PI 3-kinase p55γ Inhibitors
PI 3-kinase inhibitors, while not specifically targeting the p55γ regulatory subunit, focus on inhibiting the activity of phosphatidylinositol 3-kinases (PI 3-kinases), a family of enzymes involved in various cellular functions, including cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. The p55γ subunit is one of the regulatory subunits of class IA PI 3-kinases, which also includes the p85 regulatory and p110 catalytic subunits. These inhibitors mainly target the ATP-binding site of the p110 catalytic subunit of PI 3-kinases, which is crucial for their kinase activity. By binding to this site, these inhibitors block ATP from interacting with the kinase, thus inhibiting its ability to phosphorylate phosphatidylinositol substrates. This action effectively downregulates the PI 3-kinase/AKT signaling pathway, which is often hyperactivated in various cancers.
These inhibitors vary in their specificity and selectivity. Some, like LY294002 and Wortmannin, are broad-spectrum and affect multiple isoforms of PI 3-kinases. Others, such as Idelalisib and Copanlisib, are more selective, primarily targeting specific isoforms of the p110 catalytic subunit. The development of these inhibitors is driven by the need to address the role of dysregulated PI 3-kinase signaling in diseases, particularly in oncology.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a broad-spectrum inhibitor of PI 3-kinase, affecting various isoforms including the p55γ-associated p110 catalytic subunits. It binds to the ATP-binding site of these kinases, thereby inhibiting their activity. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin is a potent, irreversible inhibitor of PI 3-kinase, impacting multiple isoforms including those associated with p55γ. It covalently binds to a specific residue in the kinase domain, inhibiting its activity. | ||||||
PI-103 | 371935-74-9 | sc-203193 sc-203193A | 1 mg 5 mg | $33.00 $131.00 | 3 | |
PI-103 is a dual inhibitor of PI 3-kinase and mTOR, affecting the p55γ-related PI 3-kinase activity among others. It targets the ATP-binding domain of these kinases. | ||||||
CAL-101 | 870281-82-6 | sc-364453 | 10 mg | $193.00 | 4 | |
While CAL-101 predominantly targets the p110δ isoform of PI 3-kinase, it may have off-target effects on complexes involving p55γ. It inhibits kinase activity by binding to the ATP-binding site. | ||||||
BKM120 | 944396-07-0 | sc-364437 sc-364437A sc-364437B sc-364437C | 5 mg 10 mg 25 mg 50 mg | $176.00 $235.00 $281.00 $339.00 | 9 | |
BKM120, also known as Buparlisib, is a pan-class I PI 3-kinase inhibitor, affecting various isoforms including those related to p55γ. It competitively inhibits the ATP-binding site of the kinase. | ||||||
BAY 80-6946 | 1032568-63-0 | sc-503264 | 5 mg | $562.00 | ||
BAY 80-6946 is a pan-PI 3-kinase inhibitor with predominant activity against the p110α and δ isoforms, and may affect p55γ-associated complexes. It inhibits the kinase activity by binding to the ATP-binding domain. | ||||||
IPI 145 | 1201438-56-3 | sc-488318 | 5 mg | $317.00 | ||
Duvelisib primarily targets p110δ and γ isoforms of PI 3-kinase, and may indirectly influence p55γ-associated complexes. It acts by competing with ATP at the kinase domain. | ||||||
GSK2126458 | 1086062-66-9 | sc-364503 sc-364503A | 2 mg 10 mg | $265.00 $1050.00 | ||
GSK2126458 is a dual inhibitor of PI 3-kinase and mTOR, potentially affecting p55γ-related PI 3-kinase activity. It binds to the ATP-binding sites of these kinases. | ||||||
ZSTK 474 | 475110-96-4 | sc-475495 | 5 mg | $75.00 | ||
ZSTK474 inhibits class I PI 3-kinase activity, potentially affecting p55γ-associated complexes. It acts by binding to the ATP-binding domain of the kinase. | ||||||
BYL719 | 1217486-61-7 | sc-391001 sc-391001A sc-391001B sc-391001C sc-391001D sc-391001E | 5 mg 10 mg 50 mg 100 mg 500 mg 1 g | $391.00 $597.00 $755.00 $1192.00 $5000.00 $9370.00 | 2 | |
BYL719 specifically inhibits the p110α isoform of PI 3-kinase, but may have indirect effects on p55γ-associated kinase activity. It targets the ATP-binding site. | ||||||