A potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC₅₀ = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.

A stable, cell-permeable dye employed to assay cell proliferation as it is partitioned with high fidelity between daughter cells for up to eight generational divisions.

A long-acting muscarinic receptor antagonist that binds equally to human muscarinic M1, M2, and M3 receptors (Kds = 0.04, 0.02, and 0.01 nM, respectively); dissociates slowly from M1 and M3 receptors, which are located on bronchial smooth muscle and submucosal glands, and more rapidly from M2…

A potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 with IC50 values of 35 and 6 nM, respectively.

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

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 Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK, killing a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM); induces G1 phase cell-cycle arrest, dose-dependent induction of p27Kip1, apoptosis through the mitochondrial…

A hybrid molecule of indomethacin and an NO donor which combines the anti-inflammatory properties of an NSAID with the gastrointestinal protective effects of NO.

A crosslinking reagent that contains NHS ester- and maleimide-reactive groups at the opposite ends of a 4.4 Å spacer arm; used for sequential, two-stage conjugation with amine and sulfhydryl functional groups in the preparation of protein-hapten or protein-protein conjugates.

A reversible and competitive inhibitor of type IV collagen-specific MMP-2 and MMP-9 with preference towards MMP-2 (IC50 = 4 and 20 µM, respectively).

A trypsin-like protease inhibitor known to inhibit trypsin and various inflammatory proteases including plasmin, kallikrein, and thrombin; used in the treatment of chronic pancreatitis and various manifestations of fibrosis.

A cell permeable, competitive inhibitor of HIF-PH with effective concentrations in the low µM range.

An inhibitor of SREBP activation, preventing SCAP-mediated escort of either SREBP-1 or SREBP-2 to the Golgi (IC₅₀ = 5.6 µM); blocks SREBP-mediated gene expression; inhibits high glucose-induced upregulation of TGF-β in primary rat mesangial cells; reduces hepatic fat…

A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.

A natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

A proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase; inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 µM, respectively.

A nonfixable red fluorescent dye (excitation max: 586 nm; emission max: 605 nm) that can be used as a specific marker for astrocytes and an activity-dependent probe for monitoring regulated exocytosis.

A cell-permeable inhibitor of PTPs (IC₅₀s = 0.09-1.7 µM) through oxidation of the catalytic cysteine residue; inhibits redox-sensitive CYP isoforms with IC₅₀ values less than 10 µM; inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3…

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 naturally-occurring isoflavone with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC₅₀ = 80 nM) and is an effective anti-dipsotropic isoflavone.

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.

A nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (IC₅₀ = 2.7 nM); does not alter PPARγ activity.

A selective, nonpeptide AT2R antagonist (IC₅₀ = 5.6 nM vs. 100 nM for AT1R) that has been used to selectively examine the specific roles for AT1R and AT2R in hypertensive and other vascular research-related models.

An intermediate in the interconversion of glucose and galactose.

A chemiluminescent substrate of firefly luciferase which produces light upon oxidative decarboxylation in the presence of ATP.

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 potent inhibitor of kynurenine 3-hydroxylase (IC₅₀ = 37 nM), preventing the conversion of kynurenine to 3-hydroxy kynurenine; reduces ischemia-mediated neuronal damage in tissues; can be used in vivo by direct injection.

A substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.

An inhibitor of Ras-mediated signaling that inhibits the growth of PANC-1 and U87 tumor cells with IC₅₀ values of 20 and 10 µM, respectively.

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