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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.

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CG-200745 Chemical Structure

Cas No.: 936221-33-9

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Sample solution is provided at 25 µL, 10mM.

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Background

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.

Chemical Properties

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

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