CG-200745

Modify Date: 2025-08-21 12:39:15

CG-200745 Structure
CG-200745 structure
Common Name CG-200745
CAS Number 936221-33-9 Molecular Weight 427.53700
Density 1.148±0.06 g/cm3 (20 °C, 760 mmHg) Boiling Point N/A
Molecular Formula C24H33N3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CG-200745


CG-200745 is a potent HDAC inhibitor, with IC50s of <3 μM for sensitive non-small cell lung cancer (NSCLC) cell lines. CG-200745 induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of proteins encoded by p53 target genes, MDM2 and p21 (Waf1/Cip1) in human prostate cancer cells[1]. CG-200745 attenuates phosphorylation of p38 MAPK in kidneys and it has a renoprotective effect by suppressing renal fibrosis and inflammation in a unilateral ureteral obstruction (UUO) mouse model[2].

 Names

Name 2-Octenediamide, N1-[3-(dimethylamino)propyl]-N8-hydroxy-2-[(1-naphthalenyloxy)methyl]-, (2E)
Synonym More Synonyms

 CG-200745 Biological Activity

Description CG-200745 is a potent HDAC inhibitor, with IC50s of <3 μM for sensitive non-small cell lung cancer (NSCLC) cell lines. CG-200745 induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of proteins encoded by p53 target genes, MDM2 and p21 (Waf1/Cip1) in human prostate cancer cells[1]. CG-200745 attenuates phosphorylation of p38 MAPK in kidneys and it has a renoprotective effect by suppressing renal fibrosis and inflammation in a unilateral ureteral obstruction (UUO) mouse model[2].
Related Catalog
Target

HDAC

p53

p38 MAP kinase

In Vitro CG-200745 (0-10 μM; 48 hours) reduces the Calu6 cells proliferation to 40% of untreated cells[1]. CG-200745 (3 μM; 1-24 hours) significantly increases Calu6 cells proportion in G2/M phase (69%)[1]. CG-200745 (0-10 μM; 1-24 hours) treatment with low concentration significantly increases the acetylation of histone H3 and H4 in Calu6 cells at various sites in a time-dependent manner up to 24 hours after treatment[1]. Cell Proliferation Assay[1] Cell Line: Calu6 cells Concentration: 0-10 μM Incubation Time: 48 hours Result: Reduced the cell proliferation to 40% of untreated cells. Cell Cycle Analysis[1] Cell Line: Calu6 cells Concentration: 3 μM Incubation Time: 1, 8, 12, 24 hours Result: Increased significantly cell proportion in G2/M phase (69%). Western Blot Analysis[1] Cell Line: Calu6 cells Concentration: 0-10 μM Incubation Time: 1, 4, 8, 12, 24 hours Result: Increased the acetylation of histone H3 and H4 at various sites in a time-dependent manner.
In Vivo CG-200745 (p.o.; 30 mg/kg/day; for 7 days) attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys[2]. Animal Model: Male 8-week-old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)[2] Dosage: 30 mg/kg Administration: P.o.; daily; for 7 days Result: Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys.
References

[1]. Chun SM, et al. Epigenetic modulation with HDAC inhibitor CG200745 induces anti-proliferation in non-small cell lung cancer cells. PLoS One. 2015 Mar 17;10(3):e0119379.

[2]. Choi HS, et al. Histone deacetylase inhibitor, CG200745 attenuates renal fibrosis in obstructive kidney disease. Sci Rep. 2018 Aug 1;8(1):11546.

 Chemical & Physical Properties

Density 1.148±0.06 g/cm3 (20 °C, 760 mmHg)
Molecular Formula C24H33N3O4
Molecular Weight 427.53700
Exact Mass 427.24700
PSA 90.90000
LogP 4.06050

 Synonyms

cg 200745
The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.