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Cjioo(Shanghai) biotechnology co., LTD(expird)

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Cjioo(Shanghai) biotechnology co., LTD(expird)

Business Type:Lab/Research institutions

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Year Established:
2015
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Cjioo(Shanghai) biotechnology co., LTD(expird)

Country: China (Mainland)

Business Type:Lab/Research institutions

KU-0063794

CAS NO.938440-64-3

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Keywords

  • KU-0063794
  • 938440-64-3
  • 99% KU-0063794

Quick Details

  • ProName: KU-0063794
  • CasNo: 938440-64-3
  • Molecular Formula: C25H31N5O4
  • Application: 938440-64-3
  • DeliveryTime: in stock
  • ProductionCapacity: 100g Metric Ton/Day
  • Purity: 99%
  • LimitNum: 1 Gram

Superiority

In stock ,If you need HNMR\HPLC,please contact us!

Details

Compared with the mTOR inhibitor PP242, KU-0063794 exhibits higher specificity for mTOR, as being inactive against PI3Ks or 76 other kinases. In HEK-293 cells, KU-0063794 at 30 nM is sufficient to rapidly ablate S6K1 activity by blocking the phosphorylation of the hydrophobic motif (Thr389) and subsequently the phosphorylation of the T-loop residue (Thr229). In case of IGF1 stimulation of serum-starved HEK-293 cells, 300 nM of KU-0063794 is needed to inhibit the S6K1 activity by ~90%. KU-0063794 at 100-300 nM also completely inhibits the amino-acid-induced phosphorylation of S6K1 and S6 protein. Similar to S6K1, KU-0063794 inhibits the phosphorylation of mTORC1 at Ser2448 and mTORC2 at Ser2481 in a dose-dependent and time-dependent manner. In the presence of serum or following IGF1 stimulation, KU-0063794 induces a dose-dependent inhibition of the activity and phosphorylation of Akt at Ser473 and unexpected Thr308 as well as the phosphorylation of the Akt substrates PRAS40 at Thr246, GSK3α/GSK3β at Ser21/Ser9 and Foxo-1/3a at Thr24/Thr32. KU-0063794 but not rapamycin inhibits SGK1 activity and Ser422 phosphorylation as well as its physiological substrate NDGR1 in a dose-dependent manner, to the same extent as S6K1 and Akt phosphorylation, whereas KU-0063794 dose not inhibit phorbol ester induced ERK or RSK phosphorylation and RSK activation. Compared with rapamycin, KU-0063794 exhibits more significant potency to induce the complete dephosphorylation of 4E-BP1 at Thr37, Thr46 and Ser65. KU-0063794 inhibits cell growth of both wild-type and mLST8-deficient MEFs and induces a G1 cell cycle arrest, more significantly than rapamycin.

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