PIK-93

PIK-93

Catalog Number:
L002369335APE
Mfr. No.:
APE-A5449
Price:
$249
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      • Overview
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          Background

          PIK-93 is a potent and novel inhibitor of p110γ (PI3Kγ) and PI4KIIIβ (IC50= 16 nM and 19 nM, respectively).
          PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.
          Inhibition of PI3K via PIK-93 reduced the carbachol-activated translocation of TRPC6 to the plasma membrane and carbachol-activated net Ca(2+) entry into T6.11 cells. [1] PIK-93 also selectively inhibited the PI4KIIIβ enzyme, and siRNA-mediated down regulation of individual PI4-enzymes in COS-7 cells. [2] Furthermore, as a potent anti-PV compound, PIK93 targeted PI4Kβ to inhibit interaction of viral 3D polymerase and phosphatidylinositol 4-phosphate on the reorganized membrane vesicle for viral replication complex formation. [3] PIK93 also showed anti-PV with an EC50 of 0.14 μM for PV pseudovirus infection. [4]

          [1] Monet M, Francoeur N, Boulay G. Involvement of phosphoinositide 3-kinase and PTEN protein in mechanism of activation of TRPC6 protein in vascular smooth muscle cells. J Biol Chem. 2012 May 18;287(21):17672-81.
          [2] Tóth B, Balla A, Ma H et al. Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi. J Biol Chem. 2006 Nov 24;281(47):36369-77.
          [3] Hsu, N. Y., et al. 2010. Viral reorganization of the secretory pathway generates distinct organelles for RNA replication. Cell 141:799-811.
          [4] Arita M, Kojima H, Nagano T et al. Phosphatidylinositol 4-kinase III beta is a target of enviroxime-like compounds for antipoliovirus activity. J Virol. 2011 Mar;85(5):2364-72.

      • Properties
        • Alternative Name
          N-[5-[4-chloro-3-(2-hydroxyethylsulfamoyl)phenyl]-4-methyl-1,3-thiazol-2-yl]acetamide
          CAS Number
          593960-11-3
          Molecular Formula
          C14H16ClN3O4S2
          Molecular Weight
          389.88
          Appearance
          A solid
          Purity
          98.00%
          Solubility
          insoluble in H2O; ≥19.5 mg/mL in DMSO; ≥2.33 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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