CG-200745 (Synonyms: CG-200745) |
| Catalog No.GC35668 |
CG-200745 (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. CG-200745 inhibits deacetylation of histone H3 and tubulin. CG-200745 induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. CG-200745 enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-Fluorouracil (5-FU; ). CG-200745 induces apoptosis and has anti-tumour effects.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 936221-33-9
Sample solution is provided at 25 µL, 10mM.
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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]. HDAC p38 MAP kinase p53
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
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]
[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.
| Cas No. | 936221-33-9 | SDF | |
| Synonyms | CG-200745 | ||
| Canonical SMILES | O=C(NCCCN(C)C)/C(COC1=C2C=CC=CC2=CC=C1)=C/CCCCC(NO)=O | ||
| Formula | C24H33N3O4 | M.Wt | 427.54 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.339 mL | 11.6948 mL | 23.3896 mL |
| 5 mM | 0.4678 mL | 2.339 mL | 4.6779 mL |
| 10 mM | 0.2339 mL | 1.1695 mL | 2.339 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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