SML0382

KU 0063794

≥98% (HPLC)

• Synonym(s): rel-5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morp holinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
• Empirical Formula (Hill Notation): C₂₅H₃₁N₅O₄
• CAS Number: 938440-64-3
• Molecular Weight: 465.54
• NACRES: NA.77
• PubChem Substance ID: 329825382
• UNSPSC Code: 12352200
• MDL number: MFCD11977741
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: >2 mg/mL (warmed)
• storage temp.: 2-8°C
• SMILES string: COc1ccc(cc1CO)-c2ccc3c(nc(nc3n2)N4C[C@H](C)O[C@H](C)C4)N5CCOCC5
• InChI: 1S/C25H31N5O4/c1-16-13-30(14-17(2)34-16)25-27-23-20(24(28-25)29-8-10-33-11-9-29)5-6-21(26-23)18-4-7-22(32-3)19(12-18)15-31/h4-7,12,16-17,31H,8-11,13-15H2,1-3H3/t16-,17+
• InChI key: RFSMUFRPPYDYRD-CALCHBBNSA-N

Description

Application

KU 0063794 has been used:

• as a mammalian target of rapamycin (mTOR) inhibitor to study the effects of follicular stimulating hormone (FSH) in mTOR phosphorylation and vascular cell adhesion molecule-1 (VCAM-1) expression in human umbilical vascular endothelial cells (HUVECs)
• as a mTOR inhibitor to treat effector memory (EM) CD8⁺ T cells for metabolic flux analysis
• as an autophagy inducer to demonstrate the utility of p62 and LC3B-II quantification in HEK293T cells and primary cultures of rat neurons and astrocytes using time-resolved fluorescence resonance energy transfer (TR-FRET)

Biochem/physiol Actions

KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR) (IC₅₀ ~10 nM for both mTORC1 and mTORC2) that inhibits both mTORC1 and mTORC2 in vitro and in vivo (IC₅₀ ~10 nM for both mTORC1 and mTORC2). KU 0063794 does not significantly inhibit 76 other protein kinases tested as well as seven lipid kinases including PI3K and AKT.

KU 0063794 is a potent and selective inhibitor of mammalian target of rapamycin (mTOR); inhibits both mTORC1 and mTORC2 in vitro and in vivo.

KU 0063794 induces autophagy. It is cell-permeant and suppresses activation and hydrophobic motif phosphorylation of protein kinase B (Akt), p70 ribosomal S6 kinase (S6K) and serum and glucocorticoid protein kinase (SGK).

Features and Benefits

This compound is featured on the PKB/Akt page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable