CG-1521
Based on 1 Customer Validation
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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- 純度: 95.71%
- CAS 番号: 674767-29-4
- 分子式: C13H13NO2
- 分子量:215.25
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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HDAC-2 |
Aurora B |
NEK2 |
Bax |
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.
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Cell Line:SUM149PT, SUM190PT inflammatory breast cancer (IBC) cell lines
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Concentration:7.5 μM (SUM149PT); 5 μM (SUM190PT)
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Incubation Time:48 h
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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.
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Cell Line:SUM149PT, SUM190PT inflammatory breast cancer (IBC) cell lines
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Concentration:7.5 μM (SUM149PT); 5 μM (SUM190PT)
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Incubation Time:48 h
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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.
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Cell Line:SUM149PT, SUM190PT inflammatory breast cancer (IBC) cell lines
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Concentration:7.5 μM (SUM149PT); 3 μM (SUM190PT)
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Incubation Time:48 h
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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.
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Cell Line:SUM149PT inflammatory breast cancer (IBC) cell line
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Concentration:7.5 μM
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Incubation Time:24, 48, 72 h
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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.
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Cell Line:LNCaP human prostate cancer cells
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Concentration:7.5 μM
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Incubation Time:1, 3, 6, 8, 12, 24 h
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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.
化学情報
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CAS 番号 674767-29-4
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性状 Solid
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分子量 215.25
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分子式 C13H13NO2
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Color Light yellow to yellow
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SMILES
C(=C/C=C/C=C/C(NO)=O)\C1=CC=CC=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (274 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Roy S, et al. Array-based analysis of the effects of trichostatin A and CG-1521 on cell cycle and cell death in LNCaP prostate cancer cells. Mol Cancer Ther. 2008;7(7):1931-1939. [Content Brief]
[3]. Roy S, et al. Histone deacetylase inhibitors differentially stabilize acetylated p53 and induce cell cycle arrest or apoptosis in prostate cancer cells. Cell Death Differ. 2005;12(5):482-491. [Content Brief]
Calculators
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