1798292-13-3
Chemical Structure
NVP-BHS345
- CAS No.: 1798292-13-3
- Formula:C25H20N6O
- Molecular Weight:420.47
InChIKey: WFCPNAZSGVZANE-UHFFFAOYSA-N
SMILES: N#CC(C)(C)C1=CC=C(N2C(N(C)C3=C2C4=CC(C5=CN=CN=C5)=CC=C4N=C3)=O)C=C1
Biological Activity: NVP-BHS345 is an ATP-competitive TORC1/TORC2 inhibitor with an IC50 of 1 μM for both targets in yeast. NVP-BHS345 acutely inhibits TORC1/TORC2 kinase activity, even in genetically engineered TOR1M2282T Saccharomyces cerevisiae strains. NVP-BHS345 also reduces the phosphorylation levels of Ser-232/Ser-233 sites in Sch9, Ypk1/Ypk2 and Rps6, and induces hyperphosphorylation of Slt2 and activation of the cell wall integrity pathway. NVP-BHS345 causes depolarization of the actin cytoskeleton, blocks fluid-phase endocytosis, prevents the accumulation of vacuolar lipophilic dyes, and regulates the phosphorylation levels of Ent1, Pan1, Prk1, Akl1 and other cellular proteins[1][2][3][4][5].
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NVP-BHS345 | NVP-BHS345 is an ATP-competitive TORC1/TORC2 inhibitor with an IC50 of 1 μM for both targets in yeast. NVP-BHS345 acutely inhibits TORC1/TORC2 kinase activity, even in genetically engineered TOR1M2282T Saccharomyces cerevisiae strains. NVP-BHS345 also reduces the phosphorylation levels of Ser-232/Ser-233 sites in Sch9, Ypk1/Ypk2 and Rps6, and induces hyperphosphorylation of Slt2 and activation of the cell wall integrity pathway. NVP-BHS345 causes depolarization of the actin cytoskeleton, blocks fluid-phase endocytosis, prevents the accumulation of vacuolar lipophilic dyes, and regulates the phosphorylation levels of Ent1, Pan1, Prk1, Akl1 and other cellular proteins. | |||||||||||||||||||||
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References
- [1]. Rispal D, et al. Target of Rapamycin Complex 2 Regulates Actin Polarization and Endocytosis via Multiple Pathways. The Journal of biological chemistry. 2015 Jun 12;290(24):14963-78. [Content Brief]
- [2]. Yerlikaya S, et al. TORC1 and TORC2 work together to regulate ribosomal protein S6 phosphorylation in Saccharomyces cerevisiae. Molecular biology of the cell. 2016 Jan 15;27(2):397-409. [Content Brief]
- [3]. Hurst V, et al. Loss of cytoplasmic actin filaments raises nuclear actin levels to drive INO80C-dependent chromosome fragmentation. Nature communications. 2024 Nov 15;15(1):9910. [Content Brief]
- [4]. Shimada K, et al. TORC2 inhibition triggers yeast chromosome fragmentation through misregulated Base Excision Repair of clustered oxidation events. Nature communications. 2024 Nov 15;15(1):9908. [Content Brief]
- [5]. Shimada K, et al. TORC2 signaling pathway guarantees genome stability in the face of DNA strand breaks. Molecular cell. 2013 Sep 26;51(6):829-39. [Content Brief]
