Palomid 529 (P529) Chemical Structure
BEZ235 (NVP-BEZ235)is a dual ATP-competitive phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM,respectively.
Deforolimus (Ridaforolimus) is a small-molecule inhibitor of mTOR.
Perifosine is an Akt inhibitor. the antiproliferative properties of perifosine with an IC50 of 0.6–8.9 µM.
PI-103 is a potent, cell-permeable, ATP-competitive PI3K family member inhibitor with IC50 of 2, 8, 20, 26, 48, 83, 88, 150 nM for DNA-PK, p110α, mTORC1, PI3-KC2β, p110δ, mTORC2, p110β, and p110γ, respectively.
Rapamycin also known as Sirolimus & Rapamune is an mTOR inhibitor. Rapamycin Sirolimus inhibits cell motility by suppression of mTOR-mediated pathways.
Temsirolimus (Torisel) is a mTOR inhibitor.
MK-2206 is a highly selective inhibitor of Akt1, Akt2 and Akt3 with IC50 of 8 nM, 12 nM and 65 nM, respectively.
GSK690693 is a pan-Akt kinase inhibitor,IC50 of Akt 1, 2, and 3 at 2, 13, and 9 nM respectively.
Akt inhibitor
Everolimus (RAD001) also known as SDZ-RAD, Certican, Zortress and Afinitorm is an mTOR inhibitor available at Selleck with IC50 of 0.63 nM.
Palomid 529 (P529) is a novel PI3K/Akt/mTOR inhibitor with a GI50 of <35 μM in the NCI-60 cell lines panel. Palomid 529 (P529) inhibits the TORC1 and TORC2 complexes and shows both inhibition of Akt signaling and mTOR signaling similarly in tumor and vasculature. Palomid 529 (P529) inhibits tumor growth, angiogenesis, and vascular permeability. However, Palomid 529 (P529) has the additional benefit of blocking pAktS473 signaling consistent with blocking TORC2 in all cells and thus bypassing feedback loops that lead to increased Akt signaling in some tumor cells. Palomid 529 (P529) inhibited both VEGF-driven (IC50 = 20 nM) and bFGF-driven (IC50 = 30 nM) endothelial cell proliferation and retained the ability to induce endothelial cell apoptosis. In addition, Palomid 529 (P529) significantly enhanced the antiproliferative effect of radiation in prostate cancer cells (PC-3). [1][2][3]
| Molecular Weight (WM): | 406.43 |
|---|---|
| Formula: | C24H22O6 |
| CAS No.: | 914913-88-5 |
| Synonyms: |
P529
|
| Dissolve in (25°C): | DMSO ≥81mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Palomid529 for 3h,followed by 20-minute stimolation of 100ng/ml EGF. |
After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of Palomid529 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.
Data independently produced by Dr. Zhang of Tianjin Medical University Palomid 529 (P529) purchased from Selleck
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