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Cat. No. Name Size Price Add Cart
KI3485PIK-93QuoteQuote

Chemical Characteristic

Product NamePIK-93
CAS No.593960-11-3
Molecular Weight 389.88
FormulaC14H16ClN3O4S2
Chemical NameN-[5-[4-Chloro-3-[[(2-hydroxyethyl)amino]sulfonyl]phenyl]-4-methyl-2-thiazolyl]acetamide
SmilesC(=O)(C)Nc1sc(c(n1)C)c1cc(c(cc1)Cl)S(=O)(=O)NCCO
Chemical Structure

Biological activities

PIK-93 is the first potent, synthetic Phosphoinositide kinases (PIK) inhibitor. PIK-93 shows to inhibit PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 39 nM, 0.59 µM, 0.12 µM and 16 nM, respectively.[1] PIK-93 inhibits carbachol-induced translocation of TRPC6,which is a cation channel in the plasma membrane and plays a role in Ca2+ entry after the stimulation of a G(q)-protein-coupled or tyrosine-kinase receptor,to the plasma membrane and carbachol-induced net Ca2+ entry into T6.11 cells. In vitro, PIK-93 at 0.5-1 µM impairs stability of the leading edge induced by uniform f-Met-Leu-Phe (fMLP) and alters the localization of the fMLP-dependent accumulation of F-actin in differentiated HL60 (dHL60) cells.[2] In T6.11 cells, PIK-93 at 300 nM blocks carbachol- induced translocation of TRPC6 to the plasma membrane.[3]

Protocols

In vitro, PIK-93 is dissolved in DMSO.[3]

References

[1] Knight Z A, et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell, 2006, 125(4): 733-747.
[2] Van Keymeulen A, et al. To stabilize neutrophil polarity, PIP3 and Cdc42 augment RhoA activity at the back as well as signals at the front. The Journal of cell biology, 2006, 174(3): 437-445..
[3] Monet M, et al. Involvement of phosphoinositide 3-kinase and PTEN protein in mechanism of activation of TRPC6 protein in vascular smooth muscle cells. Journal of Biological Chemistry, 2012, 287(21): 17672-17681.

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