2. Cell Cycle/DNA Damage Epigenetics Apoptosis Vitamin D Related/Nuclear Receptor
  3. HDAC Apoptosis PARP Bcl-2 Family Androgen Receptor
  4. MHY219

MHY219 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂，其 IC50 为 0.276 μM。MHY219 可抑制总 HDAC 酶活性，增强组蛋白 H3 和 H4 的高乙酰化水平。MHY219 可诱导癌细胞周期阻滞、细胞凋亡 (apoptosis) 并抑制细胞增殖。MHY219 可提高 PARP 的裂解水平、Bax 与 cytochrome c 的表达量，雄激素受体 (androgen receptor) 的表达，同时降低 Bcl-2 的表达。MHY219 可用于前列腺癌的相关研究。

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MHY219

MHY219 Chemical Structure

CAS No. : 1326750-61-1

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MHY219 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 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

查看 Bcl-2 Family 亚型特异性产品:

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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

MHY219 is a histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM. MHY219 inhibits total HDAC enzyme activity, increases histone H3 and H4 hyperacetylation. MHY219 induces cance cells phase arrest, apoptosis and inhibits proliferationin. MHY219 increases cleavage of PARP, Bax, cytochrome c levels, androgen receptor expression and decreases Bcl-2 expression. MHY219 can be used for the research of prostate cancer[1].

IC50 & Target[1]

Bax

 

Bcl-2

 

体外研究
(In Vitro)

MHY219 (0.001-10 μM; 30 min) 可在无细胞荧光分析中强效抑制总 HDAC 酶活性，其 IC50 为 0.276 μM[1]。
MHY219 (0.05-5 μM; 24-48 h) 可抑制 DU145、LNCaP 和 PC3 人前列腺癌细胞的增殖，其作用 48 h 的 IC50 值分别为 0.36 μM、0.97 μM 和 5.12 μM，同时可诱导 DU145 细胞发生形态学改变[1]。
MHY219 (0.1-1 μM; 48 h) 可增强人前列腺癌细胞 DU145、LNCaP 和 PC3 中组蛋白 H3 和 H4 的高乙酰化水平，并下调特定的 I 类和 II 类 HDAC 亚型[1]。
MHY219 (0.1-1 μM; 48 h) 可诱导 DU145 细胞出现亚 G1 期累积与 G2/M 期阻滞、LNCaP 细胞出现 G1 期阻滞、PC3 细胞出现 G2/M 期阻滞，同时伴随细胞周期调控蛋白表达的相应改变[1]。
MHY219 (0.1-1 μM; 24-48 h) 可通过线粒体介导的通路诱导人前列腺癌细胞 DU145 发生凋亡，但不会诱导 LNCaP 或 PC3 细胞凋亡[1]。
MHY219 (0.5-1 μM; 48 h) 可上调人前列腺癌 DU145 细胞中雄激素受体的表达，但对 LNCaP 或 PC3 细胞中的 AR 表达无影响[1]。

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

MHY219 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: DU145, LNCaP, PC3 human prostate cancer cell lines
Concentration: 0.05, 0.1, 0.3，0.5, 0.8, 1, 3, 5 μM
Incubation Time: 24 h; 48 h
Result: Reduced cell viability in a concentration-dependent manner across all three cell lines.
At 48 h, reached IC50 values of 0.36 μM for DU145 cells, 0.97 μM for LNCaP cells, and 5.12 μM for PC3 cells.
Induced cytoplasmic enlargement and cellular flattening in DU145 cells after 48 h treatment.

Western Blot Analysis[1]

Cell Line: DU145, LNCaP, PC3 human prostate cancer cell lines
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 48 h
Result: Increased histone H3 and H4 hyperacetylation in all three cell lines; in PC3 cells, hyperacetylation of H3 was low at 0.5 μM but pronounced at 1 μM.
Down-regulated levels of all class I HDACs (1, 2, 3, 8) and most class II HDACs (except HDAC5, 6, 10) in DU145 cells.
Down-regulated HDAC1, 2, 3, and HDAC6 in LNCaP cells.
Down-regulated class I HDACs (1, 2, 3) and HDAC4 in PC3 cells.

Cell Cycle Analysis[1]

Cell Line: DU145, LNCaP, PC3 human prostate cancer cell lines
Concentration: 0.1, 0.5, 1 μM
Incubation Time: 48 h
Result: Significantly increased the sub-G1 fraction in a concentration-dependent manner, induced G2/M phase arrest, and decreased the S phase population in DU145 cells.
Induced G1 phase arrest in a concentration-dependent manner in LNCaP cells.
Induced G2/M phase arrest in PC3 cells.
Decreased cyclin A1 and cyclin B1, increased cyclin D1, and increased p21 expression in DU145 cells.
Decreased cyclin D1 and increased p21 expression in LNCaP cells.
Increased cyclin D1 without affecting p21 in PC3 cells.

Apoptosis Analysis[1]

Cell Line: DU145, LNCaP, PC3 human prostate cancer cell lines
Concentration: 0.1, 0.5, 1 μM (Annexin V/PI, WB); 1 μM (DAPI staining)
Incubation Time: 24 h; 48 h (Annexin V/PI, WB); 48 h (DAPI staining)
Result: Increased late apoptosis in a concentration-dependent manner at 48 h and increased cleavage of PARP, increased Bax and cytochrome c release, and decreased Bcl-2 expression in DU145 cells.
Showed increased condensed or fragmented chromatin (apoptotic nuclei) in DU145 cells via DAPI staining.
Did not induce apoptotic cell death in LNCaP or PC3 cells at tested concentrations.

Western Blot Analysis[1]

Cell Line: DU145, LNCaP, PC3 human prostate cancer cell lines
Concentration: 0.5, 1 μM
Incubation Time: 48 h
Result: Markedly increased AR expression in DU145 cells.
Did not affect AR expression in LNCaP or PC3 cells.
分子量

355.43

Formula

C20H25N3O3
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

MHY219 相关分类

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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:

MHY2191326750-61-1MHY 219MHY-219HDACApoptosisPARPBcl-2 FamilyAndrogen ReceptorHistone deacetylasespoly ADP ribose polymeraseDU145LNCaPprostate cancer cellsp27histone deacetylasep21class I HDACsapoptosishistone H3PC3Inhibitorinhibitorinhibit

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