Shanghai Nianxing Industrial Co., Ltd
China
Product Name: PIK-III
Price:
Purity: 98.0%
Stocking Period: 10 Day
Contact: Huang

DC Chemicals Limited
China
Product Name: PIK-III
Price: $600.0/100mg $1000.0/250mg $1900.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

ShangHai DC Chemicals Co.,Ltd
China
Product Name: PIK-III
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Lai

1383716-40-2

1383716-40-2 structure

1383716-40-2 structure

Name: Vps34-PIK-III
Chemical Name: pik-iii
CAS Number: 1383716-40-2
Molecular Formula: C₁₇H₁₇N₇
Molecular Weight: 319.36400
Catalog: Signaling Pathways Autophagy Autophagy
Create Date: 2018-04-06 13:16:44
Modify Date: 2024-01-04 15:39:41
Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM.

Name	pik-iii
Synonyms	4'-cyclopropylmethyl-N2-pyridin-4-yl-[4,5']bipyrimidinyl-2,2'-diamine 4'-cyclopropylmethyl-N2-pyridin-4-yl-[4,5'] bipyrimidinyl-2,2'-diamine Vps34-PIK-III

Description	Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Research Areas >> Neurological Disease
Target	Vps34:18 nM (IC50) PI(3)Kδ:1.2 μM (IC50) PI(3)Kγ:3.04 μM (IC50) PI(3)Kα:3.96 μM (IC50) Autophagy
In Vitro	PIK-III is a selective inhibitor of VPS34 that binds a unique hydrophobic pocket not present in related kinases such as PI3Kα. PIK-III is at least 100-fold-selective for VPS34 over related lipid kinases such as PI3K and the protein kinase mTOR. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, and leads to the stabilization of autophagy substrates. In H4 cells expressing the mCherry-GFP-LC3 reporter PIK-III inhibits the formation of mCherry-positive autolysosomes and increases the cytosolic signal of LC3 under basal conditions and when autophagy is induced with the mTOR inhibitor AZD8055. PIK-III prevents the turnover of GFP-tagged p62 under basal conditions and when autophagy is activated. PIK-III treatment leadsto an increase in the levels of LC3-I in H4 and PSN1 cells[2].
In Vivo	The DFX-induced NCOA4-dependent turnover of FTH1 and FTL is blocked with PIK-III suggesting an autophagy-dependent process[2].
References	[1]. Honda A, et al. Potent, Selective, and Orally Bioavailable Inhibitors of VPS34 Provide Chemical Tools to Modulate Autophagy in Vivo. ACS Med Chem Lett. 2015 Nov 13;7(1):72-6. [2]. 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.

Molecular Formula	C₁₇H₁₇N₇
Molecular Weight	319.36400
Exact Mass	319.15500
PSA	102.50000
LogP	3.26110
Storage condition	-20℃