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An analog of the PKC-activating second messengers collectively called DAG; equipotent to 1,2-dioctanoyl-sn-glycerol in induction of the acrosome reaction in human sperm.
A potent, selective inhibitor of HDAC6 (IC50 = 5.02 nM); dose-dependently induces hyperacetylation of α-tubulin in B16 murine melanoma cells without elevating histone H3 acetylation.
A selective inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50 = 70 nM), a serine hydrolase that catalyzes the hydrolysis of 2-AG.
A potent inhibitor of CENP-E (Ki = 3.2 nM); causes mitotic cell cycle delay, leading to apoptosis in various cancer cell lines; induces apoptosis in cancer cells in mice bearing xenografts of COLO 205 cells.
An antiparasitic drug that, in different preparations, is effective against trypanosomes; orally available and rapidly metabolized to two active metabolites.
An epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo; its effects of remain to be determined.
A small molecule inducer of definitive endoderm from embryonic stem cells; induces the differentiation of Sox17+/FoxA2+-expressing pancreatic progenitors from human and mouse embryonic stems cells (EC50 = 125.5 nM in vitro) by activating the TGF-β signaling pathway.
A first generation antihistamine which is a potent antagonist of the human H1 receptor (Ki = 11.7 nM); readily crosses the blood-brain barrier and produces diverse cognitive and psychomotor effects; also antagonizes muscarinic cholinergic receptors (Ki = 100 to 260 nM for M1 through M5).
GSH is a tripeptide (γ-glutamylcysteinylglycine) widely distributed in both plants and animals. GSH serves as a nucleophilic co-substrate to glutathione transferases in the detoxification of xenobiotics and is an essential electron donor to glutathione peroxidases in the reduction of...
Iguratimod is a disease-modifying antirheumatic drug (DMARD) and COX-2 inhibitor (IC50 = 7.7 µg/ml).{66044} It is selective for COX-2 over COX-1 (IC50 = >300 µg/ml) but also inhibits the tautomerase activity of macrophage migration inhibitory factor (MIF; IC50 = 6.81 µM).{66044,66045} Iguratimod...
JW 55 is an inhibitor of the PARP domain of tankyrases (TNKS) 1 and 2 (IC50s = 1.9 and 0.83 µM, respectively). By inhibiting TNKS1/2, JW 55 stabilizes Axin2 and increases degradation of β-catenin, inhibiting the β-catenin signaling pathway (IC50 = 470 nM). It...
A potent, reversible, and cell permeable proteasome inhibitor; a more effective inhibitor of chymotrypsin-like, trypsin-like, and peptidylglutamyl peptide hydrolyzing proteasome activities compared to (S)-MG132 (IC50s = 0.22 versus 0.89 µM (ChTL); 34.4 versus 104.43 µM (TL);...
An Hsp90 inhibitor with an IC50 value of 47 nM; induces the expression of HSP27 and Hsp72 while reducing the client proteins c-Raf, B-Raf, survivin, and PRMT5, causing cell cycle arrest and apoptosis.
A reversible, ATP-competitive inhibitor of CK1δ and CK1? (IC50 = ~1 µM for both), as well as CK1α (IC50 = 16 µM); at 1 µM, inhibits cytokinesis in primary mouse embryo fibroblasts; used to elucidate the role of CK1 in cells and in whole organisms.
A potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively); active in vivo and often used to evaluate the actions of adrenergic receptor agonists.
The first identified agonist for OPRM1-OPRD1 heterodimerization (EC50 = 403 nM) that demonstrates selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor (EC50s = 14.9, 1.1, and >40 μM, respectively).
A potent, orally bioavailable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki death proteins, like Bim, leading to apoptosis; induces apoptosis in cancer cell lines expressing mutants of β-catenin 1.
A form of stearic acid that contains a DOXYL group, creating a hydrophobic spin label.
A selective estrogen receptor (ER) modulator used as adjuvant therapy for estrogen-dependent breast cancer; increases ER activity in bone, uterus, and the cardiovasculature system as it decreases ER activity in breast tissues; metabolized by CYP450 enzymes to active metabolites; alters cholesterol...
A quinoxaline-type tyrphostin that acts as a potent and selective inhibitor of PDGF receptor kinase in vitro and in Swiss 3T3 cells (IC50s range from 0.3-1 µM); inhibits PDGF-stimulated DNA synthesis (IC50 = 2.5 µM) without affecting activity of the EGF receptor.
CAS Number: 851881-60-2 Molecular Formula: C20H17F2N3O2 Formula Weight: 369.4
Ins(4,5)P2 is a metabolite of Ins(1,4,5)P3 that lacks a phosphate at the 1' position. Ins(4,5)P2 formation has been reported as an intermediate in the metabolism Ins(1,4,5)P3 in GH3 pituitary cells.
A potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM); produces prolonged elevation of AEA in the brain and plasma in rats after treatment; significantly and persistently reduces inflammatory pain in rats through a CB receptor-dependent mechanism.
Oleyloxyethyl phosphorylcholine is an inhibitor of PLA2 with an IC50 value of 6.2 µM for porcine pancreatic PLA2.