PIK-III
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
作用于VPS34,IC50为18 nM。
PIK-III是一种VPS34抑制剂,能够抑制自噬。
研究发现VPS34激酶负责磷脂酰肌醇-3-磷酸在自噬体形成位点的合成和沉积,导致PtdIns(3)P结合蛋白的募集。
体外:在先前的研究中,PIK-III被鉴定为VPS34与疏水性口袋结合的选择性抑制剂。此外,PIK-III可以急性抑制LC3的自噬和脂质化,这导致自噬底物的稳定。此外,通过在PIK-III处理的细胞上进行泛素-亲和蛋白质组测定来鉴定底物(如NCOA4),其在具有ATG7缺陷的细胞中积累并与自噬溶酶体共定位。 NCOA4可直接结合铁蛋白重链-1,以在饥饿或铁耗尽后靶向铁结合铁蛋白复合物[1]。
体内:动物研究显示,PIK-III-处理的Ncoa4-/-小鼠在脾巨噬细胞中具有铁沉积,这对于吞噬红细胞的铁再利用十分重要。总之,该体内研究结果提供了铁蛋白选择性自噬的一种新机制,并揭示了先前未触及的自噬和NCOA4在控制体内铁稳态中的作用[1]。
临床试验:到目前为止,PIK-III仍处于临床前研究阶段。
参考文献:
[1] Dowdle WE 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.
- 1. Manuela Antonioli , Benedetta Pagni, et al. "HPV sensitizes OPSCC cells to cisplatin-induced apoptosis by inhibiting autophagy through E7-mediated degradation of AMBRA1." Autophagy. 2020 Nov 23;1-13. PMID:33172332
- 2. Ge L, Zhang M, et al. "Remodeling of ER-exit sites initiates a membrane supply pathway for autophagosome biogenesis." EMBO Rep. 2017 Sep;18(9):1586-1603. PMID:28754694
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 319.36 |
Cas No. | 1383716-40-2 |
Formula | C17H17N7 |
Solubility | ≥31.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5'-bipyrimidine]-2,2'-diamine |
SDF | Download SDF |
Canonical SMILES | NC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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