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 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂，可稳定 Ac-Lys373 P53，增加 P21 水平并促进 HDAC2 降解。CG-1521 可抑制增殖，诱导细胞周期阻滞和凋亡 (apoptosis)。CG-1521 促进 Bax 向线粒体转位并引发其切割。CG-1521 下调 KIF4、Aurora B 和 Nek2 蛋白表达及 DNA 合成。CG-1521 可用于前列腺癌和炎性乳腺癌的研究。

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CG-1521

CG-1521 Chemical Structure

CAS No. : 674767-29-4

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CG-1521 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

查看 NEKs 亚型特异性产品:

查看所有亚型
NEK1 NEK2 NEK6 NEK7

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

CG-1521 (7.5 μM；0-72 h) 在 LNCaP 细胞中上调 p21、Gadd45a 和 Wee1，同时下调 cyclin B1、Cks2、Cdc20、Plk1、Stk6 和 Kntc2[1]。
CG-1521 (7.5 μM；0-72 h) 在 LNCaP 细胞中上调促凋亡基因 (Gadd153、Bnip3、Bnip3L、Pig3、Gdf15、p21B)，并下调抗凋亡基因 survivin[1]。
CG-1521 (0-10 μM；48 h) 在 SUM149PT 和 SUM190PT IBC 细胞中诱导剂量依赖性生长抑制[2]。
CG-1521 (7.5 μM；24-48 h)，在 SUM149PT 细胞中诱导 G1 期阻滞、凋亡，并调节 mRNA 表达[2]。
CG-1521 (5 μM ; 24-48 h) 诱导 SUM190PT 细胞发生 G0/G1 期阻滞、凋亡，并调节 mRNA 表达[2]。
CG-1521 (7.5 μM；48 h) 在 SUM149PT 细胞中诱导形成伸长的中间区结构并导致细胞分裂终末失败[2]。
CG-1521 (7.5 μM；48-72 h) 在 SUM149PT 细胞中下调 KIF4 蛋白表达，且轻微降低 Aurora B 蛋白表达[2]。
CG-1521 (7.5 μM；24-48 h) 在 24 h 时轻微下调 SUM149PT 细胞中的 Nek2 蛋白表达，但在 48 h 时出现恢复[2]。
CG-1521 (1-10 μM；0-96 h) 抑制 LNCaP 细胞的增殖并诱导 G2/M 期阻滞和凋亡，而在 PC-3 细胞中仅诱导 G2/M 期阻滞而不引起凋亡[3]。
CG-1521 (7.5 μM；1-24 h) 在 LNCaP 细胞中诱导组蛋白 H3 和 H4 的持续高乙酰化，并下调 HDAC2 蛋白水平[3]。
CG-1521 (7.5 μM；1-48 h) 能稳定 LNCaP 细胞中在 Lys373 位乙酰化的 p53，并增加总 p53 和 P21 水平[3]。
CG-1521 (7.5 μM；1-48 h) 在 LNCaP 细胞中诱导 Bax 从胞质转移到线粒体，并随后切割为 t-Bax[3]。

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

CG-1521 相关抗体:

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.
分子量

215.25

Formula

C13H13NO2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CG-1521 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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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