1. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  2. HDAC Autophagy Apoptosis
  3. HDAC-IN-36

HDAC-IN-36 (compound 23 g) 是一种口服有效的HDAC (组蛋白去乙酰化酶)抑制剂,其 IC50 为 11.68 nM (HDAC6)。HDAC-IN-36 可促进细胞凋亡 (apoptosis),自噬 (autophagy) 和抑制迁移。HDAC-IN-36 具有抗肿瘤和抗转移活性,可用于乳腺癌研究。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

HDAC-IN-36 Chemical Structure

HDAC-IN-36 Chemical Structure

CAS No. : 2482992-54-9

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research[1].

IC50 & Target

HDAC6

11.68 nM (IC50)

HDAC10

13.24 nM (IC50)

HDAC3

79.17 nM (IC50)

HDAC1

86.93 nM (IC50)

HDAC2

97.32 nM (IC50)

HDAC8

378.2 nM (IC50)

HDAC4

>1000 nM (IC50)

HDAC5

>1000 nM (IC50)

HDAC7

>1000 nM (IC50)

HDAC9

>1000 nM (IC50)

HDAC11

>1000 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-36 (compound 23 g) (0-10, 24 h) exhibits good antiproliferative activity in MDA-MB-231 cells, promotes the acetylation of α-Tubulin and HSP90[1].
HDAC-IN-36 (0-10, 24 h) induces apoptosis in MDA-MB-231 cells in a dose-dependent manner, and mainly induces mitochondrial-dependent apoptosis[1].
HDAC-IN-36 (0-10, 24 h) inhibits MDA-MB-231 cells migration in a dose-dependent manner, increases the expression of E-cadherin and decreases the expression of MMP-2 obviously[1].
HDAC-IN-36 (0-10, 24 h) induces noteworthy autophagy, increases the expression of Beclin1, LC3II and decreases the expression of SQSTM1/p62[1].

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

Cell Viability Assay

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Exhibited good anti-proliferative activity in MDA-MB-231 cells, with IC50 of 1.32 ± 0.13 μM, increased the acetylation level of intracellular proteins, and promoted the acetylation of α-Tubulin and HSP90.

Apoptosis Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced apoptosis in MDA-MB-231 cells in a dose-dependent manner.

Cell Autophagy Assay

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced noteworthy autophagy with increased aggregation of LC3 puncta.

Western Blot Analysis

Cell Line: MDA-MB-231 cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Mainly induced mitochondrial-dependent apoptosis, up-regulated the expression of Bax and downregulated the expression of Bcl-2, and increased the cleavage of caspase3, caspase8 and caspase9; increased the expression of E-cadherin and decreased the expression of MMP-2 obviously; increased the expression of Beclin1, LC3II and decreased the expression of SQSTM1/p62.
体内研究
(In Vivo)

HDAC-IN-36 (compound 23 g) (Zebrafish tumor xenograft model; 0-5 μg/mL, 3 days) shows potent anti-tumor and anti-metastatic activity, and improves in vivo anti-tumor efficacy[1].
HDAC-IN-36 (Beagles, 20 mg/kg, Orally, once) shows a significant improvement in pharmacokinetic parameters[1].
Pharmacokinetic Parameters of HDAC-IN-36 in male Beagles[1].

Parameters 23g (20 mg/kg)
T1/2 (h) 1.24 ± 0.21
Tmax (h) 0.79 ± 0.33
Cmax (μg/L) 120.36 ± 15.53
AUC0-t (μg/L∗h) 1275.35 ± 70.17
AUC0-∞ (μg/L∗h) 1289.40 ± 88.91

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

Animal Model: Zebrafish (MDA-MB-231-derived xenograft model, Wild-type AB strain)[1]
Dosage: 0, 2.5, 5 μg/mL
Administration: 3 days
Result: Inhibited tumor formation and migration in a dose-dependent manner, and improved in vivo anti-tumor efficacy.
Animal Model: Beagles (female, 8-10 kg, n = 4)[1]
Dosage: 20 mg/kg (dissolved 0.5% sodium carboxyl methyl cellulose (CMC-Na) aqueous solution)
Administration: Orally, once (Pharmacokinetic Analysis)
Result: Showed a significant improvement in pharmacokinetic parameters with T1/2 value of 1.24 h.
分子量

537.65

Formula

C29H39N5O5

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
  • 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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
HDAC-IN-36
目录号:
HY-146684
需求量: