CG-200745
Modify Date: 2024-01-05 22:50:07
CG-200745 structure
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Common Name | CG-200745 | ||
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| 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-200745CG-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]. |
| Name | 2-Octenediamide, N1-[3-(dimethylamino)propyl]-N8-hydroxy-2-[(1-naphthalenyloxy)methyl]-, (2E) |
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| Synonym | More Synonyms |
| 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]. |
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| 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 |
| 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 |
| cg 200745 |