1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
    MAPK/ERK Pathway
    Autophagy
  2. HDAC
    MDM-2/p53
    p38 MAPK
    Autophagy
  3. CG-200745

CG-200745 

Cat. No.: HY-16138
Handling Instructions

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. 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.

For research use only. We do not sell to patients.

CG-200745 Chemical Structure

CG-200745 Chemical Structure

CAS No. : 936221-33-9

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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].

IC50 & 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.
Molecular Weight

427.54

Formula

C₂₄H₃₃N₃O₄

CAS No.

936221-33-9

SMILES

O=C(NCCCN(C)C)/C(COC1=C2C=CC=CC2=CC=C1)=C/CCCCC(NO)=O

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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