IACS-010759 (IACS-10759)

Catalog No.S8731

For research use only.

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

IACS-010759 (IACS-10759) Chemical Structure

CAS No. 1570496-34-2

Selleck's IACS-010759 (IACS-10759) has been cited by 14 publications

Purity & Quality Control

Choose Selective OXPHOS Inhibitors

Biological Activity

Description IACS-010759 (IACS-10759) is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.
Targets
oxidative phosphorylation [2]
10 nM
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[1]. 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[2]. 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[3].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Z-138 MnvTVJJwdGmoZYLheIlwdiCjc4PhfS=> NU\TdFVIPzJiaB?= M12wb2lCS1NvMEGwO|U6KGmwaHnibZRm\CC2aHWgdJJwdGmoZYLheIlwdiCxZjDaMVE{QCCrbjDhJIRwe2WmZYDlcoRmdnRibXHucoVzKGG2IH7hco9ud2yjcjDjc45k\W62cnH0bY9vew>? NYTMdpF{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOlg1PDBpPkOxNFY5PDRyPD;hQi=>
Maver-1 NU\KR4pSWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUjtPZlvPzJiaB?= M2DiUWlCS1NvMEGwO|U6KGmwaHnibZRm\CC2aHWgdJJwdGmoZYLheIlwdiCxZjDNZZZmei1zIHnuJIEh\G:|ZXTldIVv\GWwdDDtZY5v\XJiYYSgcoFvd22xbHHyJINwdmOnboTyZZRqd26| M{XpU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzME[4OFQxLz5|MUC2PFQ1ODxxYU6=
H1975 M4HqRnBzd2yrZnXyZZRqd25iYYPzZZk> NWm1NoxxOiCmYYnz NYLMfZRUcGG|IHzpcYl1\WRiZX\m[YN1KG:wIHPlcIwheHKxbHnm[ZJifGmxbh?= M1nBb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkK1N|I6Lz5|ME[yOVMzQTxxYU6=
CLL cells NIPLXYxHfW6ldHnvckBie3OjeR?= NVzvd2NnOTByIH7N M{fpVlI1KGh? MlHGbY5pcWKrdIOgU2NTKGGwZDDpcoNz\WG|ZYOg[4x6[2:ueYPpd{BqdiCFTFygZ4VtdHN? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTh4MUi0O{c,Ojl6NkG4OFc9N2F-
Assay
Methods Test Index PMID
Western blot Cyto c / VDAC1 / β-Actin ; Cleaved PARP / Cleaved Caspase 3 / GAPDH ; Actin / LC3B I / LC3B II 32847115 29861847 32792483
Growth inhibition assay Tumor Volume 32581056
IHC pimonidazole stain ; pimonidazole stain of skull section ; H&E stain 30787016 32695673
Immunofluorescence Bodipy 493-503 / DAPI ; VDAC1 : IP3R1 32792483

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: CLL cells
  • Concentrations: 30 nM, 100 nM, 300 nM, 1 μM, and 3 μM
  • Incubation Time: 24 or 48 h
  • Method:

    CLL cells are treated with IACS-010759 for 24 or 48 h and were then stained with acridine orange and analyzed by flow cytometry.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 562.56
Formula

C25H25F3N6O4S

CAS No. 1570496-34-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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