TGX-221
Catalog No.S1169
Molecular Weight(MW): 364.44
TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α.
5 Customer Reviews
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A p110β-selective antagonist rescues increased protein synthesis in synaptic fractions from Fmr1 KO mice and in LCLs from a patient with FXS. (A–C) Treatment of synaptoneurosomes with TGX-221 (1 μmol/L, 30 min) reduces p110β-specific PI3K activity and phosphorylation of the downstream target AKT in both WT and Fmr1 KO SNS, shown by a radioactive PI3K assay and phosphoAkt- specific western blot-ting (A). (B) Quantification of PI3K activity using a competitive ELISA showed a significant reduction in PI3K activity in both genotypes after treatment [ n = 4, 2-way ANOVA, *P (genotype) = 0.0086, * P (treatment) = 0.0087, P (interaction) = 0.7154]. (C) Densitometric quantification of phosphoAkt-specific western blots showed a significant effect of treatment (C, n = 4, 2-way ANOVA, *P (treatment) = 0.0005, P (genotype) =0.372, P (interaction) = 0.4894).
Mol Med 2012 18, 336-45. TGX-221 purchased from Selleck.
(E) TGX-221 treatment (0.5 μmol/L, 30 min) of control and FXS LCLs reduces PI3K activity as shown by a radioactive PI3K assay of p110β-specific immunoprecipitates from LCL lysates, and decreases PI3K/mTOR down-stream signaling as shown by strongly reduced phosphorylation of S6 independently of the genotype. (F, G) Quantification demonstrates a significant, dose-dependent effect of TGX-221 treatment on PI3K activity [F, competitive ELISA, n = 4, 2-way ANOVA, *P (genotype) = 0.0079, *P (treatment) = 0.0258, P (interaction) = 0.9418], and on S6 phosphorylation[G, ELISA, n = 4, 2-way ANOVA, *P (genotype) = 0.013), *P (treatment) < 0.0001, P (interaction) = 0.195].
Mol Med 2012 18, 336-45. TGX-221 purchased from Selleck.
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(H) 30-min pretreatment of LCLs with 0.5 μmol/L TGX-221 significantly reduces protein synthesis in FXS patient cells [n = 40, 4 independent experiments, 2-way ANOVA: * P (genotype) < 0.001, * P (treatment) = 0.005, * P (interaction) < 0.001, Bon-ferroni post hocanalyses, * P = 0.001, #P = 0.002, ≠P = 0.02]. Example images are shown on the left: upper panel: signal for newly synthesized proteins (red), lower panel: overlay with tubulin staining (green). Scale bar is 20 μm. (I) Increasing concentrations of TGX-221 (5 μmol/L and 10 μmol/L) further reduce protein synthesis rates in FXS LCLs to healthy control levels.
Mol Med 2012 18, 336-45. TGX-221 purchased from Selleck.
We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
Saraswati Sukumar of Johns Hopkins University School of Medicine. TGX-221 purchased from Selleck.
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Breast cancer cells were pretreated with 100ng/ml EGF for 15 min and then treated with the indicated concentrations of TGX-221 for 24 hours.
Dr. Zhang of Tianjin Medical University. TGX-221 purchased from Selleck.
Purity & Quality Control
Choose Selective PI3K Inhibitors
Biological Activity
| Description | TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, 1000-fold more selective for p110β than p110α. | |||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. [1] TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. [2] A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform. [3] |
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| Cell Data |
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| In vivo | As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups. [4] |
Protocol
| Kinase Assay:[1] |
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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. |
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| Cell Research:[3] |
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| Animal Research:[3] |
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Solubility (25°C)
| In vitro | DMSO | 12 mg/mL (32.92 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents individually and in order: 1% DMSO+30% polyethylene glycol+1% Tween 80 |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 364.44 |
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| Formula | C21H24N4O2 |
| CAS No. | 663619-89-4 |
| Storage | powder |
| Synonyms | N/A |
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