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Merck

SML0440

Sigma-Aldrich

Spautin-1

≥98% (HPLC)

Synonym(e):

6-Fluoro-N-[(4-fluorophenyl)methyl]-4-quinazolinamine, C43

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About This Item

Empirische Formel (Hill-System):
C15H11F2N3
CAS-Nummer:
Molekulargewicht:
271.26
MDL-Nummer:
UNSPSC-Code:
12352200
PubChem Substanz-ID:
NACRES:
NA.77

Qualitätsniveau

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 15 mg/mL (clear solution)

Lagertemp.

2-8°C

SMILES String

FC1=CC=C(C=C1)CNC2=C3C=C(F)C=CC3=NC=N2

InChI

1S/C15H11F2N3/c16-11-3-1-10(2-4-11)8-18-15-13-7-12(17)5-6-14(13)19-9-20-15/h1-7,9H,8H2,(H,18,19,20)

InChIKey

AWIVHRPYFSSVOG-UHFFFAOYSA-N

Anwendung

Spautin-1 has been used as an autophagy inhibitor:
  • to study its effects on vascular, glial, and neuronal alterations in the oxygen-induced retinopathy mouse model
  • to evaluate its pre-treatment effect on the response of canine osteosarcoma cells to doxorubicin
  • to study its effects on the production of interleukin (IL)-6 by oxidatively stressed dendritic cells (OS-DCs) in Luminex assay

Biochem./physiol. Wirkung

Spautin-1 inhibits the activity of two ubiquitin-specific peptidases, USP10 and USP13, causing an increase in proteasomal degradation of class III PI3 kinase complexes, which have been shown to regulate autophagy.
Specific and potent autophagy inhibitor-1 (Spautin-1) is a small molecule, which can inhibit autophagy and induce cancer cell death. It inhibits autophagy by degrading beclin-1. Spautin-1 augments the efficiency of radiation therapy and chemotherapy in various human cancer cell lines.

Piktogramme

CorrosionExclamation mark

Signalwort

Danger

H-Sätze

Gefahreneinstufungen

Acute Tox. 4 Oral - Eye Dam. 1

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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Analytical biochemistry, 549, 58-65 (2018-03-17)
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Alice Verchère et al.
Scientific reports, 2, 306-306 (2012-03-09)
We describe an original activity assay for membrane transport that uses the proton motive force-dependent efflux pump MexAB from Pseudomonas aeruginosa. This pump is co-reconstituted into proteoliposomes together with bacteriorhodopsin (BR), a light-activated proton pump. In this system, upon illumination
Daniel G Panaccione et al.
Scientific reports, 7(1), 8930-8930 (2017-08-23)
Neosartorya fumigata (Aspergillus fumigatus) is the most common cause of invasive aspergillosis, a frequently fatal lung disease primarily affecting immunocompromised individuals. This opportunistic fungal pathogen produces several classes of specialised metabolites including products of a branch of the ergot alkaloid
Ge Yang et al.
Scientific reports, 7(1), 17970-17970 (2017-12-23)
Presenilin (PS1 or PS2) functions as the catalytic subunit of γ-secretase, which produces the toxic amyloid beta peptides in Alzheimer's disease (AD). The dependence of folding and structural stability of PSs on the lipophilic environment and mutation were investigated by
Kuntal Ganguly et al.
Drug delivery, 23(8), 2838-2851 (2015-11-05)
Microspheres of chitosan (CS) cross-linked with polyethylene glycol (PEG) were prepared by emulsion-cross-linking followed by the solvent evaporation technique. The formulations were characterized and subjected to in vitro and in vivo tests to assess cell growth, changes in cell morphology

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