| Name | TGX-221 |
| Description | TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment. |
| Cell Research | For measurement of proliferation, cells are seeded in triplicate in 96-well culture plates and incubated overnight to allow cell attachment. The cells are incubated with TGX-221 for 24, 48, and 72 hours. At designated time intervals, cells are quantified by a crystal violet staining-based colorimetric assay. Briefly, cells are fixed by addition of 100 μl of 2.5% glutaraldehyde solution and incubated at room temperature for 30 minutes. Plates are washed three times by submersion in PBS solution. Plates are air-dried and stained by addition of 100 μL of 0.1% solution of crystal violet dissolved in deionized water and incubated for 20 minutes at room temperature, excess dye is removed by extensive washing with deionized water, and plates are air-dried prior to bound dye solubilization in 100 μL of 10% acetic acid. The optical density of dye extracts is measured directly in plates using a microplate reader at 570 nm.(Only for Reference) |
| Kinase Assay | Lipid kinase activity : IC50 values are measured using a standard lipid kinase activity with PI as a substrate. (i)100 μM cold ATP is used instead of 10 μM, (ii) the DMSO concentration is 1%, and (iii) [γ-33P]ATP is used instead of [γ-32P]ATP. The TLC plates are quantified using a phosphorimager screen. The reported IC50 values are determined by non-linear regression analysis on the basis of at least three independent experiments repeated across multiple preparations of recombinant protein. |
| In vitro | In mouse models, TGX-221 has been shown to enhance blood flow, prolonging tail bleeding and renal bleeding time. |
| In vivo | In J774.2 macrophages, TGX-221 inhibits the phosphorylation of Ser473 on PKB induced by insulin. It also impedes platelet-ECC (extracorporeal circulation) interactions, platelet aggregation, and the binding between platelets and granulocytes in an ECC model. Furthermore, in the PC3 cells, TGX-221 (at concentrations of 0.2-20 μM) can suppress cell proliferation and reduce the activity of the p110β subunit of PI3K. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (137.2 mM), Sonication is recommended.
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| Keywords | TGX 221 | Phosphoinositide 3-kinase | TGX-221 | Inhibitor | inhibit | PI3K |
| 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-Colorectal Cancer Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Oxidation-Reduction Compound Library |
United States
