Spautin-1 is a novel and potent autophagy inhibitor, which enhances imatinib-induced (MI) apoptosis in chronic myeloid leukemia. Autophagy has been proposed to play a role in MI resistance. Spautin-1 markedly inhibits IM-induced autophagy in CML cells by downregulating Beclin-1. Spautin-1 enhances IM-induced CML cell apoptosis by reducing the expression of the anti-apoptotic proteins Mcl-1 and Bcl-2. Spautin-1 enhances IM-induced apoptosis by inactivating PI3K/AKT and activating downstream GSK3β, leading to downregulation of Mcl-1 and Bcl-2, which represents a promising approach to improve the efficacy of IM in the treatment of patients with CML.
CAS Number: 1262888-28-7
Molecular Weight: 271.26
Chemical Name: 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-amine
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 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: ≥360 days 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
Spautin-1 was used at 10 µM final concentration in the cellular assays.
no in vivo use of Spautin-1 was reported so far.
- Liu J, et al. Beclin1 Controls the Levels of p53 by Regulating the Deubiquitination Activity of USP10 and USP13. (2011) Cell 147(1), 223-234.
- Joseph D. Mancias, et al. Targeting Autophagy Addiction in Cancer. (2011) Oncotarget 2(12):1302-6
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