For research use only. Not for therapeutic Use.
PIK-III（Cat No.:I008763）, also known as VPS34-IN2, is a selective inhibitor that targets the enzymatic activity of VPS34, a class III phosphatidylinositol 3-kinase (PI3K). It effectively inhibits autophagy, preventing the re-lipidation of LC3 and leading to the stabilization of autophagy substrates. PIK-III exhibits potent inhibitory activity, with IC50 values of 0.018 μM for VPS34 and 1.2 μM for PI(3)Kδ. By specifically targeting VPS34, PIK-III offers a valuable tool for studying autophagy-related processes and may hold therapeutic potential for diseases associated with dysregulated autophagy pathways.
| Catalog Number | I008763 |
| CAS Number | 1383716-40-2 |
| Synonyms | PIK-III; VPS34-IN2; VPS34-IN 2; VPS34-IN-2.;4/’-(cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5/’-bipyrimidine]-2,2/’-diamine |
| Molecular Formula | C17H17N7 |
| Purity | ≥95% |
| Target | Autophagy |
| Solubility | Soluble in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | 4-(cyclopropylmethyl)-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-amine |
| InChI | InChI=1S/C17H17N7/c18-16-21-10-13(15(23-16)9-11-1-2-11)14-5-8-20-17(24-14)22-12-3-6-19-7-4-12/h3-8,10-11H,1-2,9H2,(H2,18,21,23)(H,19,20,22,24) |
| InChIKey | XXSDLQLNIVFIJI-UHFFFAOYSA-N |
| SMILES | C1CC1CC2=NC(=NC=C2C3=NC(=NC=C3)NC4=CC=NC=C4)N |
| Reference | </br>1: 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. PubMed PMID: 25327288. |
