2. Epigenetics Apoptosis
  3. Histone Acetyltransferase c-Myc
  4. P300-IN-6

P300-IN-6 是一种具有口服活性的组蛋白乙酰转移酶 (histone acetyltransferase) p300 HAT 结构域抑制剂，对人源的 IC50 值为 7 nM。P300-IN-6 可抑制 c-Myc 表达，降低 H3K18ac 和 H3K27ac 水平，并抑制癌细胞增殖。P300-IN-6 可抑制异种移植小鼠模型中的肿瘤生长。P300-IN-6 可用于多发性骨髓瘤的研究。

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

P300-IN-6

P300-IN-6 Chemical Structure

CAS No. : 3034595-62-2

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

P300-IN-6 相关抗体

Top Publications Citing Use of Products

查看 Histone Acetyltransferase 亚型特异性产品:

查看所有亚型
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma[1].

IC50 & Target[1]

p300-HAT

7 nM (IC50)

体外研究
(In Vitro)

P300-IN-6 (Compound B6) 可强效抑制重组人 p300 HAT 结构域，其 IC50 为 7 nM[1]。
P300-IN-6 可强效抑制人多发性骨髓瘤 OPM-2 细胞的增殖，其 IC50 为 8.8 nM[1]。
P300-IN-6 (100 nM; 6 days) 可抑制人前列腺癌 22RV1 细胞的增殖，在 100 nM 浓度下可达到 70-80% 的生长抑制率[1]。
P300-IN-6 (1-20 nM; 24 h) 可剂量依赖性地抑制 c-Myc 的表达，并降低 OPM-2 和 22RV1 细胞中 H3K18ac/H3K27ac 的水平[1]。

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

P300-IN-6 相关抗体:

Western Blot Analysis[1]

Cell Line: OPM-2 cells，22RV1 cells
Concentration: 1, 5, 10, 15, 20 nM
Incubation Time: 24 h
Result: Dose-dependently suppressed c-Myc expression as early as 6 h, and c-
Myc remained markedly suppressed through 12-24 h.
Reduced H3K18ac and H3K27ac levels.
Showed active inhibitory effect at 5-10 nM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUC0-last CL MRT Vss Tmax Cmax F
Mice[1] 0.5 mg/kg p.o. 3.77 h 7.45 ng·h/mL / 4.16 h / 0.25 h 9.30 ng/mL 9.9 %
Mice[1] 0.5 mg/kg i.v. 0.26 h 75.1 ng·h/mL 118 mL/min/kg 0.26 h 1886 mL/kg / / /
体内研究
(In Vivo)

P300-IN-6 (Compound B6) (20 mg/kg；灌胃；每天一次；17 天) 在小鼠 OPM-2 多发性骨髓瘤异种移植模型中实现了 60% 的肿瘤生长抑制[1]。

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

Animal Model: BALB/c nude mice (female, 6 weeks old)[1]
Dosage: 20 mg/kg
Administration: I.g.; once daily; 17 consecutive days
Result: Achieved a tumor growth inhibition (TGI) value of 60%.
Showed good tolerability, with no mortality and only a slight decrease in body weight over the dosing period.
分子量

454.52

Formula

C26H26N6O2
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

P300-IN-6 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:

P300-IN-63034595-62-2Histone Acetyltransferasec-MycHATsHATMycxenograft mouse models22RV1 cellsOPM-2 cellsp300 HAT domainH3K27acH3K18acprostate cancermultiple myelomahistone acetyltransferaseInhibitorinhibitorinhibit

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：
P300-IN-6
目录号：
HY-181669
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