients with type 2 diabetes in a randomized, placebo-controlled clinical trial.

A non-steroidal androgen receptor antagonist (IC50 = 36 nM); reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

A channel blocker that acts on several TRP channels, including TRPM2, TRPM8, and TRPC6 (IC₅₀ = 1.7, 3.8, and 2.3 μM, respectively); inhibits PLA2, blocking the release of arachidonic acid when given at 50 μM.

An ERα selective agonist with a 410-fold relative binding affinity for ERα versus ERβ.

An antagonist of lipid A activation of TLR4 (IC₅₀ =1.68 μM), in a cell-based assay; significantly improves survival of mice given intraperitoneal LPS.

A natural isoflavone which is biotransformed by intestinal bacteria to give the phytoestrogens daidzein and equol, resulting in antithrombotic, antiallergic, and other salutary effects; modulates serotonin receptors when given intraperitoneally; suppresses LPS-mediated activation of NF-κB in…

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

Mn(III)TBAP is a cell-permeable SOD mimic. At a concentration of 30 µM, it decreases the doubling time of SOD-null E. coli. by 2-fold.

FeTMPyP is a synthetic porphyrin complexed with iron, which acts as a peroxynitrite decomposition catalyst. The rate constant for decomposition of peroxynitrite by FeTMPyP is 2.2 x 106 M−1s−1 with a turnover number of 360 ± 170 s−1. The predominant product (>90%) of this…