PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1 in adipocytes and myotubes. PI 3-kinase (PI3K) catalyzes the synthesis of the second messengers PtdIns-(3)-P, PtdIns-(3,4)-P2, and PtdIns-(3,4,5)-P3. The PI 3-kinase family of enzymes is comprised of 15 members that are divided into three classes according to their structure, substrate specificity, and mode of regulation. In the class I PI 3-kinases, p110α is the primary PI 3-kinase isoform required for insulin signaling in adipocytes and myotubes and is frequently mutated in primary tumors. Small molecule inhibitors of p110α are of interest in cancer treatment research. PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM. PIK-75 inhibits p110γ and p110β considerably less effectively.
1 Fan, Q., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9 341-349 (2006). 2 Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 733-747 (2006).
Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2021 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.