Kenpaullone (Synonyms: 9-Bromopaullone; NSC-664704)

目录号: HY-12302 纯度: 98.20%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Kenpaullone 是一种有效的 CDK1/cyclin B 和 GSK-3β 抑制剂，IC₅₀ 值分别为 0.4 μM 和 23 nM，同时可抑制 CDK2/cyclin A，CDK2/cyclin E 和 CDK5/p25 的活性，IC₅₀ 值分别为 0.68 μM，7.5 μM 和 0.85 μM。Kenpaullone，一种 KLF4 的小分子抑制剂，在体外降低乳腺癌干细胞的自我更新和细胞活力。

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Kenpaullone Chemical Structure

CAS No. : 142273-20-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥770	In-stock
1 mg	￥318	In-stock
5 mg	￥700	In-stock
10 mg	￥1080	In-stock
25 mg	￥2195	In-stock
50 mg	￥3513	In-stock
100 mg	￥4918	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 5 篇科研文献

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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GSK-3 GSK-3α GSK-3β

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC₅₀s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC₅₀s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.

IC₅₀ & Target^[1]^[2]

Cdk1/cyclin B

0.4 μM (IC₅₀)

cdk2/cyclin A

0.68 μM (IC₅₀)

Cdk5/p25

0.85 μM (IC₅₀)

CDK2/cyclinE

7.5 μM (IC₅₀)

GSK-3β

0.023 μM (IC₅₀)

erk1

20 μM (IC₅₀)

erk2

9 μM (IC₅₀)

c-raf

38 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Fibroblast	IC₅₀	10000 nM Compound: 3	Inhibition of human SOD1 expressed in mouse fibroblasts after 48 hrs by ELISA relative to control Inhibition of human SOD1 expressed in mouse fibroblasts after 48 hrs by ELISA relative to control	[PMID: 24560539]
HCT-15	IC₅₀	23.86 μM Compound: 4a	Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay Cytotoxicity against human HCT15 cells after 48 hrs by SRB assay	[PMID: 19217301]
K562	IC₅₀	> 100 μM Compound: 4a	Cytotoxicity against human K562 cells after 48 hrs by SRB assay Cytotoxicity against human K562 cells after 48 hrs by SRB assay	[PMID: 19217301]
MCF7	IC₅₀	> 100 μM Compound: 4a	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay	[PMID: 19217301]
Oocyte	IC₅₀	0.5 μM Compound: 2	Inhibition of M-phase starfish oocytes CDK1/cyclin B assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting Inhibition of M-phase starfish oocytes CDK1/cyclin B assessed as incorporation of [gamma-33P]-ATP into histone H1 substrate after 30 mins by scintillation counting	[PMID: 20621478]
PC-3	IC₅₀	> 100 μM Compound: 4a	Cytotoxicity against human PC3 cells after 48 hrs by SRB assay Cytotoxicity against human PC3 cells after 48 hrs by SRB assay	[PMID: 19217301]
Sf9	IC₅₀	23 nM Compound: 3	Inhibition of GSK3beta (unknown origin) expressed in sf9 cells after 30 mins by scintillation counting analysis in presence of [gamma-32P]ATP Inhibition of GSK3beta (unknown origin) expressed in sf9 cells after 30 mins by scintillation counting analysis in presence of [gamma-32P]ATP	[PMID: 24560539]
U-251	IC₅₀	> 100 μM Compound: 4a	Cytotoxicity against human U251 cells after 48 hrs by SRB assay Cytotoxicity against human U251 cells after 48 hrs by SRB assay	[PMID: 19217301]

体外研究
(In Vitro)

KenpauLlone 对 c-src (IC₅₀，15 μM)、酪蛋白激酶 2 (IC₅₀，20 μM)、erk 1 (IC₅₀，20 μM) 和 erk 2 (IC₅₀，9 μM)。KenpauLlone 通过竞争性抑制 ATP 结合发挥作用，K_i 值为 2.5 μM。KenpauLlone 可以抑制培养物中肿瘤细胞的生长 (平均 GI₅₀，43 μM) 并导致细胞周期进程改变，这在血清饥饿恢复的条件下最为明显^[1]。KenpauLlone 具有广泛的生物学效用，从维持胰腺 β 细胞存活和增殖到诱导癌细胞凋亡^[2]。

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

分子量

327.18

Formula

C₁₆H₁₁BrN₂O

CAS 号

142273-20-9

性状

固体

颜色

Off-white to yellow

中文名称

肯帕罗酮

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 : 100 mg/mL (305.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0564 mL	15.2821 mL	30.5642 mL
5 mM	0.6113 mL	3.0564 mL	6.1128 mL
10 mM	0.3056 mL	1.5282 mL	3.0564 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)

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)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.64 mM); 悬浊液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

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

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.20%

选择批次：

Data Sheet (648 KB) SDS (393 KB)

COA (294 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Zaharevitz DW, et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9. [Content Brief]

[2]. Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7. [Content Brief]

[3]. F Yu, et al. Kruppel-like factor 4 (KLF4) is required for maintenance of breast cancer stem cells and for cell migration and invasion. Oncogene. 2011 May 5;30(18):2161-72. [Content Brief]

Kinase Assay ^[1]	The kinase assay is run for 10 min at 30°C with 1 mg/mL histone H1, in the presence of 15 μM [g-³²P]ATP (3000 Ci/μmol; 1 mCi/mL) in a final volume of 30 ml. Purification and assays or inhibition of other kinases are performed. In kinetic experiments, the histone H1 concentration is lowered to 3.5 mg/mL; the ATP concentration ranged from 50 to 400 μM, and the kenpaullone concentration ranges from 1 to 4 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Zaharevitz DW, et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9. [Content Brief] [2]. Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7. [Content Brief] [3]. F Yu, et al. Kruppel-like factor 4 (KLF4) is required for maintenance of breast cancer stem cells and for cell migration and invasion. Oncogene. 2011 May 5;30(18):2161-72. [Content Brief]

Kinase Assay
^[1]

The kinase assay is run for 10 min at 30°C with 1 mg/mL histone H1, in the presence of 15 μM [g-³²P]ATP (3000 Ci/μmol; 1 mCi/mL) in a final volume of 30 ml. Purification and assays or inhibition of other kinases are performed. In kinetic experiments, the histone H1 concentration is lowered to 3.5 mg/mL; the ATP concentration ranged from 50 to 400 μM, and the kenpaullone concentration ranges from 1 to 4 μM.

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

参考文献

[1]. Zaharevitz DW, et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999 Jun 1;59(11):2566-9. [Content Brief]

[2]. Lyssiotis CA, et al. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7. [Content Brief]

[3]. F Yu, et al. Kruppel-like factor 4 (KLF4) is required for maintenance of breast cancer stem cells and for cell migration and invasion. Oncogene. 2011 May 5;30(18):2161-72. [Content Brief]

Kenpaullone 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0564 mL	15.2821 mL	30.5642 mL	76.4105 mL
	5 mM	0.6113 mL	3.0564 mL	6.1128 mL	15.2821 mL
	10 mM	0.3056 mL	1.5282 mL	3.0564 mL	7.6411 mL
	15 mM	0.2038 mL	1.0188 mL	2.0376 mL	5.0940 mL
	20 mM	0.1528 mL	0.7641 mL	1.5282 mL	3.8205 mL
	25 mM	0.1223 mL	0.6113 mL	1.2226 mL	3.0564 mL
	30 mM	0.1019 mL	0.5094 mL	1.0188 mL	2.5470 mL
	40 mM	0.0764 mL	0.3821 mL	0.7641 mL	1.9103 mL
	50 mM	0.0611 mL	0.3056 mL	0.6113 mL	1.5282 mL
	60 mM	0.0509 mL	0.2547 mL	0.5094 mL	1.2735 mL
	80 mM	0.0382 mL	0.1910 mL	0.3821 mL	0.9551 mL
	100 mM	0.0306 mL	0.1528 mL	0.3056 mL	0.7641 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.

Keywords:

Kenpaullone142273-20-99-Bromopaullone NSC-664704肯帕罗酮NSC664704NSC 664704NSC-664704CDKGSK-3Cyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Kenpaullone (Synonyms: 9-Bromopaullone; NSC-664704)

Customer Review

MCE 顾客使用本产品发表的 5 篇科研文献