Compound 401 CAS: 168425-64-7
MF: C16H15N3O2
MW: 281.3
A selective inhibitor of DNA-PK and FRAP.

Compound 401 (CAS 168425-64-7)

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Ansökan Compound 401 is a selective inhibitor of DNA-PK and FRAP
CAS Nr: 168425-64-7
Renhet: >95%
Molekylvikt: 281.3
Molekylär formel: C16H15N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (FRAP) (IC50 = 5.3 μM). Compound 401 exhibits much reduced or no activity against 43 other commonly studied kinases, including PI 3-K, ATM, and ATR. Compound 401 has been shown to induce apoptosis and inhibit FRAP-dependent growth in TSC1-/- murine embryo fibroblasts.


Konferenser

Ballou, L.M., et al. 2007. J. Biol. Chem. 282, 24463. Griffin, R.J., et al. 2005. J. Med. Chem. 48, 569

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), and ethanol (5 mM).
LAGRING :
Store at 4° C
Melting Point :
187.05° C (Predicted)
Boiling Point :
456.92° C at 760 mmHg (Predicted)
Density :
1.36 g/cm3 (Predicted)
Refractive Index :
n20D 1.70 (Predicted)
IC50 :
DNA-PK: IC50 = 0.28 µM; mTOR: IC50 = 5.3 µM; FK506 binding protein 12: IC50 = 5.3 µM (human); PI 3-K: IC50 = >100 µM; ATM: IC50 = >100 µM; ATR: IC50 = >100 µM
pK Values :
pKb: 1.01
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
MDL Number :
MFCD10568147
SMILES :
C1COCCN1C2=CC(=O)[N+]3=C(N2)C4=CC=CC=C4C=C3

Download SDS (MSDS)

Certificate of Analysis

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Compound 401 (CAS 168425-64-7)  Produkt Citat

See how others have used Compound 401 (CAS 168425-64-7). Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 23373904  Shepelev, MV. et al. 2013. Mol. Pharm. 10: 931-9.

PMID: # 17562705  Ballou, LM. et al. 2007. J. Biol. Chem. 282: 24463-24470.

PMID: # 12941142  Tamai, R. et al. 2003. Immunology. 110: 66-72.

PMID: # 1937825  Wang, MH. et al. 1991. Infect. Immun. 59: 4655-4664.

Citations 1 to 4 of 4 total
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