CG-1521 is a histone deacetylase ( HDAC ) inhibitor that stabilizes Ac-Lys373 P53, increases P21 levels and HDAC2 degradation. CG-1521 can inhibit proliferation, induce cell cycle arrest and apoptosis. CG-1521 promotes Bax translocation to the mitochondria and cleavage. CG-1521 downregulates KIF4, Aurora B and Nek2 protein expression and DNA synthesis. CG-1521 can be used for the research of prostate cancer and inflammatory breast cancer [1] [2] [3].
In Vitro, CG-1521 (7.5 μM; 0-72 h) upregulates p21, Gadd45a, and Wee1 and downregulates cyclin B1, Cks2, Cdc20, Plk1, Stk6, and Kntc2 in LNCaP cells[1]. CG-1521 (7.5 μM; 0-72 h) upregulates proapoptotic genes (Gadd153, Bnip3, Bnip3L, Pig3, Gdf15, p21B) and downregulates the antiapoptotic gene survivin in LNCaP cells[1]. CG-1521 (0-10 μM; 48 h) induces dose-dependent growth inhibition in SUM149PT and SUM190PT IBC cells[2]. CG-1521 (7.5 μM; 24-48 h) induces G1 arrest, apoptosis and modulates mRNA expression, apoptosis and modulates mRNA expressionin SUM149PT cells[2]. CG-1521 (5 μM; 24-48 h) induces G0/G1 arrest, apoptosis and modulates mRNA expression in SUM190PT cells[2]. CG-1521 (7.5 μM; 48 h) induces elongated midzone structures and abscission failure in SUM149PT cells[2]. CG-1521 (7.5 μM; 48-72 h) downregulates KIF4 protein expression and slightly reduces Aurora B protein expression in SUM149PT cells[2]. CG-1521 (7.5 μM; 24-48 h) slightly downregulates Nek2 protein expression in SUM149PT cells at 24 h, with recovery by 48 h[2]. CG-1521 (1-10 μM; 0-96 h) inhibits growth and induces G2/M arrest and apoptosis in LNCaP cells and induce G2/M arrest without apoptosis in PC-3 cells[3]. CG-1521 (7.5 μM; 1-24 h) induces sustained hyperacetylation of histones H3 and H4 and downregulates HDAC2 protein levels in LNCaP cells[3]. CG-1521 (7.5 μM; 1-48 h) stabilizes p53 acetylated at Lys373 and increases total p53 and P21 levels in LNCaP cells[3]. CG-1521 (7.5 μM; 1-48 h) induces Bax translocation from the cytosol to mitochondria and subsequent cleavage to t-Bax in LNCaP cells[3].
References:
[1]. Roy S, et al. Array-based analysis of the effects of trichostatin A and CG-1521 on cell cycle and cell death in LNCaP prostate cancer cells. Mol Cancer Ther. 2008;7(7):1931-1939.
[2]. Chatterjee N, et al. Molecular actions of the novel histone deacetylase inhibitor CG-1521 in models of inflammatory breast cancer[J]. 2014.
[3]. Roy S, et al. Histone deacetylase inhibitors differentially stabilize acetylated p53 and induce cell cycle arrest or apoptosis in prostate cancer cells. Cell Death Differ. 2005;12(5):482-491.
In Vitro, CG-1521 (7.5 μM; 0-72 h) upregulates p21, Gadd45a, and Wee1 and downregulates cyclin B1, Cks2, Cdc20, Plk1, Stk6, and Kntc2 in LNCaP cells[1]. CG-1521 (7.5 μM; 0-72 h) upregulates proapoptotic genes (Gadd153, Bnip3, Bnip3L, Pig3, Gdf15, p21B) and downregulates the antiapoptotic gene survivin in LNCaP cells[1]. CG-1521 (0-10 μM; 48 h) induces dose-dependent growth inhibition in SUM149PT and SUM190PT IBC cells[2]. CG-1521 (7.5 μM; 24-48 h) induces G1 arrest, apoptosis and modulates mRNA expression, apoptosis and modulates mRNA expressionin SUM149PT cells[2]. CG-1521 (5 μM; 24-48 h) induces G0/G1 arrest, apoptosis and modulates mRNA expression in SUM190PT cells[2]. CG-1521 (7.5 μM; 48 h) induces elongated midzone structures and abscission failure in SUM149PT cells[2]. CG-1521 (7.5 μM; 48-72 h) downregulates KIF4 protein expression and slightly reduces Aurora B protein expression in SUM149PT cells[2]. CG-1521 (7.5 μM; 24-48 h) slightly downregulates Nek2 protein expression in SUM149PT cells at 24 h, with recovery by 48 h[2]. CG-1521 (1-10 μM; 0-96 h) inhibits growth and induces G2/M arrest and apoptosis in LNCaP cells and induce G2/M arrest without apoptosis in PC-3 cells[3]. CG-1521 (7.5 μM; 1-24 h) induces sustained hyperacetylation of histones H3 and H4 and downregulates HDAC2 protein levels in LNCaP cells[3]. CG-1521 (7.5 μM; 1-48 h) stabilizes p53 acetylated at Lys373 and increases total p53 and P21 levels in LNCaP cells[3]. CG-1521 (7.5 μM; 1-48 h) induces Bax translocation from the cytosol to mitochondria and subsequent cleavage to t-Bax in LNCaP cells[3].
References:
[1]. Roy S, et al. Array-based analysis of the effects of trichostatin A and CG-1521 on cell cycle and cell death in LNCaP prostate cancer cells. Mol Cancer Ther. 2008;7(7):1931-1939.
[2]. Chatterjee N, et al. Molecular actions of the novel histone deacetylase inhibitor CG-1521 in models of inflammatory breast cancer[J]. 2014.
[3]. Roy S, et al. Histone deacetylase inhibitors differentially stabilize acetylated p53 and induce cell cycle arrest or apoptosis in prostate cancer cells. Cell Death Differ. 2005;12(5):482-491.