2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. HDAC-IN-84

HDAC-IN-84 (compound 4a) 是一种强效的 HDAC 抑制剂，HDAC1，HDAC2，HDAC3，HDAC6，HDAC8 和 HDAC11 的 IC50 值分别为 0.0045, 0.015, 0.013, 0.038, 5.8 和 26 μM。HDAC-IN-84 能有效抑制白血病细胞的增殖而不引起毒性。

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

HDAC-IN-84 Chemical Structure

HDAC-IN-84 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

HDAC-IN-84 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-84 (compound 4d) is a potent HDAC inhibitor, with IC50 values of 0.0045, 0.015, 0.013, 0.038, 5.8 and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC11, respectively. HDAC-IN-84 effectively inhibits the proliferation of leukemia cells without causing toxicity[1].

IC50 & Target

HDAC1

0.0045 μM (IC50)

HDAC2

0.015 μM (IC50)

HDAC-3

0.013 μM (IC50)

HDAC4

>100 μM (IC50)

HDAC6

0.038 μM (IC50)

HDAC8

5.8 μM (IC50)

HDAC11

26 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-84 (95min) 抑制 HDAC1, HDAC2, HDAC3, HDAC4, HDAC6, HDAC8 and HDAC11 的IC50 值分别为 0.0045, 0.015, 0.013, >100, 0.038, 5.8 和 26 μM [1]。
HDAC-IN-84 (0.005-25 μM, 72 h) 抑制 HL60，HPBALL 和 K562 细胞，IC50 分别为 76.8，110.6 和 180.8 nM[1]。
HDAC-IN-84 (0.25 μM, 48 h) 导致显著的 α-tubulin 乙酰化 和 HDAC6 更多的 PARP 蛋白裂解[1]。
HDAC-IN-84 (0.25 μM, 48 h) 促进 HL60 细胞凋亡[1].
HDAC-IN-84 (0.15-0.2 μM, 24 h) 诱导 HL60 细胞的细胞周期阻滞[1]。
HDAC-IN-84 (2.5, 50 nM, 1 μM, 24 h) 在 37°C，24 h 内检测的人血浆中表现出优异的稳定性[1]。
HDAC-IN-84 (2.5, 50 nM, 1 μM, 48 h) 与血浆蛋白结合，在观察到的浓度范围内平均结合率为 99.0%，无浓度依赖性[1]。
HDAC-IN-84 (0-1 μM) 抑制 MV4-11 细胞的 IC50 0.036 μM，与 Vorinosta (HY-10221) 相比，效力增加了 7 倍以上[1]。
HDAC-IN-84 (0-10 μM, 72 h) 和 Vorinosta (HY-10221) 以浓度依赖性方式影响 C1498 细胞的生长，IC50 0.425 和 1.06 μM[1]。
HDAC-In-84 与 Vorinostatas 体外药代动力学数据的比较

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

HDAC-IN-84 相关抗体:

Apoptosis Analysis[1]

vorinostatas HDAC-IN-84
log D 1.46 1.47
plasma stability/t1/2 75 min >24 h
KB/P 2.0 1.26
plasma protein binding 71% 99%
microsomal stability/t1/2( clearance category) 60 min 35.9 min
Cell Line: HL60 cells
Concentration: 0.25 μM
Incubation Time: 48 h
Result: Induced Apoptosis, leading to cytotoxic impacts on leukemia cells.

Cell Viability Assay[1]

Cell Line: K562, HL60, HPBALL cells
Concentration: 0.005-25 μM
Incubation Time: 72 h
Result: Inhibited HL60, HPBALL, and K562 cells with IC50s of 76.8, 110.6 and 180.8 nM respectively.

Western Blot Analysis[1]

Cell Line: HL60 cells
Concentration: 0.25μM
Incubation Time: 48 h
Result: Resulted in notable α-tubulin acetylation (indicating effective inhibition) of HDAC6.
Resulted in higher PARP cleavage (indicator of apoptosis induction).

Cell Cycle Analysis[1]

Cell Line: HL60 cells
Concentration: 0.15, 0.2 μM
Incubation Time: 24 h
Result: Induced cell cycle arrest in leukemia cells.
体内研究
(In Vivo)

HDAC-IN-84 (10 mg/kg, 腹腔注射, 一天一次, 14 天) 抑制临床前白血病异种移植小鼠 (NSG) 模型中 MV4-11 和C1498 细胞的生长[1]。
HDAC-IN-84 (10 mg/kg, i.p.) 在三只 C57BL/6 小鼠中半衰期为 0.35 h[1]。
HDAC-IN-84 (20 mg/kg, i.p., daily, 21 days) 在同种异体移植白血病模型中显示出明显较低的白血病负担，在体重上没有显著差异。
根据给 HDAC-IN-84 药前和给药后的实际采血时间计算出来血药浓度的非房室分析 (NCA) 药代动力学参数 Pharmacokinetic Parameters/sub>)

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

variable mouse 1 mouse 2 mouse 3 mean [±SD] vorinostat vorinostat
intraperitoneal 10 mg/kg per oral 50 mg/kg
Cmax (ng/mL) 1490 1030 1230 1250[±232] 501 580
Tmax (h) 0.25 0.25 0.25 0.25[±0] na 0.08
AUClast (h・ng/mL) 523 396 480 466[±65] 619 347
t1/2 0.275 0.554 0.227 0.352[±0.177] 0.75 0.8
Animal Model: preclinical leukemic xenograft mouse (NSG) model. Each mouse received 0.5 × 106 MV4-11 luc-GFP+ leukemic cells. After confirmation of tumor engraftment via monitoring bioluminescence-based in vivo imaging system (IVIS)[1] .
Dosage: 10 mg/kg
Administration: i.p., daily, 42 days
Result: Significantly suppressed the in vivo growth of MV4-11 leukemia cells as compared to the vehicle control.
Exhibited a minor (not significant) reduction in body weight.
Animal Model: Allograft leukemia model. In this model, leukemia is established by injecting (C57BL/6) derived murine AM L(C1498) cells by intravenous injection in immunocompetent wildtpye (C57BL/6) mice[1] .
Dosage: 20 mg/kg
Administration: i.p., daily, 21 days
Result: Exhibited significantly lower leukemia burden after the second treatment cycle, with this difference becoming more pronounced by day 19.
No significant differences in body weight were observed during the treatment course.
分子量

379.43

Formula

C17H21N3O5S
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-84 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-84HDACApoptosisHistone deacetylasesDNA methylationleukemiaHDAC1HDAC2HDAC3HDAC4HDAC6HDAC8HDAC11Inhibitorinhibitorinhibit

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-84
目录号：
HY-170379
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