Cas No.: | 1448427-02-8 |
Chemical Name: | 1-(4-((4-methyl-3,4-dihydroquinoxalin-1(2H)-yl)sulfonyl)phenyl)pyrrolidin-2-one |
SMILES: | N(C1=CC=C(S(N2C3=C(C=CC=C3)N(C)CC2)(=O)=O)C=C1)1CCCC1=O |
Formula: | C19H21N3O3S |
M.Wt: | 371.455 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Wnt-p53 inhibitor compound 2 is a novel inhibitor targets both Wnt signaling and ATM/p53, potently inhibits Wnt transcription (IC50=11 nM) and p53 transcription (EC50=1.9 nM); decreases HCT-116 CRC cell viability (IC50=10 nM) and proliferation (IC50=8 nM), decreases DLD-1, SW480 and 10.1 cancer cell viability (IC50=12, 27 and 41 nM) and proliferation (IC50=18,15 and 13 nM); compound 2 potently activates apoptosis of HCT-116, DLD-1 and SW480 cells (EC50=13, 15 and 18 nM) in a p53-dependent manner; inhibits cell migration and invasion in HCT-116 at 20-200 nM, also modulates mitotic stress signaling, leading to both inhibition of Wnt responsiveness and stabilization and activation of p53 to cause cell cycle arrest; induces cell death and inhibits tumor growth in mouse xenografts (20 mg/kg/day, i.p.), without acute cytotoxicity nor toxicity. |