Biological Activity Description MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Features A moderately potent γ-secretase inhibitor. Targets γ secretase(Aβ40) Aβ (in human SH-SY5Y cells) 5 nM In vitro MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. In vivo MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16, while decreases levels of Aβ 1-17.

In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. Total Molecular Weight: g/mol Tip: Chemical formula is case sensitive.

DAPT (GSI-IX) is a γ-secretase inhibitor with IC50 of 0.12 and 0.2 μM for total Aβ and Aβ42 levels, respectively. Find all the information about DAPT (GSI-IX) for. RF Cafe Calculator Workbook v7.3 uploaded April 9, 2017 - download for free.

C10H16N2O2 c10h16n2o2 Instructions to calculate molar mass (molecular weight) of a chemical compound: To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'. Definitions of molecular mass, molecular weight, molar mass and molar weight: Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12) Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol. Clinical Trial Information (data from, updated on 2017-02-16) NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases Completed Advanced Cancer Merck Sharp & Dohme Corp. February 2011 Phase 1 Terminated Neoplasms Malignant Merck Sharp & Dohme Corp.

November 2010 Phase 1 Completed Pancreatic Cancer Cancer Research UK April 2010 Phase 1 Completed Healthy Merck Sharp & Dohme Corp. December 2008 Phase 1 Terminated Brain and Central Nervous System Tumors Pediatric Brain Tumor Consortium National Cancer Institute (NCI) July 2008 Phase 1 Active, not recruiting Breast Cancer Loyola University Merck Sharp & Dohme Corp. • PF-03084014 (PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. • AZD3839 is a potent and selective BACE1 inhibitor with K i of 26.1 nM, about 14-fold selectivity over BACE2. • Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. • Avagacestat (BMS-708163) is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0. Counter Strike Condition Zero Weapon Pack Download more. 3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch.

Features:Appears to be more “notch sparing” than semagacestat (LY450139). • RO4929097 is a γ secretase inhibitor with IC50 of 4 nM in a cell-free assay, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively. • Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, also inhibits Notch signaling with IC50 of 14.1 nM in H4 human glioma cell. Features:The best characterized γ-secretase inhibitor that has reached the clinic.

• DAPT (GSI-IX) is a novel γ-secretase inhibitor, which inhibits Aβ production with IC50 of 20 nM in HEK 293 cells. • LY411575 is a potent γ-secretase inhibitor with IC50 of 0.078 nM/0.082 nM (membrane/cell-based), also inhibits Notch cleavage with IC50 of 0.39 nM in APP or NΔE expressing HEK293 cells.

• Dibenzazepine (YO-01027) is a dipeptidic γ-secretase inhibitor with IC50 of 2.6 nM and 2.9 nM in cell-free assays for APPL and Notch cleavage, respectively. • FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.