2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  3. HDAC SHMT Apoptosis Reactive Oxygen Species (ROS) Ferroptosis
  4. HDAC11-IN-5

HDAC11-IN-5 是一种选择性强、效力高且具有口服活性 HDAC11 抑制剂，其 IC50 为 0.021 μM。HDAC11-IN-5 可提高急性髓系白血病 (AML) 细胞中底物 SHMT2 的脂肪酸酰化水平。HDAC11-IN-5 可诱导 AML 细胞发生细胞凋亡 (apoptosis)、G1 期细胞周期阻滞、铁死亡 (ferroptosis)、活性氧 (ROS) 产生以及终末髓系分化。HDAC11-IN-5 在 MLL-AF9 诱导的小鼠 AML 模型中表现出抗肿瘤活性。HDAC11-IN-5 可用于癌症研究，例如急性髓系白血病。

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

HDAC11-IN-5

HDAC11-IN-5 Chemical Structure

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

HDAC11-IN-5 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 SHMT 亚型特异性产品:

查看所有亚型
SHMT1 SHMT2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia[1].

IC50 & Target[1]

HDAC11

0.021 μM (IC50)

SHMT2

 

体外研究
(In Vitro)

HDAC11-IN-5 (Compound 25) 可强效抑制纯化的 HDAC11 蛋白，其 IC50 为 0.021 ± 0.005 μM，在浓度高达 10 μM 时对 HDAC1、HDAC6、HDAC7 或 HDAC8 无显著抑制作用[1]。
HDAC11-IN-5 (96 h) 可强效抑制 U937、OCI-AML2、THP-1 和 MOLM13 这四种 AML 细胞系的增殖，其 IC50 值分别为 6.3 μM、5.7 μM、5.4 μM 和 6.7 μM[1]。
HDAC11-IN-5 (10-20 μM; 6 h) 可在 U937 急性髓系白血病 (AML) 细胞中选择性抑制细胞内 HDAC11；正如 10 μM 作用 6 h 时 SHMT2 的脂肪酰化水平升高，以及 20 μM 作用 6 h 时组蛋白 H3 或 α-微管蛋白的乙酰化水平无显著变化所示[1]。
HDAC11-IN-5 (8 μM; 48 h) 可在 U937 和 OCI-AML2 急性髓系白血病 (AML) 细胞中强烈诱导细胞凋亡[1]。
HDAC11-IN-5 (8 μM; 48 h) 可在 U937 急性髓系白血病 (AML) 细胞中诱导 G1 期细胞周期阻滞[1]。
HDAC11-IN-5 (8 μM; 48 h) 可促进 U937 急性髓系白血病 (AML) 细胞的髓系分化，表现为 CD14 和 CD11b 的表达水平升高[1]。
HDAC11-IN-5 (8 μM; 48 h) 可诱导 U937 急性髓系白血病 (AML) 细胞发生铁死亡，表现为脂质过氧化水平、细胞活性氧 (ROS) 及细胞内 Fe2+ 水平升高[1]。
HDAC11-IN-5 (5-20 μM; 96 h) 在 U937、OCI-AML2 和 MLL-AF9 小鼠急性髓系白血病 (AML) 细胞中与 Ivosidenib (HY-18767) 表现出强烈的协同抗增殖活性[1]。

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

HDAC11-IN-5 相关抗体:

Western Blot Analysis[1]

Cell Line: U937 AML cells
Concentration: 10 μM (SHMT2 fatty acylation analysis); 20 μM (histone H3 and α-tubulin acetylation analysis)
Incubation Time: 6 h
Result: Significantly increased fatty acylation levels of SHMT2 (a specific HDAC11 substrate) at 10 μM for 6 h.
Had negligible effects on acetylation levels of histone H3 (a class I HDAC substrate) and α-tubulin (an HDAC6 substrate) at 20 μM for 6 h.

Apoptosis Analysis[1]

Cell Line: U937, OCI-AML2 AML cell lines
Concentration: 8 μM
Incubation Time: 48 h
Result: Significantly induced apoptosis in both U937 and OCI-AML2 cells.

Cell Differentiation Assay[1]

Cell Line: U937 AML cells
Concentration: 8 μM
Incubation Time: 48 h
Result: Significantly increased expression of the myeloid differentiation markers CD14 and CD11b in U937 cells, with a stronger effect than FT895.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-∞ Vss CL Tmax Cmax F
Mice[1] 5 mg/kg i.v. 3.74 h 613 ng·h/mL 14.87 L/kg 136 mL/min/kg / / /
Mice[1] 50 mg/kg p.o. 2.39 h 1273 ng·h/mL / / 0.25 h 812 ng/mL 20.8 %
体内研究
(In Vivo)

HDAC11-IN-5 (Compound 25) (50 mg/kg；灌胃；每日 1 次；连续 14 天) 可使 MLL-AF9 诱导的 AML 小鼠模型的外周血白血病细胞负荷降低，并显著延长其生存期；与 Ivosidenib (HY-18767) 联用时疗效进一步增强[1]。

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

Animal Model: C57BL/6 (6-week-old female, 20-22 g, tail vein injection of 1×105 MLL-AF9-GFP+ leukemic cells)[1]
Dosage: 50 mg/kg
Administration: I.g.,; once daily; 14 days
Result: Reduced the percentage of GFP+ leukemic cells in peripheral blood.
Significantly extended the survival of AML mice compared to vehicle control.
Reduced the percentage of GFP+ leukemic cells when combined with ivosidenib, with greater survival extension than either agent alone.
Caused no significant body weight loss prior to the moribund stage.
分子量

529.38

Formula

C24H25Cl2F3N4O2
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

HDAC11-IN-5 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:

HDAC11-IN-5HDACSHMTApoptosisReactive Oxygen Species (ROS)FerroptosisHistone deacetylasesSerine hydroxymethyltransferaseCD14CD11bG1 phase cell cycle arrestHDAC11terminal myeloid differentiationapoptosisMLL-AF9-induced mouse AML modelferroptosisSHMT2AML cellsInhibitorinhibitorinhibit

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：
HDAC11-IN-5
目录号：
HY-182019
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z