1. Epigenetics TGF-beta/Smad
  2. PKC
  3. PKC-IN-1

PKC-IN-1 是一种有效的,ATP-竞争性的,可逆的 PKC 抑制剂,对人 PKCβPKCαKi 值分别为 5.3 和 10.4 nM,对人 PKCα,PKCβI,PKCβII,PKCθ,PKCγ,PKC mu 和 PKCεIC50 值分别为 2.3,8.1,7.6,25.6,57.5,314,808 nM。

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PKC-IN-1 Chemical Structure

PKC-IN-1 Chemical Structure

CAS No. : 1046787-18-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3855
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2 mg ¥2333
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5 mg ¥3500
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10 mg ¥5000
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100 mg   询价  

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

IC50 & Target[1]

Human PKCα

2.3 nM (IC50)

Human PKCβII

7.6 nM (IC50)

Human PKCβI

8.1 nM (IC50)

Human PKCθ

25.6 nM (IC50)

Human PKCγ

57.5 nM (IC50)

Human PKC mu

314 nM (IC50)

Human PKCε

808 nM (IC50)

Human PKCβ

5.3 nM (Ki)

Human PKCα

10.4 nM (Ki)

体外研究
(In Vitro)

PKC-IN-1 (Compound A) is a potent, ATP-competitive and reversible of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively[1].

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

体内研究
(In Vivo)

PKC-IN-1 (Compound A; 15 and 30 mg/kg, p.o., bid (twice a day)) dose-dependently and significantly reduces maximum EAE severity and end severity in autoimmune encephalitis (EAE) model in Lewis rats[1].

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

分子量

500.61

Formula

C25H37FN8O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 25 mg/mL (49.94 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9976 mL 9.9878 mL 19.9756 mL
5 mM 0.3995 mL 1.9976 mL 3.9951 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Animal Administration
[1]

Rats[1]
PKC-IN-1 is tested in the experimental autoimmune encephalitis (EAE) model in Lewis rats. EAE is induced by MBP69-88/CFA immunization and pertussis toxin injection in Lewis rats. PKC-IN-1 is prepared as an oral suspension and dosed orally, twice per day (BID) at three doses, 7.5 and 15 and 30 mg/kg for total daily doses of 15, 30 and 60 mg/kg. The efficacy is compared to animals that receive the positive control FTY720 dosed once per day at a dose of 0.5 mg/kg. The treatment starts on Day 8, when 48% of the rats have signs of EAE[1].

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

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9976 mL 9.9878 mL 19.9756 mL 49.9391 mL
5 mM 0.3995 mL 1.9976 mL 3.9951 mL 9.9878 mL
10 mM 0.1998 mL 0.9988 mL 1.9976 mL 4.9939 mL
15 mM 0.1332 mL 0.6659 mL 1.3317 mL 3.3293 mL
20 mM 0.0999 mL 0.4994 mL 0.9988 mL 2.4970 mL
25 mM 0.0799 mL 0.3995 mL 0.7990 mL 1.9976 mL
30 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6646 mL
40 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
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.

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产品名称:
PKC-IN-1
目录号:
HY-16903
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