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Enzymes for Research, Diagnostic and Industrial Use

CGK 733

Cat No.
CEI-0938
Description
CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
CAS No.
905973-89-9
Molecular Weight
555.84
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Targets
ATM, ATR
IC50
200 nM; 200 nM
Molecular Formula
C23H18Cl3FN4O3S
Chemical Name
Benzeneacetamide, α-phenyl-N-[2,2,2-trichloro-1-[[[(4-fluoro-3-nitrophenyl)amino]thioxomethyl]amino]ethyl]-
Solubility
DMSO 100 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL
In vitro
CGK733 is able to confer robust growth to senescent cells that have ceased proliferation. Senescence-associated β-galactosidase (SA–β-gal) activity disappears in CGK733-treated cells. CGK733 shows greater potency in inhibiting ATM/ATR than LY294002 (IC50, ~5 μM for ATM and ATR), a pan-inhibitor of PI3K and PIKKs. CGK733 (30 μM) treated for 24h causes ~60% cell death in senescent MCF-7 cells.CGK733 (20 μM) induces the loss of cyclin D1 via the ubiquitin- dependent proteasomal degradation pathway in MCF-7 and T47D breast cancer cell lines. CGK733 at concentrations ranging from 0.6- 40 μM, inhibits proliferation of MCF-7 and T47D estrogen receptor (ER) positive breast cancer cells, MDA-MB436 ER negative breast cancer cells, LnCap pros-tate cancer cells and HCT116 colon cancer cells. Furthermore, CGK733 also suppresses proliferation of non- transformed mouse BALB/c 3T3 embryonic fibroblast cells. The CGK733-mediated inhibition of proliferation is dose dependent and significant at doses as low as 2.5 μM.
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