2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis MDM-2/p53 Aurora Kinase NEKs DNA/RNA Synthesis Bcl-2 Family
  4. CG-1521

CG-1521 is a histone deacetylase (HDAC) inhibitor that stabilizes Ac-Lys373 P53, increases P21 levels and HDAC2 degradation. CG-1521 can inhibit proliferation, induce cell cycle arrest and apoptosis. CG-1521 promotes Bax translocation to the mitochondria and cleavage. CG-1521 downregulates KIF4, Aurora B and Nek2 protein expression and DNA synthesis. CG-1521 can be used for the research of prostate cancer and inflammatory breast cancer.

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CG-1521

CG-1521 Chemical Structure

CAS No. : 674767-29-4

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CG-1521 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Aurora Kinase Aurora A Aurora B Aurora C

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NEK1 NEK2 NEK4 NEK6 NEK7

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

CG-1521 is a histone deacetylase (HDAC) inhibitor that stabilizes Ac-Lys373 P53, increases P21 levels and HDAC2 degradation. CG-1521 can inhibit proliferation, induce cell cycle arrest and apoptosis. CG-1521 promotes Bax translocation to the mitochondria and cleavage. CG-1521 downregulates KIF4, Aurora B and Nek2 protein expression and DNA synthesis. CG-1521 can be used for the research of prostate cancer and inflammatory breast cancer[1][2][3].

IC50 & Target[3][2]

HDAC-2

 

Aurora B

 

NEK2

 

Bax

 

In Vitro

CG-1521 (7.5 μM; 0-72 h) upregulates p21, Gadd45a, and Wee1 and downregulates cyclin B1, Cks2, Cdc20, Plk1, Stk6, and Kntc2 in LNCaP cells[1].
CG-1521 (7.5 μM; 0-72 h) upregulates proapoptotic genes (Gadd153, Bnip3, Bnip3L, Pig3, Gdf15, p21B) and downregulates the antiapoptotic gene survivin in LNCaP cells[1].
CG-1521 (0-10 μM; 48 h) induces dose-dependent growth inhibition in SUM149PT and SUM190PT IBC cells[2].
CG-1521 (7.5 μM; 24-48 h) induces G1 arrest, apoptosis and modulates mRNA expression, apoptosis and modulates mRNA expressionin SUM149PT cells[2].
CG-1521 (5 μM ; 24-48 h) induces G0/G1 arrest, apoptosis and modulates mRNA expression in SUM190PT cells[2].
CG-1521 (7.5 μM; 48 h) induces elongated midzone structures and abscission failure in SUM149PT cells[2].
CG-1521 (7.5 μM; 48-72 h) downregulates KIF4 protein expression and slightly reduces Aurora B protein expression in SUM149PT cells[2].
CG-1521 (7.5 μM; 24-48 h) slightly downregulates Nek2 protein expression in SUM149PT cells at 24 h, with recovery by 48 h[2].
CG-1521 (1-10 μM; 0-96 h) inhibits growth and induces G2/M arrest and apoptosis in LNCaP cells and induce G2/M arrest without apoptosis in PC-3 cells[3].
CG-1521 (7.5 μM; 1-24 h) induces sustained hyperacetylation of histones H3 and H4 and downregulates HDAC2 protein levels in LNCaP cells[3].
CG-1521 (7.5 μM; 1-48 h) stabilizes p53 acetylated at Lys373 and increases total p53 and P21 levels in LNCaP cells[3].
CG-1521 (7.5 μM; 1-48 h) induces Bax translocation from the cytosol to mitochondria and subsequent cleavage to t-Bax in LNCaP cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CG-1521 Related Antibodies

Cell Cycle Analysis[2]

Cell Line: SUM149PT, SUM190PT inflammatory breast cancer (IBC) cell lines
Concentration: 7.5 μM (SUM149PT); 5 μM (SUM190PT)
Incubation Time: 48 h
Result: Induced accumulation of SUM149PT cells in the G1 phase with a reduction in G2/M phase (no change in S phase).
Induced accumulation of SUM190PT cells in G0/G1 phase with almost complete loss of S phase cells.

Apoptosis Analysis[2]

Cell Line: SUM149PT, SUM190PT inflammatory breast cancer (IBC) cell lines
Concentration: 7.5 μM (SUM149PT); 5 μM (SUM190PT)
Incubation Time: 48 h
Result: Induced a significant increase in apoptotic cells (fragmented DNA) in both cell lines.
Showed higher sensitivity to apoptosis induction in SUM190PT cells compared to SUM149PT cells.

Immunofluorescence[2]

Cell Line: SUM149PT, SUM190PT inflammatory breast cancer (IBC) cell lines
Concentration: 7.5 μM (SUM149PT); 3 μM (SUM190PT)
Incubation Time: 48 h
Result: Induced elongated midbody structures (indicative of abscission failure) and a significant increase in their frequency in SUM149PT cells.
Showed no such effect in SUM190PT cells.

Western Blot Analysis[2]

Cell Line: SUM149PT inflammatory breast cancer (IBC) cell line
Concentration: 7.5 μM
Incubation Time: 24, 48, 72 h
Result: Caused a significant and sustained decrease in KIF4 protein levels after 48 h of treatment.
Caused a slight reduction in Aurora B protein expression over the 72 h time course.
Caused a slight decrease in overall Nek2 protein expression after 24 h, which was restored by 48 h.

Western Blot Analysis[3]

Cell Line: LNCaP human prostate cancer cells
Concentration: 7.5 μM
Incubation Time: 1, 3, 6, 8, 12, 24 h
Result: Induced hyperacetylation of both isoforms of histone H3 and H4 as early as 1 h, which was sustained up to 24 h.
Induced stabilization of p53 acetylated at Lys373/Lys382 and total P53 and P21 as early as 3 h, with levels maintained for at least 24 h.
Showed Bax levels decreasing in S100 and increasing in NNMF over time.
Caused a significant decrease in HDAC2 protein levels.
Molecular Weight

215.25

Formula

C13H13NO2
CAS No.
Appearance

Solid

SMILES

C(=C/C=C/C=C/C(NO)=O)\C1=CC=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 95.71%

COA (242 KB)

Handling Instructions (2659 KB)
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CG-1521 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CG-1521674767-29-4CG1521CG 1521HDACApoptosisMDM-2/p53Aurora KinaseNEKsDNA/RNA SynthesisBcl-2 FamilyHistone deacetylasesNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesLNCaP cellsbreast cancerSUM149PTprostate cancerSUM190PTPC-3Baxhistone deacetylaseAc-Lys373 p53P21HDAC2Inhibitorinhibitorinhibit

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