An internal standard for the quantification of DHA by GC- or LC-MS.

A selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay (pA2 = 8.1); demonstrates analgesic activity in a mouse writhing assay (ED50 = 0.9 mg/kg); potentiates the vasorelaxation of human pulmonary vein induced by PGE2 (EC50 = 7.75 µM).

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 competitive inhibitor of human lysosomal β-glucosidase (Ki = 0.016-0.025 µM; IC₅₀ = 0.06 µM) that interacts with the catalytic pocket of β-glucosidase, acting as a chemical chaperone that stabilizes and/or promotes the folding of the enzyme; increases lysosomal…

CAS Number: 745046-84-8 Synonyms: Ivachtin Molecular Formula: C₂₀H₂₁N₃O₇S

An inhibitor of class III receptor tyrosine kinases (IC₅₀s = 0.3 µM for c-Fms, c-Kit, ITD-FLT3 and 1 µM for PDGFRβ); blocks the proliferation of leukemia cells stimulated with FLT3 ligand by preventing the activation of STAT5.

A cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…

A FAHFA consisting of palmitoleic acid esterified at the 9-position of hydroxy stearic acid; significantly elevated in serum of glucose tolerant AG4OX mice; may be a bioactive lipid with roles in metabolic syndrome and inflammation.

A β1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity; often used to examine the activity of the drug-transporting MDR1 gene product P-glycoprotein.

CAS Number: 883986-34-3 Molecular Formula: C₂₄H₂₅N₅O₄ Formula Weight: 447.5

A sesterterpenoid fungal phytotoxin that binds and irreversibly antagonizes calmodulin, blocking the activation of calmodulin-dependent phosphodiesterase with an IC₅₀ value of 9 μM.

Selective inhibitor of IDH1 R132H and R132C mutants in vitro (IC₅₀s = 0.07 and 0.16 µM, respectively) but not wild-type IDH1, wild-type IDH2, or IDH2 mutants (IC₅₀s > 100 μM); anti-tumor efficacy in vitro and in vivo; induces demethylation of histone H3K9me3 and…

An allosteric, reversible inhibitor of PAR1 on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC₅₀ value of 0.26 µM; also blocks platelet activation induced by thrombin but not by PMA, U-46619, or collagen.

An inactive analog of U-73122; can be used as a negative control.

Inhibits several isoforms of protein kinase C (PKC; IC₅₀ = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.

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 metabolite of estradiol 3-sulfate that has been modified by a UDP-glucuronosyltransferase; enhances utilization by anion transporters, most commonly leading to excretion in urine and bile.

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…

An activator of sGC that binds to a regulatory site, resulting in activation in an NO-independent manner (Kd = 3.2 nM); reduces hypertension, limits cardiomyocyte hypertrophy, protects against ischemia/reperfusion injury, and reduces morbidity and mortality in response to endotoxic shock.

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 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.

An endogenous, maturation-inducing steroid that at 1 µg/ml induces germinal vesicle breakdown in oocytes from several teleost species; can also influence spermiation by stimulating milt production when administered at 5 mg/kg to various male teleosts.

A thiophene carboximide derivative proposed to inhibit IKK2; likely to be useful in the treatment of inflammatory diseases and cancer.

CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

A naturally-occurring lipid which is produced by the enzymatic removal of the acylated group of sphingomyelin; serves as a substrate for autotaxin to produce sphingosine-1-phosphate; occurs naturally in plasma, is a constituent of lipoproteins, and is increased in some diseases.

A small diffusible signaling molecule involved in quorum sensing in the model symbiont V. fischeri and the pathogens A. tumefaciens and P. aeruginosa.

A purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC₅₀ = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC₅₀ = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…

A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.

An analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.

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 selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC₅₀ = 26.4 nM; Ki = 5 nM).