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Spautin 1
- MBCQ derivative C43
- Soluble in DMSO
- MF: C15H11F2N3
- MW: 271.26
Description
Inhibitor of USP10 and USP13, that target the Beclin1 subunit of Vps34 complexes, thereby promoting the degradation of Vps34 PI3 kinase complexes. Beclin1 is a tumor suppressor and regulating deubiquitination activity of USP10 and USP13 by Beclin1 provides a mechanism for Beclin1 to control the levels of p53. Moreover, Spautin 1 inhibits autophagy which enhances imatinib-induced apoptosis in chronic myeloid leukemia. The pro-apoptotic activity of Spautin-1 was also associated with activation of GSK-3β, an important downstream effector of PI3K/AKT.
More Information
| Parent CAS No. | 1262888-28-7 |
|---|---|
| Chemical Name | 6-fluoro-N-(4-fluorobenzyl)quinazolin-4-amine |
| SMILES | N1=C2C(C=C(F)C=C2)=C(NCC2=CC=C(F)C=C2)N=C1 |
| MFCD | MFCD16962292 |
| InChi | 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 |
| CID | 51037431 |
| Short Description | USP10-USP13 inhibitor |
References
- S. Shao et al. Spautin-1, a novel autophagy inhibitor, enhances imatinib-induced apoptosis in chronic myeloid leukemia. Int J Oncol. 2014 May;44(5):1661-8.
- R. Mateo et al. Inhibition of cellular autophagy deranges dengue virion maturation. J Virol. 2013 Feb;87(3):1312-21.
- J. Liu et al. Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13. Cell. 2011 Sep 30;147(1):223-34.
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