1383716-33-3 Usage
Uses
Used in Pharmaceutical Research:
Vps34-IN-1 is used as a research tool for studying the role of VPS34 in various cellular processes, particularly autophagy. By inhibiting VPS34, researchers can gain insights into the molecular mechanisms underlying autophagy and its implications in various diseases.
Used in Autophagic Process Investigation:
Vps34-IN-1 is used as an inhibitor for investigating autophagic processes. Autophagy is a cellular mechanism that degrades and recycles damaged or unnecessary components, and its dysregulation has been linked to several diseases, including cancer, neurodegenerative disorders, and infections. Understanding the role of VPS34 in autophagy can help develop targeted therapies for these conditions.
Used in Cancer Research and Treatment:
Vps34-IN-1 is used as a potential therapeutic agent in cancer research and treatment. As a selective inhibitor of VPS34, it can disrupt the autophagic process in cancer cells, which may lead to their death. This property makes Vps34-IN-1 a promising candidate for the development of novel cancer therapies.
Used in Drug Delivery Systems:
In the context of drug delivery systems, Vps34-IN-1 can be used as a component in the development of targeted therapies. By incorporating Vps34-IN-1 into nanoparticles or other drug carriers, it may be possible to enhance its delivery to specific cells or tissues, improving its bioavailability and therapeutic outcomes.
Biological Activity
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].
IC 50
25 nm
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 1383716-33-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,8,3,7,1 and 6 respectively; the second part has 2 digits, 3 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1383716-33:
(9*1)+(8*3)+(7*8)+(6*3)+(5*7)+(4*1)+(3*6)+(2*3)+(1*3)=173
173 % 10 = 3
So 1383716-33-3 is a valid CAS Registry Number.
1383716-33-3Relevant academic research and scientific papers
BI-HETEROARYL COMPOUNDS AS VPS34 INHIBITORS
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, (2012/07/13)
The present invention includes novel methods of treating a disease or disorder characterized by hyperactivity of Vps34, and compound as Vps34 inhibitors; particularly compounds of Formula I or a pharmaceutically acceptable salt thereof, as well as methods
