2. Cell Cycle/DNA Damage Epigenetics Apoptosis Cytoskeleton
  3. HDAC Apoptosis Histone Acetyltransferase Microtubule/Tubulin Caspase
  4. HDAC-IN-99

HDAC-IN-99 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂，IC50 为 37.73 nM，对 HDAC1 (IC50 = 48.09 nM)、HDAC2 (IC50 = 300.28 nM) 和 HDAC6 (IC50 = 9.16 nM) 表现出强的抑制效力。HDAC-IN-99 可抑制 HDAC 的酶活性，在多种癌细胞系中发挥广谱抗增殖活性。HDAC-IN-99 诱导结肠癌细胞的 S 期细胞周期阻滞和细胞凋亡 (apoptosis)，升高组蛋白 H3、组蛋白 H4 和 α-微管蛋白 (Tubulin) 的乙酰化水平、上调 p21 表达以及 caspase-3 的剪切。HDAC-IN-99 在结肠癌异种移植模型中展现出抗肿瘤活性。HDAC-IN-99 可用于结肠癌的研究。

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HDAC-IN-99

HDAC-IN-99 Chemical Structure

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HDAC-IN-99 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

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

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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-99 is a histone deacetylase (HDAC) inhibitor with an IC50 of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC50 = 48.09 nM), HDAC2 (IC50 = 300.28 nM) and HDAC6 (IC50 = 9.16 nM). HDAC-IN-99 inhibits the enzymatic activity of HDAC and exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer[1].

IC50 & Target[1]

HDAC1

48.09 nM (IC50)

HDAC2

300.28 nM (IC50)

HDAC6

9.16 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-99 (Z16) 可强效抑制 HDAC1 (IC50 = 48.09 nM)、HDAC2 (IC50 = 300.28 nM) 和 HDAC6 (IC50 = 9.16 nM) 的活性，对 HDAC6 的选择性较 I 类 HDAC 高出 15 倍以上，而对 HDAC8 的活性极低 (IC50 = 37.77 μM)[1]。
HDAC-IN-99 可抑制多种癌细胞系的生长，其对不同细胞系的 IC50 值分别为 0.05 μM (HeLa)、0.07 μM (HCT116)、0.1 μM (SKOV3)、0.04 μM (MDA-MB-231) 和 0.02 μM (Jurkat)[1]。
HDAC-IN-99 (0-250 nM, 48 h) 可在 HCT116 细胞中诱导浓度依赖性的 S 期细胞周期阻滞和细胞凋亡，同时伴随组蛋白 H3、组蛋白 H4 和 α-微管蛋白的乙酰化水平升高、p21 表达上调以及 caspase-3 的剪切[1]。

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

HDAC-IN-99 相关抗体:

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 0, 40, 100, 250
Incubation Time: 48 h
Result: Induced concentration-dependent S-phase cell cycle arrest and apoptosis in HCT116 cells, accompanied by increased acetylation of histone H3, histone H4, and α-tubulin, upregulation of p21, and cleavage of caspase-3.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax T1/2 CL Vz AUC0-t AUC0-∞ F
Rat[1] 2 mg/kg i.v. 2880.00 ng/mL 0.08 h 1.28 h 1.45 L/h/kg 2.63 L/kg 1667.93 ng·h/mL 1750.26 ng·h/mL /
Rat[1] 20 mg/kg i.p. 2040.83 ng/mL 2.00 h 5.48 h 0.96 L/h/kg 7.24 L/kg 16130.71 ng·h/mL 17274.30 ng·h/mL 98.70 %
Mice[1] 2 mg/kg i.v. 1245.26 ng/mL 0.08 h 0.66 h 6.25 L/h/kg 5.77 L/kg 405.27 ng·h/mL 425.22 ng·h/mL /
Mice[1] 20 mg/kg i.p. 1248.09 ng/mL 1.40 h 1.25 h 4.83 L/h/kg 8.53 L/kg 4226.64 ng·h/mL 4092.64 ng·h/mL 96.25 %
体内研究
(In Vivo)

HDAC-IN-99 (腹腔注射，每日一次， 30-40 mg/kg) 在 HCT116 结肠癌异种移植模型中呈现剂量依赖性抗肿瘤功效[1]。

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

Animal Model: BALB/c nude (female, 4-6 weeks old, SPF grade)[1]
Dosage: 30 mg/kg; 40 mg/kg
Administration: i.p.; q.d.
Result: Achieved a tumor growth inhibition (TGI) rate of 26.32%.
Achieved a tumor growth inhibition (TGI) rate of 45.80%.
Caused no significant changes in body weight during the study.
分子量

448.35

Formula

C23H25BN4O3S
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-99 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-99HDACApoptosisHistone AcetyltransferaseMicrotubule/TubulinCaspaseHistone deacetylasesHATsHAThistone deacetylase inhibitorcolon cancerHeLa cellsHCT116 cellsSKOV3 cellsMDA-MB-231cellsapoptosisBALB/c nude mice
Inhibitorinhibitorinhibit

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