2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Cytoskeleton Apoptosis
  3. HDAC Carbonic Anhydrase Microtubule/Tubulin PARP Apoptosis Bcl-2 Family Caspase
  4. HDAC-IN-91

HDAC-IN-91 是 HDAC (HDAC1 的 IC50 = 134.22 nM，HDAC2 的 IC50 = 66.29 nM)、碳酸酐酶 (CA) (CA IX 的 KI = 72.03 nM，XII 的 KI = 50.76 nM) 和微管蛋白聚合 (IC50 = 2.56 μM) 的多重抑制剂。HDAC-IN-91 抑制 PARP1 并增加 Bax/Bcl-2 比率。HDAC-IN-91 将细胞周期阻滞在 G2/M 期，并通过线粒体凋亡 (apoptosis) 激活机制诱导细胞凋亡 (apoptosis)。HDAC-IN-91 可以通过抑制微管蛋白聚合发挥强大的细胞毒活性。HDAC-IN-91 可用于乳腺癌、结直肠癌、宫颈癌和肺癌研究。

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HDAC-IN-91

HDAC-IN-91 Chemical Structure

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HDAC-IN-91 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 Carbonic Anhydrase 亚型特异性产品:

查看所有亚型
CA CA I CA Ⅱ CA IX CA XII

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:

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

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-91 is a multiple inhibitor of HDAC (IC50 = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (Ki = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC50 = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research[1].

IC50 & Target[1]

HDAC1

134.22 nM (IC50)

HDAC2

66.29 nM (IC50)

CA IX

72.03 nM (Ki)

CA XII

50.76 nM (Ki)

Bax

 

Bcl-2

 

Caspase-9

 

Caspase-7

 

体外研究
(In Vitro)

HDAC-IN-91 (Compounds 6e) 对 MCF7、Hela、HCT116 和 A549 细胞表现出细胞毒性，IC50 分别为 1.40 μM、2.22 μM、1.57 μM 和 2.54 μM[1]。

HDAC-IN-91 对 HDAC 亚型 3、4、6 和 8 表现出良好的抑制活性，IC50 范围为 100-900 nM[1]。

HDAC-IN-91 (1.40 μM, 48 小时) 通过干扰细胞有丝分裂并最终诱导细胞凋亡来抑制 MCF-7 细胞的生长[1]。

HDAC-IN-91 (1.40 μM, 48 小时) 通过增加 MCF-7 细胞中的 Bax/Bcl-2 比例以及 caspase-9 和 caspase-7 水平来诱导细胞凋亡[1]。

HDAC-IN-91 (1.40 μM, 48 小时) 在 MCF-7 细胞中具有潜在的 PARP1 抑制活性[1]。

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

HDAC-IN-91 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.40 μM
Incubation Time: 48 h
Result: Reduced the cell population in the S phase (DNA synthesis phase) to 22.3%, reduced the G0-G1 phase (non-proliferating cell ratio) to 31.6%.
Increased the proportion in the G2/M phase to 46.1, caused significant cell death, and increased the number of cells in the Sub-G1 phase to 42.09%.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1.40 μM
Incubation Time: 48 h
Result: Induced apoptosis in breast cancer cells with an apoptotic rate of 26.75 and induced necrotic cell death of 15.36.

ELISA Assay[1]

Cell Line: MCF-7 cells
Concentration: 1.40 μM
Incubation Time: 48 h
Result: Increased Bax protein levels to 391.6 Pg/mL, decreased Bcl-2 protein levels to 2.11 ng/mL, increased the Bax/Bcl-2 ratio, increased Caspase-9 and Caspase-7 protein levels to 13.57 ng/mL and 2.62 ng/mL, respectively, and decreased PARP1 to 73.92 ng/mL, suggesting potential PARP1 inhibitory activity.
分子量

517.39

Formula

C23H21BrN2O5S
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

HDAC-IN-91 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

HDAC-IN-91HDACCarbonic AnhydraseMicrotubule/TubulinPARPApoptosisBcl-2 FamilyCaspaseHistone deacetylasesCarbonate dehydratasepoly ADP ribose polymerase Inhibitor,MCF7 cellsInhibitorinhibitorinhibit

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