TG100-115 (CAS 677297-51-7)
See product citations (1)
QUICK LINKS
TG100-115 inhibits PI 3-kinase p110 gamma and PI 3-kinase p110 delta (PI3Kgamma and -delta), with IC50 of 83 and 235 nM, respectively. TG100-115 is not active for PI3Kalpha and -beta, with IC50 of 1.2 and 1.3 mM. TG100-115 (10 muM) interrupts other VEGF signaling pathways, such as those that culminate in VE-cadherin phosphorylation. In HUVECs, TG100-115 (10 muM) inhibits the VEGF-induced increase of total level of VE-cadherin. TG100-115 inhibits VEGF mediated phosphorylation of mTOR, also known as FRAP, and p70S6 kinase, both of which are downstream of PI3K. TG100-115 (125 nM to 10 muM) also inhibits FGF-stimulated phosphorylation of Akt. TG100-115 is a promising small molecule with significant implications in medicine and biochemistry. Derived from pteridine, an aromatic ring structure occurring in natural compounds, TG100-115 has garnered recent attention due to its potential applications. Researchers have extensively examined its interactions with diverse biological molecules.
TG100-115 (CAS 677297-51-7) References
- Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. | Doukas, J., et al. 2006. Proc Natl Acad Sci U S A. 103: 19866-71. PMID: 17172449
- Isoform-selective PI3K inhibitors as novel therapeutics for the treatment of acute myocardial infarction. | Doukas, J., et al. 2007. Biochem Soc Trans. 35: 204-6. PMID: 17371238
- Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. | Min, S., et al. 2010. Antimicrob Agents Chemother. 54: 254-8. PMID: 19884365
- The effect of lopinavir/ritonavir and darunavir/ritonavir on the HIV integrase inhibitor S/GSK1349572 in healthy participants. | Song, I., et al. 2011. J Clin Pharmacol. 51: 237-42. PMID: 20489027
- In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. | Kobayashi, M., et al. 2011. Antimicrob Agents Chemother. 55: 813-21. PMID: 21115794
- Effect of atazanavir and atazanavir/ritonavir on the pharmacokinetics of the next-generation HIV integrase inhibitor, S/GSK1349572. | Song, I., et al. 2011. Br J Clin Pharmacol. 72: 103-8. PMID: 21342217
- S/GSK1349572, a new integrase inhibitor for the treatment of HIV: promises and challenges. | Lenz, JC. and Rockstroh, JK. 2011. Expert Opin Investig Drugs. 20: 537-48. PMID: 21381981
- Pharmacokinetics of the HIV integrase inhibitor S/GSK1349572 co-administered with acid-reducing agents and multivitamins in healthy volunteers. | Patel, P., et al. 2011. J Antimicrob Chemother. 66: 1567-72. PMID: 21493648
- Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). | Hare, S., et al. 2011. Mol Pharmacol. 80: 565-72. PMID: 21719464
- Dolutegravir (S/GSK1349572) exhibits significantly slower dissociation than raltegravir and elvitegravir from wild-type and integrase inhibitor-resistant HIV-1 integrase-DNA complexes. | Hightower, KE., et al. 2011. Antimicrob Agents Chemother. 55: 4552-9. PMID: 21807982
- Carbamoyl pyridone HIV-1 integrase inhibitors 3. A diastereomeric approach to chiral nonracemic tricyclic ring systems and the discovery of dolutegravir (S/GSK1349572) and (S/GSK1265744). | Johns, BA., et al. 2013. J Med Chem. 56: 5901-16. PMID: 23845180
- Phosphoinositide 3-kinase δ/γ inhibition does not prevent concanavalin A-induced hepatitis. | Liu, Y., et al. 2013. Mol Med Rep. 8: 1305-10. PMID: 23969545
- Dolutegravir(DTG, S/GSK1349572) combined with other ARTs is superior to RAL- or EFV-based regimens for treatment of HIV-1 infection: a meta-analysis of randomized controlled trials. | Jiang, J., et al. 2016. AIDS Res Ther. 13: 30. PMID: 27617024
- Identification of TG100-115 as a new and potent TRPM7 kinase inhibitor, which suppresses breast cancer cell migration and invasion. | Song, C., et al. 2017. Biochim Biophys Acta Gen Subj. 1861: 947-957. PMID: 28161478
- Sorafenib-loaded hydroxyethyl starch-TG100-115 micelles for the treatment of liver cancer based on synergistic treatment. | Li, G. and Zhao, L. 2019. Drug Deliv. 26: 756-764. PMID: 31357893
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TG100-115, 5 mg | sc-364634 | 5 mg | $245.00 | |||
TG100-115, 100 mg | sc-364634A | 100 mg | $1836.00 |