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

目錄號(hào): HY-12302 純度: 98.20%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Kenpaullone 是一種有效的 CDK1/cyclin B 和 GSK-3β 抑制劑，IC₅₀ 值分別為 0.4 μM 和 23 nM，同時(shí)可抑制 CDK2/cyclin A，CDK2/cyclin E 和 CDK5/p25 的活性，IC₅₀ 值分別為 0.68 μM，7.5 μM 和 0.85 μM。Kenpaullone，一種 KLF4 的小分子抑制劑，在體外降低乳腺癌干細(xì)胞的自我更新和細(xì)胞活力。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Kenpaullone Chemical Structure

CAS No. : 142273-20-9

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規(guī)格	價(jià)格	是否有貨
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		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)

•Mil Med Res. 2020 Nov 1;7(1):52. [Abstract]
•Mil Med Res. 2020 Sep 6;7(1):42. [Abstract]
•Adv Sci (Weinh). 2024 Jan 6:e2305260. [Abstract]
•Sci Adv. 2021 Apr 14;7(16):eabb2213. [Abstract]
•J Transl Med. 2024 Oct 10;22(1):922. [Abstract]

Kenpaullone 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 CDK 亞型特異性產(chǎn)品:

查看所有亞型

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

查看 GSK-3 亞型特異性產(chǎn)品:

查看所有亞型

GSK-3 GSK-3α GSK-3β

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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)

細(xì)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]

體外研究
(In Vitro)

KenpauLlone 對(duì) 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 通過(guò)競(jìng)爭(zhēng)性抑制 ATP 結(jié)合發(fā)揮作用，K_i 值為 2.5 μM。KenpauLlone 可以抑制培養(yǎng)物中腫瘤細(xì)胞的生長(zhǎng) (平均 GI₅₀，43 μM) 并導(dǎo)致細(xì)胞周期進(jìn)程改變，這在血清饑餓恢復(fù)的條件下最為明顯^[1]。KenpauLlone 具有廣泛的生物學(xué)效用，從維持胰腺 β 細(xì)胞存活和增殖到誘導(dǎo)癌細(xì)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 號(hào)

142273-20-9

性狀

固體

顏色

Off-white to yellow

中文名稱

肯帕羅酮

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 100 mg/mL (305.64 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.64 mM); 懸濁液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 98.20%

選擇批次：

Data Sheet (648 KB) SDS (393 KB)

COA (294 KB) LCMS (96 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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.

參考文獻(xiàn)

[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 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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肯帕羅酮NSC664704NSC 664704NSC-664704CDKGSK-3Cyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 5 篇科研文獻(xiàn)