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SAR405

37 Cited Publications
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Based on 37 publication(s) in Google Scholar

SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

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  • Reinheit: 99.74%
  • CAS. Nr.: 1523406-39-4
  • Formel: C19H21ClF3N5O2
  • Molecular Weight:443.85
  • Speicherung:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • SAR405 Chemical Structure
    SAR405 Chemical Structure
  • Experimental Validation Results for SAR405
  • Experimental Validation Results for SAR405
  • Experimental Validation Results for SAR405
  • Experimental Validation Results for SAR405
  • Experimental Validation Results for SAR405
CAS. Nr.: 1523406-39-4
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  • SAR405 Chemical Structure
    SAR405 Chemical Structure
    1/16
  • 1/16

    SAR405 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2021 Apr;53(4):435-444. [Abstract]

    Customer Validation
     Immunofluorescence staining of LC3B in uninfected or SARS-CoV-2-infected Huh7 cells treated with SAR405 (12.5 μM; 6 h) showed that PI3K type 3 inhibition completely abolished the formation of LC3-positive puncta and induced vacuoles in treated cells.

  • 1/16

    SAR405 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2021 Apr;53(4):435-444. [Abstract]

    Customer Validation
     Time series experiments showed an early stage post-receptor binding effect of the PI3K type 3 inhibitor SAR405 on HCoV-229E infection. Huh7 cells were infected, treated with SAR405 at different timepoints, and followed by determination of viral RNA levels at 10 hours post infection by qPCR. Inhibition of HCoV-229E by SAR405 occurred later in the viral life cycle than the attachment stage, as benchmarked by the attachment inhibitor Urtica dioica agglutinin (UDA), but earlier than the onset of intracellular replication as identified using the viral RNA synthesis inhibitor remdesivir.

  • 1/16

    SAR405 purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2021 Aug;18(8):2024-2039. [Abstract]

    Customer Validation
     PIK3C3 was an important regulator of myeloid cell function and a potential therapeutic target for treating EAE. SAR405 treatment delayed the onset of EAE. EAE was induced by active immunization with MOG35–55 peptide, and SAR405 (10 mg/kg; once daily) was administered orally starting 3 days after immunization for 11 consecutive days.

  • 1/16

    SAR405 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Cell Res. 2019 May;1866(5):793-805. [Abstract]

    Customer Validation
     Serum-starved H4IIEC3 cells are treated with 100 nM ins for 0, 5, 15, and 30 min, and electrophoresed protein extracts subjected to western blotting using antibodies against pAktS473 and Akt.

  • 1/16

    SAR405 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Cell Res. 2019 May;1866(5):793-805. [Abstract]

    Customer Validation
     Serum-starved H4IIEC3 cells are treated with 100 nM ins for 0, 5, 15, and 30 min and electrophoresed protein extracts subjected to western blotting using antibodies against total or phosphorylated p42/p44 MAPK.

  • SAR405