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Vps34-PIK-III

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Chemical Structure| 1383716-40-2 同义名 : PIK-III;Vacuolar Protein Sorting 34 Inhibitor 2;Vps34 Inhibitor 2;VPS34-IN2
CAS号 : 1383716-40-2
货号 : A837347
分子式 : C17H17N7
纯度 : 99%+
分子量 : 319.364
MDL号 : MFCD28963904
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(93.94 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110δ

    PI3Kδ, IC50:1.2μM

  • Vps34

    Vps34, IC50:0.018μM
描述 Cells rely on autophagy to clear misfolded proteins and damaged organelles to maintain cellular homeostasis. PIK-III is an autophagy inhibitor which can acutely inhibit autophagy and de novo lipidation of LC3, and lead to the stabilization of autophagy substrates. PIK-III could modulate PtdIns(3)P-mediated effectors in mammalian cells. The IC50s of PIK-III are 0.018 μM, 1.2 μM, 3.04 μM, 3.96 μM and 4.43 μM for Vps34, PI3Kδ, PI3Kγ, PI3Kα and PI4Kβ, respectively. In a vitro study, CD34 + cells were treated ex vivo for 48h with PIK-III (5 µM). The reduction in engrafted cells following single PIK-III treatment, including primitive CD34+CD38- and CD34+CD133+ populations, confirmed the essential role of autophagy in the maintenance of the LSC pool[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.66mL

3.13mL

1.57mL

31.31mL

6.26mL

3.13mL
参考文献

[1]Dowdle WE, Nyfeler B, et al. Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat Cell Biol. 2014 Nov;16(11):1069-79.

[2]Dowdle WE, Nyfeler B, Nagel J, Elling RA, Liu S, Triantafellow E, Menon S, Wang Z, Honda A, Pardee G, Cantwell J, Luu C, Cornella-Taracido I, Harrington E, Fekkes P, Lei H, Fang Q, Digan ME, Burdick D, Powers AF, Helliwell SB, D'Aquin S, Bastien J, Wang H, Wiederschain D, Kuerth J, Bergman P, Schwalb D, Thomas J, Ugwonali S, Harbinski F, Tallarico J, Wilson CJ, Myer VE, Porter JA, Bussiere DE, Finan PM, Labow MA, Mao X, Hamann LG, Manning BD, Valdez RA, Nicholson T, Schirle M, Knapp MS, Keaney EP, Murphy LO. Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat Cell Biol. 2014 Nov;16(11):1069-79. doi: 10.1038/ncb3053. Epub 2014 Oct 19. PMID: 25327288.