Description
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
Product information
CAS Number: 1644443-47-9
Molecular Weight: 346.73
Formula: C14H11ClN6O3
Chemical Name: 6-chloro-N-(5-methyl-1H-pyrazol-3-yl)-2-(4-nitrophenoxy)pyrimidin-4-amine
Smiles: CC1=CC(NC2C=C(Cl)N=C(N=2)OC2C=CC(=CC=2)[N+]([O-])=O)=NN1
InChiKey: CEUMAXLRGBKFQP-UHFFFAOYSA-N
InChi: InChI=1S/C14H11ClN6O3/c1-8-6-13(20-19-8)17-12-7-11(15)16-14(18-12)24-10-4-2-9(3-5-10)21(22)23/h2-7H,1H3,(H2,16,17,18,19,20)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 30 mg/mL (86.52 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Autophinib (0.01-1 μM) inhibits LC3 lipidation to form LC3-II in a dose-dependent manner in starved MCF7-LC3 cells. Consistent with inhibition of autophagic flux, Autophinib also inhibits p62 degradation by autophagy dose-dependently in MCF7-LC3 cells. Autophinib enhances cell death (EC50 of 264 nM) of starved cells as compared to fed cells, which occurred via the induction of apoptosis (EC50 of 234 nM) in MCF7 cells.
Products are for research use only. Not for human use.
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