InformationIACS-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.Targetsoxidative phosphorylation 10 nMIn vitroIACS-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.Cell Research(from reference)Cell lines:CLL cells Concentrations:30 nM, 100 nM, 300 nM, 1 μM, and 3 μM Incubation Time:24 or 48 h.
Specifications and Purity: ≥99%
Molecular Formula: C25H25F3N6O4S
Molecular Weight: 562.56
PubChem CID: 86711931
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
Related Documents: https://aladdin-for-icloud-store.oss-cn-hangzhou.aliyuncs.com/aladdinsci/pdp/sds/1/I414142-SCI_4fa1ad2d99b5b8d3f7dc454c4b5d0f4b.pdf
- UPC:
- 42181902
- Condition:
- New
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- I414142-25mg
- CAS:
- 1570496-34-2
- Product Size:
- 25mg
- Hazard Statement Codes:
- H335:H319:H315:H302
- Precautionary Statement Codes:
- P305+P351+P338:P261
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