Vps34 inhibitor PIK-III

Research use only, not for human use.

Vps34 inhibitor PIK-III (PIK-III) is a potent, selective inhibitor of Vps34 with IC50 of 18 nM.

Vps34 inhibitor PIK-III (PIK-III) is a potent, selective inhibitor of Vps34 with IC50 of 18 nM, shows >100-fold selectivity over other class I PI3Ks, PI4Kβ and mTOR; inhibits the localization of GFP-FYVE in mammalian cells with IC50 of 55 nM, which is >10,000 times more potent than the non-selective VPS34 inhibitor 3-MA; robustly inhibits autophagy and LC3 lipidation, leads to the stabilization of autophagy substrates in mammalian cells.

Cell Viability Assay Cell Line:DLD1 cellsConcentration:1, 5, 10 μM Incubation Time:24 h Result:Prevented the degradation of autophagy substrates p62, NCOA4, NBR1, NDP52, and FTH1.RT-PCR Cell Line:HCC cells Concentration:5 μM Incubation Time:24 h Result:Inhibited stemness genes expression.Western Blot Analysis Cell Line:Huh7 and MHCC97H cells Concentration:5 μM Incubation Time:24 h Result:Inhibited liver CSCs by activating AMPK.

Animal Model:C57BL/6 mice.Dosage:10 mg/kg; 2 mg/kg Administration:Oral administration; intravenous injection.

PIK-III

PI3K/Akt/mTOR signaling

PI3K

PI3Kα|PI3Kβ|PI3Kγ|PI3Kδ|Vps34

Other Indications

——

1383716-40-2

319.3638

C17H17N7

>98% (HPLC)

DMSO: ≥ 31 mg/mL

NC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1

[4,5'-Bipyrimidine]-2,2'-diamine, 4'-(cyclopropylmethyl)-N2-4-pyridinyl-

(-20℃)

With Ice Pack

≥ 2 years