Compound 401|cas 168425-64-7|DC Chemicals

Cas No.:	168425-64-7
Chemical Name:	2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one
Synonyms:	COMPOUND 401;2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one;2-morpholin-4-ylpyrimido[2,1-a]isoquinolin-4-one;Compound-401;HMS3229D15;2-(Morpholin-4-yl)pyrimido[2,1-a]isoquinolin-4-one;2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one;4H-PyriMido[2,1-a]isoquinolin-4-one, 2-(4-Morpholinyl)-;Compound401;2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one;HMS3413H20;HMS3677H20;BCP04303;BDBM50159620;AK546312;M2537;B7337;4H-Pyri
SMILES:	O1C([H])([H])C([H])([H])N(C2=C([H])C(N3C([H])=C([H])C4=C([H])C([H])=C([H])C([H])=C4C3=N2)=O)C([H])([H])C1([H])[H]
Formula:	C₁₆H₁₅N₃O₂
M.Wt:	281.3092
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.

In Vitro:

Compound 401 is a potent inhibitor of DNA-PK (IC50=0.28 μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC50=5.3 μM) but not p110α/p85α PI3K (IC50>100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr389 and Akt Ser473, respectively). By contrast, there is no direct inhibition of Akt Thr308 phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5 μM or 10 μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1-/- fibroblasts is inhibited in the presence of Compound 401, but TSC1+/+ cells are resistant[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7235	PIK-75	PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.
DC3100	NU-7441 (KU-57788)	NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM.
DC2085	Compound 401	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 FRAP (mTOR) (IC50 = 5.3 µM).