PIK93 is a phenylthiazole-based inhibitor of PI4KIIIb (IC50 = 19 nM) used to evaluate the role of PI4-K isoforms in calcium signaling. [1] At a concentration of 300 nM PIK93 inhibited the p110g isoform of PI3K (Class I) was inhibited at IC50 of 16 nM, while weakly inhibiting PI3K-C2a (IC50 = 16 uM). [2] PIK93 is selective for PI4KIIIb over PI4KIIIa (EC90 = 250 nM and EC50 >10 uM, respectively) and is inactive toward type II PI4Ks. [3] PIK93 was also identified as a potent anti-poliovirus and anti-HCV agent, with EC50s of 0.14 and 1.9 uM, respectively. [4]
Technical information:
| Chemical Formula: | C14H16ClN3O4S2 | |
| CAS #: | 593960-11-3 | |
| Molecular Weight: | 389.88 | |
| Purity: | >98% | |
| Appearance: | White | |
| Chemical Name: | N-[5-[4-Chloro-3-[(2-hydroxyethyl)sulfamoyl]phenyl]-4-methylthiazol-2-yl]acetamide | |
| Solubility: | Up to 22 mM in DMSO | |
| Synonyms: | PIK-93, PIK 93, PIK93 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Knight et al., A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell, 2006, 125(4), 733-747. Pubmed ID: 16647110 |
| 2. | Monet et al., Involvement of phosphoinositide 3-kinase and PTEN protein in mechanism of activation of TRPC6 protein in vascular smooth muscle cells. J. Biol. Chem. 2012, 287(21), 17672-17681. Pubmed ID: 22493444 |
| 3. | Toth et al., Phosphatidylinositol 4-kinase IIIbeta regulates the transport of ceramide between the endoplasmic reticulum and Golgi. J. Biol. Chem. 2006, 281(47), 36369-36377. Pubmed ID: 17003043 |
| 4. | Arita et al., Phosphatidylinositol 4-kinase III beta is a target of enviroxime-like compounds for antipoliovirus activity. J. Virol. 2011, 85(5), 2364-2372. Pubmed ID: 22493444 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
