2. Apoptosis TGF-beta/Smad Epigenetics
  3. Apoptosis PKC
  4. Evo312

Evo312 是蛋白激酶 CβⅠ (PKCβⅠ) 的抑制剂 (IC50 为 117.34 nM) 且有剂量依赖性。Evo312 通过抑制 PKCβⅠ 蛋白表达，引起 PANC-GR (获得性耐吉西他滨 PC 细胞) 细胞周期阻滞和凋亡。Evo312 在胰腺癌细胞 PANC-1 和 PANC-GR 细胞中有抗增殖作用，IC50 为 0.08 μM 和 0.07 μM，在人正常胰腺导管上皮细胞 HPDE6-c7 中 IC50 为 2.95 μM。Evo312 在 PANC-GR 细胞移植小鼠模型中表现出抗肿瘤活性。

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

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

Evo312 Chemical Structure

Evo312 Chemical Structure

CAS No. : 2820245-53-0

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

Evo312 相关抗体

Top Publications Citing Use of Products

查看 PKC 亚型特异性产品:

查看所有亚型
PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model[1].

IC50 & Target

PKC-βI

117.34 nM (IC50)

体外研究
(In Vitro)

Evo312 (0-160 nM，24 h) 抑制 PANC-GR 细胞中 PKCβ1 蛋白表达和下游靶蛋白磷酸化[1]。
Evo312 (0-160 nM，24 h) 诱导 PANC-GR 细胞 G2/M 细胞周期阻滞，抑制细胞有丝分裂[1]。
Evo312 (0-160 nM，48 h) 诱导 PANC-GR 细胞凋亡[1]。

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

Evo312 相关抗体:

Cell Cycle Analysis[1]

Cell Line: PANC-GR (an acquired gemcitabine-resistant PC cell line, cell line PANC-GR was established in vitro from PANC-1 cells by exposing gemcitabine with gradually increasing concentrations (0.1−2 μM))
Concentration: 0, 40, 80, 160 nM
Incubation Time: 24 h
Result: Increased the number of G2/M cells from 37.53% to 58.51%, leading to mitosis.

Apoptosis Analysis[1]

Cell Line: PANC-GR, PANC-1
Concentration: 40, 80, 160 nM
Incubation Time: 48 h
Result: Increased total cell death (including early apoptosis, late apoptosis and necrosis) by 15.83%, 20.63% and 24.95%.

Western Blot Analysis[1]

Cell Line: PANC-GR, PANC-1
Concentration: 0, 40, 80, 160 nM
Incubation Time: 24 h; 48 h
Result: Inhibited the expression of PKCβ1 protein at 24 h, and inhibited the phosphorylation of glycogen synthase kinase 3β (GSK3β), protein kinase B (Akt), signal transducer and activator of transcription 5 (STAT5), and ribosomal protein S6 kinase β-1 (70S6K) in a dose-dependent manner.
Downregulated the expression levels of CDK (CDK2 and cdc2) and cyclin D1 proteins at 24 h, while upregulated the expression levels of cyclin B1 and p27 proteins.
Increased the expression levels of apoptosis markers caspase3, caspase8, and caspase9 proteins at 48 h.
体内研究
(In Vivo)

Evo312 (5 mg/kg，i.p.，three times a week，20 days) 通过下调 PKCβⅠ 抑制 PANC-GR (吉西他滨耐性细胞) 小鼠异种移植模型的肿瘤生长，而吉西他滨治疗对肿瘤生长的抑制作用可以忽略不计[1]。

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

Animal Model: PANC-GR cell mouse xenograft model; PANC-1 cell mouse xenograft model[1]
Dosage: 40 mg/kg; 5 mg/kg, three times a week, 20 days
Administration: Intraperitoneal injection (i.p.)
Result: Did not cause mouse death or significant toxicity at a dose of 40 mg/kg. At a dose of 5 mg/kg, the tumor volume was inhibited by 72%, and the tumor weight was reduced by 44.89% compared with the drug-loaded treatment group, with no significant toxicity or weight changes, and the expression of PKCβI in tumor tissues implanted with PANC-GR cells was effectively inhibited.
分子量

361.39

Formula

C21H19N3O3
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

Evo312 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:

Evo3122820245-53-0Evo 312Evo-312ApoptosisPKCProtein kinase CPANC-1PANC-GRMRC-5Pancreatic cancer (PC)Inhibitorinhibitorinhibit

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：
Evo312
目录号：
HY-169006
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