PIT-1

Names

[ Name ]:
PIT-1

[Synonym ]:
Benzamide, N-[[(3-chloro-2-hydroxy-5-nitrophenyl)amino]thioxomethyl]-
N-[[(3-Chloro-2-hydroxy-5-nitrophenyl)amino]thioxomethyl]-benzamide
PIT-1
Impentamine dihydrobromide
N-[(3-Chloro-2-hydroxy-5-nitrophenyl)carbamothioyl]benzamide

Biological Activity

[Description]:

PIT-1 is a selective PIP3 (phosphatidylinositol 3,4,5-trisphosphate) antagonist. PIT-1 inhibits cancer cell survival and induces apoptosis by inhibition of PIP3 dependent PI3K / Akt signaling. PIT-1 exhibits antitumor activity in vivo[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

[References]

[1]. Miao B, et al. Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains. Proc Natl Acad Sci U S A. 2010 Nov 16;107(46):20126-31.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C₁₄H₁₀ClN₃O₄S

[ Molecular Weight ]:
351.765

[ Exact Mass ]:
351.008057

[ PSA ]:
139.27000

[ LogP ]:
4.28

[ Index of Refraction ]:
1.747

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H400

[ Precautionary Statements ]:
P273

[ RIDADR ]:
UN 3077 9 / PGIII

Articles

Small molecule inhibition of phosphatidylinositol-3,4,5-triphosphate (PIP3) binding to pleckstrin homology domains.

Proc. Natl. Acad. Sci. U. S. A. 107(46) , 20126-31, (2010)

The PI3-kinase (PI3K) pathway regulates many cellular processes, especially cell metabolism, cell survival, and apoptosis. Phosphatidylinositol-3,4,5-trisphosphate (PIP3), the product of PI3K activity...

Inhibition of cell migration by PITENINs: the role of ARF6.

Oncogene 31(39) , 4317-32, (2012)

We have reported previously the development of small-molecule phosphatidylinositol-3,4,5-trisphosphate (PIP3) antagonists (PITs) that block pleckstrin homology (PH) domain interaction, including activ...