| Name | A66 |
| Description | A66 is a specific and effective p110α inhibitor(IC50=32 nM). |
| Kinase Assay | IC50 values are evaluated using the PI3K (human) HTRF Assay. p85α/p110δ is obtained from Invitrogen. All other isoforms are produced in-house by co-expressing full-length human p85α with the indicated human full-length catalytic subunit containing a histidine tag at the N-terminus to allow purification. The PI3Ks are titrated and used at a concentration between their EC65-EC80 values. PI3K activity in immunoprecipitates is assayed using an antibody to the N-SH2 (N-Src homology 2) domain of p85α. Assays for other lipid kinases and protein kinases are performed by the National Centre for Protein Kinase Profiling and Invitrogen Drug Discovery Services[1]. |
| In vitro | In male CD1 mice, A66 (10 mg/kg) increased glucose production during the pyruvate tolerance test. In SK-OV-3 tumor tissues, A66 (100 mg/kg) effectively reduced the phosphorylation of Akt/PKB and p70 S6 kinase, inhibiting tumor cell growth. |
| In vivo | A66 significantly inhibits the oncogenic forms of p110α, such as p110αE545K (IC50=30 nM) and p110αH1047R (IC50=43 nM), effectively reducing their activity. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 1 mg/mL (2.54 mM)
DMSO : 60 mg/mL (152.47 mM), Sonication is recommended.
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| Keywords | Phosphoinositide 3-kinase | inhibit | PI3K | Inhibitor | A66 | A-66 | A 66 |
| Inhibitors Related | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | GDC0084 | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Neuronal Differentiation Compound Library | Oxidation-Reduction Compound Library |
United States
