An imidazole that potently antagonizes the α2-adrenoceptor (Ki = 1.6 nM); shows selectivity over the α1-adrenoceptor (Ki = 13,300 nM) and is a poor antagonist at a wide variety of other receptors and channels.

A cyanoquinoline that irreversibly inhibits the receptor tyrosine kinases EGFR (IC₅₀ = 39 nM) and HER2 (IC₅₀ = 1.2 μM); disrupts Akt and MAPK pathways, inducing apoptosis and suppressing the growth of tumor cell lines.

A selective PI3K inhibitor with an IC₅₀ value of 1.4 µM.

A third generation inhibitor of p38 MAP kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively); inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.

An imidazotetrazine that is converted to a compound capable of alkylating DNA, thus interfering with DNA replication and leading to cytotoxicity in proliferating cells; rapidly and completely absorbed from the gastrointestinal tract after oral administration and readily crosses the blood-brain barrier.

A less potent IWP-2 derivative that has been used to determine which structural features of IWP-2 are essential for impairing Wnt/ β-catenin pathway activity.

A selective SIP1 agonist (EC₅₀ = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC₅₀ = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.

An agonist of GPR81 (EC₅₀ = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.

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 RARβ agonist, RARα/γ antagonist that inhibit the proliferation of normal breast cells via the induction of TGF-β activity, causing G1 arrest; used to trigger the differentiation of mouse embryonic stem cells.

Spermine NONOate is a NO donor. It spontaneously dissociates in a pH-dependent, first-order process with a half-life of 39 minutes and 230 minutes at 37°C and 22-25°C, respectively, (pH 7.4) to liberate 2 moles of NO per mole of parent compound.

An estrogen metabolite that acts as a substrate of MRP2 (Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

An aminopyridazine derivative that acts as a GABAA receptor antagonist that can be used as an intermediate in the synthesis of SR 95531.

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

An inverse agonist of LRH-1 (IC₅₀ = 3.7 µM) with maximum efficacy of 64% repression; inactive at the related SF1 transcriptional activator; alters the expression of haptoglobin, SAA1, and SAA4, induces the death of ER negative MDA-MB-231 breast cancer cells, and inhibits the StAR…

A selective inhibitor of ASK1 (IC₅₀ = 3 μM; Ki = 500 nM); promotes survival of induced pluripotent stem cell populations and protects neurons from reactive oxygen species-induced apoptosis in a model of ischemia.

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.

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.

A cell permeable analog of cAMP that activates PKA with a Ka value of 0.05 μM; more stable to hydrolysis and has increased membrane permeability compared to unmodified cAMP.

A major component of the root of P. suffruiticosa that at 30 µM inhibits the growth of human hepatocellular carcinoma SK-HEP-1 cells by causing cell cycle arrest and suppressing the activation of NF-κB.

A selective inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to AA; orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.

CAS Number: 1000998-59-3 Molecular Formula: C₂₂H₂₁ClN₂O₆ Formula Weight: 444.9

An inhibitor of EGF receptor kinase with an IC50 value of 1 µM in HT-22 cells.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

An α-hydroxy acid, overproduced in 2-hydroxyglutaric aciduria; mutations in IDH1 and IDH2 cause these enzymes to convert isocitrate to 2-hydroxyglutarate; competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases.

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 dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC₅₀s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis; inhibits proliferation of multiple cancer cell lines (EC₅₀s = 11-37 nM) and prevents the growth of various human carcinoma xenografts in mice.

An inhibitor of ALK5, ALK4, and ALK7 (IC₅₀s = 12, 45, and 7.5 nM, respectively); blocks the phosphorylation of Smad2/3 and inhibits TGF-β-induced epithelial-to-mesenchymal transition; used to reprogram fibroblasts into alternative lineages.

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.

A derivative of halopemide which potently inhibits both PLD1 (IC₅₀ = 25 nM) and PLD2 (IC₅₀ = 20 nM); prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis.

The major active lignin in fruits of the burdock plant A. lappa that demonstrates potent antiviral, anti-inflammatory, and antiproliferative activity.