VPS34-IN1

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.
IC50: 25 nM
VPS34-IN1 is a Vps34 inhibitor.
The vacuolar protein sorting 34 (Vps34) class III phosphoinositide 3-kinase (PI3K) phosphorylates phosphatidylinositol (PtdIns) to generate PtdIns(3)P that regulates membrane trafficking processes through its ability to recruit a subset of proteins possessing PtdIns(3)P-binding phox homology (PX) and FYVE domains.
In vitro: VPS34-IN1 was identified to be able to inhibit in-vitro Vps34, but did not significantly inhibit the activity of tested 340 protein kinases or 25 lipid kinases that include all isoforms of class I and class II PI3Ks. Treatment of VPS34-IN1 to cells dose-dependently induced a quick dispersal of a specific PtdIns(3)P-binding probe, without altering the ability of class I PI3K to regulate Akt. Moreover, VPS34-IN1 could also induce a quick ~50-60% loss of SGK3 phosphorylation within 1 min. However, VPS34-IN1 could not inhibit activity of the SGK2 isoform without a PtdIns(3)P-binding PX domain. In addition, the combination of VPS34-IN1 and class I PI3K inhibitor of GDC-0941 resulted in the reduced SGK3 activity ~80-90%. Therefore, these data demonstrated that VPS34-IN1 would be a useful probe to delineate physiological roles of the Vps34 and the combination of class I such as GDC-0941 and class III such as VPS34-IN1 PI3K inhibitors could be used to better analyse the roles and regulation of the elusive class II PI3K [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, VPS34-IN1 is still in the preclinical development stage.
Reference:
[1] Bago R et al. Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase. Biochem J.2014 Nov 1;463(3):413-27.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 425.91 |
Cas No. | 1383716-33-3 |
Formula | C21H24ClN7O |
Solubility | Soluble in DMSO |
Chemical Name | 1-((2-((2-chloropyridin-4-yl)amino)-4'-(cyclopropylmethyl)-[4,5'-bipyrimidin]-2'-yl)amino)-2-methylpropan-2-ol |
SDF | Download SDF |
Canonical SMILES | CC(CNC1=NC=C(C(CC2CC2)=N1)C3=NC(NC4=CC(Cl)=NC=C4)=NC=C3)(O)C |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
