PI 3-kinase p110 Inhibitors
PI 3-kinase p110 inhibitors are a class of chemical compounds designed to target and inhibit the activity of phosphoinositide 3-kinase (PI 3-kinase) isoform p110. PI 3-kinases are a family of lipid kinases that play a crucial role in intracellular signaling pathways, regulating various cellular processes such as cell growth, proliferation, survival, and metabolism. Within this family, p110 isoforms are particularly significant as they are often associated with oncogenic mutations and aberrant signaling in numerous cancer types. Inhibitors targeting p110 isoforms are designed to disrupt these signaling pathways and hinder the growth and survival of cancer cells.
The mechanism of action of PI 3-kinase p110 inhibitors typically involves binding to the active site of the p110 enzyme, thereby preventing its phosphorylation of phosphoinositide substrates. This interference disrupts downstream signaling cascades, which are normally activated in response to growth factor receptor activation. As a result, the inhibitors may impede the activation of protein kinase B (Akt) and downstream effectors, which are critical for cell proliferation and survival. By selectively inhibiting the activity of p110 isoforms, these compounds aim to target cancer cells with aberrant PI 3-kinase signaling while sparing normal cells. The development of PI 3-kinase p110 inhibitors represents a promising avenue in the field of cancer research, as they have the ability to be used as a target for various malignancies characterized by dysregulated PI 3-kinase signaling pathways.
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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 | $121.00 $392.00 | 148 | |
LY294002 is a synthetic molecule that selectively inhibits PI3Ks, particularly the p110 isoforms. It competes with ATP for binding to the kinase domain, thus inhibiting the enzyme's activity and downstream signaling. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is a potent and irreversible inhibitor of PI3K. It covalently binds to the p110 subunit, leading to the inhibition of its kinase activity. This compound is found in the fungus Penicillium wortmannin. | ||||||
PI-103 | 371935-74-9 | sc-203193 sc-203193A | 1 mg 5 mg | $32.00 $128.00 | 3 | |
PI-103 is a small molecule inhibitor that targets PI3K p110 isoforms and mTOR, disrupting their kinase activities. By doing so, it helps in modulating cell growth and survival signaling pathways. | ||||||
GDC-0941 | 957054-30-7 | sc-364498 sc-364498A | 5 mg 10 mg | $184.00 $195.00 | 2 | |
GDC-0941 is a potent and selective inhibitor of class I PI3K, including the p110 isoforms. It acts by binding to the ATP-binding site of the enzyme, resulting in inhibition of its activity and downstream effects. | ||||||
BEZ235 | 915019-65-7 | sc-364429 | 50 mg | $207.00 | 8 | |
BEZ235 is a dual PI3K/mTOR inhibitor, effectively targeting p110 isoforms and mTOR complexes. It blocks ATP binding, reducing kinase activity and modulating cell proliferation and survival. | ||||||
BKM120 | 944396-07-0 | sc-364437 sc-364437A sc-364437B sc-364437C | 5 mg 10 mg 25 mg 50 mg | $173.00 $230.00 $275.00 $332.00 | 9 | |
BKM120 is an pan-PI3K inhibitor, acting on all p110 isoforms. It competes with ATP for binding to the kinase domain, leading to the inhibition of PI3K activity and its downstream signaling. | ||||||
ZSTK 474 | 475110-96-4 | sc-475495 | 5 mg | $75.00 | ||
ZSTK474 is a specific PI3K inhibitor, with a preference for the p110 isoforms. It blocks the ATP binding site of the enzyme, resulting in reduced kinase activity and altered cell signaling. | ||||||
PX-866 | 502632-66-8 | sc-396764 sc-396764A | 1 mg 5 mg | $146.00 $282.00 | ||
PX-866 is a synthetic derivative of wortmannin and acts as a potent inhibitor of PI3K, including the p110 subunit. It leads to the modulation of cellular growth and survival pathways. | ||||||
SF1126 | 936487-67-1 | sc-391584 sc-391584A | 5 mg 10 mg | $719.00 $1331.00 | 7 | |
SF1126 is a compound of LY294002, specifically designed to increase its bioavailability. It inhibits PI3K p110 isoforms by competing with ATP for binding to the kinase domain. | ||||||
CAL-101 | 870281-82-6 | sc-364453 | 10 mg | $189.00 | 4 | |
CAL-101, also known as Idelalisib, is a selective inhibitor of PI3Kδ, one of the p110 isoforms. It interferes with the ATP binding site, diminishing the enzyme’s activity and affecting cell proliferation and survival. | ||||||