CGK-733


Catalog No. size PriceQuantity
M104-2S 2mg solid $79
M104-10S 10mg solid $312

Description

Product Information
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month
Chemical Name: 2,2-diphenyl-N-(2,2,2-trichloro-1-(3-(4-fluoro-3-nitrophenyl)thioureido)ethyl)acetamide
Solubility: 10 mM in DMSO
CAS#: 905973-89-9
Purity: >98%
Formula: C23H18CI3FN4O3S
Molecular Weight: 555.84

Biological Activity:


CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.

How to use:

In Vitro:  CGK733 (4.2 ng/μL-12.5 ng/μL) enhances taxol-induced cytotoxicity in HBV-positive HCC cells. CGK733 (4.2 ng/μL) accelerates the formation of multinucleated cells and promotes the exit of mitosis in taxol-treated HBV-positive HCC cells[1]. CGK733 (10 μM) causes the loss of cyclin D1 through the ubiquitin-dependent proteasomal degradation pathway in MCF-7 and T47D breast cancer cell lines. CGK733 (0.6-40 μM) shows inhibitory activities against proliferation of LnCap prostate cancer cells, HCT116 colon cancer cells, MCF-7 and T47D estrogen receptor positive breast cancer cells, and MDA-MB436 ER negative breast cancer cells. Moreover, CGK733 inhibits proliferation of non-transformed mouse BALB/c 3T3 embryonic fibroblast cells. In addition, CGK733 (10 μM) inhibits MCF-7 proliferation, and the effect can not be suppressed by pan-caspase inhibition[2]. CGK733 (10 μM) results in 1.6-fold increase in ATM reporter activity in HEK-293 cells[3].

In Vivo: CGK733 (25 mg/kg, i.p.) increases the ATM reporter activity (reports inactivation of ATM kinase activity) compared to control mice, with 2.4-fold, 3.1-fold, and 1.3-fold changes at 1, 4, and 8 hours, respectively[3].

Reference:

[1]. Wang H, et al. CGK733 enhances multinucleated cell formation and cytotoxicity induced by taxol in Chk1-deficient HBV-positive hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2012 May 25;422(1):103-8.
[2]. Alao JP, et al. The ATM and ATR inhibitors CGK733 and caffeine suppress cyclin D1 levels and inhibit cell proliferation. Radiat Oncol. 2009 Nov 10;4:51.
[3]. Williams TM, et al. Molecular imaging of the ATM kinase activity. Int J Radiat Oncol Biol Phys. 2013 Aug 1;86(5):969-77.

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