|6-氟-N-(4-氟苄基)喹唑啉-4-胺|CsnPharm

CAS No.: 1262888-28-7

6-Fluoro-N-(4-fluorobenzyl)quinazolin-4-amine Catalog No. CSN13809

Synonyms: Spautin-1

Spautin-1 is inhibitor of USP10 and USP13 with IC50 of ∼0.6 and 0.7 μM respectively, it's also a potent and specific autophagy inhibitor.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 USP10

IC50:∼0.6-0.7μM USP13

IC50:∼0.6-0.7μM
描述Autophagy is an important intracellular catabolic mechanism that mediates the degradation of cytoplasmic proteins and organelles. Spautin-1 is a specific and potent inhibitor of autophagy which promotes the degradation of Vps34 PI3 kinase complexes by inhibiting two ubiquitin-specific peptidases (USP10 and USP130; IC₅₀s among 0.6 - 0.7 μM) that target the Beclin1 subunit of Vps34 complexes. Bcap-37 cells treated with spautin-1 under glucose-free condition for 48 hr showed apoptotic morphology and characteristic PARP cleavage. Spautin-1 inhibited etoposide induced autophagic cell death of Bax-Bak DKO (double knockout) cells^[3]. Treatment of VSMCs (vascular smooth muscle cells) with spautin-1 (10 µM; 24 hr) prevented platelet-derived growth factor (PDGF)-induced increases in LC3 abundance and prevented losses of calponin and α-SMA (α-smooth muscle cell-actin) after PDGF exposure. Spautin-1 also prevented PDGF-induced disorganization of actin filaments^[4].
动物研究
剂量
Mice: 1 mg/kg^[3] (i.p.), 20 mg/kg/day^[4] (i.p.), 40 mg/kg^[5] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 1 mg/kg^[3] (i.p.), 20 mg/kg/day^[4] (i.p.), 40 mg/kg^[5] (i.p.)
给药途径	i.p.

[1] Mateo R, Nagamine CM, et al. Inhibition of cellular autophagy deranges dengue virion maturation. J Virol. 2013 Feb;87(3):1312-21.
[2] Liu J, Xia H, 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
[3] Liu J, Xia H, Kim M, Xu L, Li Y, Zhang L, Cai Y, Norberg HV, Zhang T, Furuya T, Jin M, Zhu Z, Wang H, Yu J, Li Y, Hao Y, Choi A, Ke H, Ma D, Yuan J. Beclin1 controls the levels of p53 by regulating the deubiquitination activity of USP10 and USP13. Cell. 2011 Sep 30;147(1):223-34. doi: 10.1016/j.cell.2011.08.037. PMID: 21962518; PMCID: PMC3441147.
[4] Salabei JK, Cummins TD, Singh M, Jones SP, Bhatnagar A, Hill BG. PDGF-mediated autophagy regulates vascular smooth muscle cell phenotype and resistance to oxidative stress. Biochem J. 2013 May 1;451(3):375-88. doi: 10.1042/BJ20121344. PMID: 23421427; PMCID: PMC4040966.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.6864 mL
- 18.4322 mL
- 36.8643 mL
- 5 mM
- 0.7373 mL
- 3.6864 mL
- 7.3729 mL
- 10 mM
- 0.3686 mL
- 1.8432 mL
- 3.6864 mL

技术信息

CAS号

1262888-28-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H11F2N3

运输

蓝冰

分子量

271.26

别名

Spautin-1

溶解度

DMSO	54.0 mg/mL (199.1 mM)
Water	Insoluble
Ethanol	7.0 mg/mL (25.8 mM)

动物实验配方

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靶点	Description	IC50
USP10		IC50:∼0.6-0.7μM
USP13		IC50:∼0.6-0.7μM

6-Fluoro-N-(4-fluorobenzyl)quinazolin-4-amine Catalog No. CSN13809

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