IACS-010759 (IACS-10759) - 10mM in DMSO , CAS No.1570496-34-2

CAS: 1570496-34-2 Cat. No.: I408373 Molecular Weight: 562.56

GRADE & PURITY 10mM in DMSO

Synonyms

Piperidine, 4-​(methylsulfonyl)​-​1-​[3-​[[5-​methyl-​3-​[3-​[4-​(trifluoromethoxy)​phenyl]​-​1,​2,​4-​oxadiazol-​5-​yl]​-​1H-​1,​2,​4-​triazol-​1-​yl]​methyl]​phenyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

IACS-010759 (IACS-10759) IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.
In vitro

IACS-010759 significantly reduced viability measured by CTG assay in all cell lines tested (Notch mutant: Pf382, 1301, Jurkat, MOLT-4, P12-Ichikawa and Notch wt: T-ALL1). Treatment of T-ALL with IACS-010759 had effectively inhibited FA-stimulated mitochondrial respiration indicated by decreased oxygen consumption rates (OCR). However, the cells maintain an ability to generate energy via glycolysis, indicated by high extracellular acidification rate (ECAR) in both, control and IACS-treated groups. In CLL cells, IACS-010759 causes minimal cell death, inhibits oxygen consumption rate (OCR) and increases glycolysis. It also decreases intracellular ribonucleotide triphosphate pools in CLL. In sensitive AML cells IACS-010759 induces AMPK activation leading to mTOR suppression which results in cell growth inhibition in AML cells. AMPK and mTOR could be putative biomarkers of anti-leukemia activity of the novel OxPhosi IACS-010759.

In vivo

Cell Data

cell lines：LoVo and SW620 colorectal cancer cells and A549 non–small-cell lung carcinoma cells.

Concentrations：30 nM, 100 nM, 300 nM, 1 μM, and 3 μM

Incubation Time：24 or 48 h

Powder Purity:≥99%

Specifications

Synonyms

Piperidine, 4-​(methylsulfonyl)​-​1-​[3-​[[5-​methyl-​3-​[3-​[4-​(trifluoromethoxy)​phenyl]​-​1, ​2, ​4-​oxadiazol-​5-​yl]​-​1H-​1, ​2, ​4-​triazol-​1-​yl]​methyl]​phenyl]​-

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: CC1=NC(=NN1CC2=CC(=CC=C2)N3CCC(CC3)S(=O)(=O)C)C4=NC(=NO4)C5=CC=C(C=C5)OC(F)(F)F
• Molecular Weight: 562.56
• Reaxy-Rn: 26653384
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26653384&ln=