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

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

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.

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3

A selective, cell-permeable, reversible inhibitor of MKLP-2 (IC50s = 0.83-1.35 μM); treatment with 10-50 μM results in binucleated cells, perturbing relocation of Aurora B kinase and survivin to the central spindle in anaphase cells without affecting microtubule polymerization.

A neutral RARα-selective antagonist (Ki = 2.5 nM); antagonizes agonist-induced coactivator recruitment and moderately decreases SMRT binding to RAR but does not significantly affect nuclear receptor corepressor binding.

Cloprostenol is a synthetic PGF2α analog and a potent FP receptor agonist. (+)-15-epi Cloprostenol is the 15(S), or 15β-hydroxy enantiomer of (+)-cloprostenol. This epimer is less active by several orders of magnitude as an FP receptor ligand when compared to 15(R)-cloprostenol. However,…

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

A multi-target inhibitor that potently blocks EGFR and HER2 (IC₅₀s = 2.4 and 16.4 nM, respectively) and inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC₅₀s = 4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively).

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

A selective, orally bioavailable inhibitor of Akt1, 2, and 3 (Kis = 0.08, 2, and 2.6 nM, respectively); inhibits the proliferation of human cancer cell lines with Akt pathway activation and various cell lines derived from hematologic malignancies.

A potent, orally available inhibitor of CDKs, blocking the Cdk9 activity of P-TEFb (IC50 = 8 nM) as well as all other CDK isoforms (IC50 = 100-300 nM); less effectively inhibits EGFR and PKA (IC50 = 21 and 122 μM, respectively); has potential applications in cancer therapy.

A mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.

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 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.

An irreversible, membrane-permeable inhibitor of lysosomal and cytosolic cysteine proteases; at 20-200 µM arrests human epidermoid carcinoma A431 cells at mitotic metaphase; inhibits protease-resistant protein accumulation in scrapie-infected neuroblastoma cells (IC₅₀ = 0.5 µM).

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 DR5 agonist (Kd= 1.2 µM; IC₅₀ = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.

8-iso PGF2β is an isomer of PGF2α with a non-enzymatic, non-cyclooxygenase origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and…

Zileuton (Zyflo™) is a reversible 5-LO inhibitor that was approved in 1997 for the prevention and treatment of asthma in the USA, but was withdrawn by Abbott Laboratories in 2003. Zileuton inhibits 5-LO from rat basophilic leukemia-1 (RBL-1) cells with an IC50 value of 0.5 µM. It is a…

A selective, ATP-competitive inhibitor of the DNA damage control kinase, Chk2 (IC₅₀ = 15 nM); prevents apoptosis in human T-cells exposed to ionizing radiation (EC₅₀ = 3-7.6 µM).

13,14-dihydro-15-keto PGF1α is a metabolite of PGF1α that has been reported in the rat stomach. The measurement of 13,14-dihydro-15-keto PGF1α can be used as a marker of the in vivo production of PGF1α.

A homolog of LOEA, characterized by the addition of an (S)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.

A selective inhibitor of PAD4 (IC₅₀ = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils.

AMC-AA is one of several fatty acid amides which can be used to measure FAAH activity. Exposure of AMC-AA to FAAH results in the release of the fluorescent aminomethyl coumarin that absorbs at 360 nm and emits at 465 nm, allowing for fast and convenient measurement of FAAH activity using a simple…

Activates cardiac differentiation, inducing the expression of early cardiac genes in mouse pluripotent and embryonic stem cells in vitro at low micromolar concentrations; drives differentiation of human peripheral blood mononuclear cells, mobilized by G-CSF, toward a cardiac phenotype.

A cell-permeable derivative of 2-HG.

A carboxylic acid-based inhibitor of aldose reductase (IC₅₀ = 0.01-15 μM) that suppresses high glucose-induced proliferation of vascular smooth muscle cells as well as prevents high glucose-induced intracellular NADH/NAD+ increase and membrane-bound protein kinase C activation.

An endogenous agonist for LXRα (EC₅₀ = 325 nM) that can induce the expression of the ABCA1 reverse cholesterol transporter to inhibit the overall absorption of cholesterol; used as a substrate to monitor cholesterol transport or as an endogenous positive control for testing LXR agonists.

An L-type calcium channel blocker that is selective over N-, R-, P/Q- and T-type calcium channels; displays antihypertensive activity, lowering arterial blood pressure without altering cardiac contractility.

A metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.

Formal Name: 4-[6-methoxy-2-[(1E)-2-(3-nitrophenyl)ethenyl]-4-oxo-3(4H)-quinazolinyl]-benzoic acid CAS Number: 1237744-13-6 Molecular Formula: C₂₄H₁₇N₃O₆