Kenpaullone | NSC-664704 | CDK1/GSK-3β Inhibitor | AmBeed-信号通路专用抑制剂

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肯帕罗酮 /Kenpaullone {[allProObj[0].p_purity_real_show]}

货号：A196851 同义名： NSC-664704;9-Bromopaullone

Kenpaullone是一种ATP竞争性抑制剂，针对CDK1/周期蛋白B（IC50 = 0.4 µM）、CDK2/周期蛋白A（IC50 = 0.68 µM）、CDK5/p25（IC50 = 0.85 µM）、淋巴细胞激酶（IC50 = 0.47 µM）和GSK-3β（IC50 = 0.23 μM）。

Kenpaullone 化学结构
CAS号：142273-20-9

Kenpaullone 3D分子结构
CAS号：142273-20-9

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Kenpaullone 纯度/质量文件产品仅供科研

货号：A196851 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

GSK-3 亚型比较
CDK 亚型比较
Src 亚型比较

产品名称	GSK-3 ↓ ↑	GSK-3α ↓ ↑	GSK-3β ↓ ↑	纯度
AZD2858	+ GSK-3, IC50: 68 nM			99%
Bikinin	✔			99%+
GSK 3 Inhibitor IX	++++ GSK-3, IC50: 5 nM			99%+
AZD1080		+++ GSK-3α, IC50: 6.9 nM	++ GSK-3β, IC50: 31 nM	99%+
BIO-acetoxime		+++ GSK-3α, IC50: 10 nM	+++ GSK-3β, IC50: 10 nM	95%
SB-216763		++ GSK-3α, IC50: 34.3 nM	++ GSK-3β, IC50: ~34.3 nM	98%
SB 415286		+ GSK-3α, IC50: 78 nM	+ GSK-3β, IC50: ~78 nM	99%+
CHIR-98014		++++ GSK-3α, IC50: 0.65 nM	++++ GSK-3β, IC50: 0.58 nM	98%
LY2090314		++++ GSK-3α, IC50: 1.5 nM	++++ GSK-3β, IC50: 0.9 nM	99%+
CHIR 99021		+++ GSK-3α, IC50: 10 nM	++++ GSK-3β, IC50: 6.7 nM	99%+
TDZD-8			+ GSK-3β, IC50: 2 μM	99%+
Indirubin			+ GSK-3β, IC50: 0.6 μM	98%
IM-12			++ GSK-3β, IC50: 53 nM	98%
TWS119			++ GSK-3β, IC50: 30 nM	99%
1-Azakenpaullone			+++ GSK-3β, IC50: 18 nM	99%+
AR-A014418			++ GSK-3β, Ki: 38 nM	99%+
Tideglusib			+ GSK-3β, IC50: 60 nM	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 hydrochloride	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinA, IC50: 70 nM CDK2/CyclinE, IC50: 35 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(A144C), Kd: 9.7 nM CDK2(C118L), Kd: 18.6 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinA, IC50: 4 nM CDK2/CyclinE, IC50: 3 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinA, IC50: 8 nM CDK2/CyclinE, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinA, IC50: 45 nM CDK2/CyclinE, IC50: 363 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinA, IC50: 0.68μM CDK2/CyclinE, IC50: 7.5μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinA, IC50: 38 nM CDK2/CyclinE, IC50: 48 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 hydrochloride	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinA, IC50: 0.7 μM CDK2/CyclinE, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 dihydrochloride									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinA, IC50: 224 nM CDK2/CyclinE, IC50: 2.54 μM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			99+%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ CLK4, IC50: 136 nM Dyrk1B , IC50: 1648 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Fyn ↓ ↑	Lck ↓ ↑	Lyn ↓ ↑	Src ↓ ↑	Yes ↓ ↑	其他靶点	纯度
Saracatinib	++ Fyn, IC50: 10 nM	++++ LCK, IC50: <4 nM	+++ Lyn, IC50: 5 nM	++++ c-Src, IC50: 2.7 nM			99%+
SU6656	+ Fyn, IC50: 170 nM		+ Lyn, IC50: 130 nM	+ Src, IC50: 280 nM	++ YES, IC50: 20 nM		98%
PP1	+++ Fyn, IC50: 6 nM	+++ LCK, IC50: 5 nM				EGFR	99%+
PP2	+++ Fyn, IC50: 5 nM	++++ LCK, IC50: 4 nM					98%
WH-4-023		++++ Lck, IC50: 2 nM		+++ Src, IC50: 6 nM			99%+
NVP-BHG 712				+ c-Src, IC50: 1.266 μM			99%+
CCT196969		++ LCK, IC50: 0.02 μM		+ Src, IC50: 0.03 μM			98%
MNS				+ Src, IC50: 29.3 μM		p97,Syk	98%
Tirbanibulin				++ Src (Hep 3B), GI50: 26 nM Src (HuH7), GI50: 13 nM			99%+
PP121				++ Src, IC50: 14 nM		VEGFR,PDGFR	99%+
Bosutinib				++++ Src, IC50: 1.2 nM			99%
Dasatinib monohydrate				++++ Src, IC50: 0.8 nM			98%
Quercetin				✔		PKC,Sirtuin	97%
Dasatinib				++++ Src, IC50: 0.8 nM			98%
Repotrectinib				+++ Src, IC50: 5.3 nM			99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Kenpaullone 生物活性

靶点

CDK5

CDK5/p35, IC50:0.85μM
CDK2

CDK2/CyclinA, IC50:0.68μM

CDK2/CyclinE, IC50:7.5μM
CDK1

CDK1/CyclinB, IC50:0.4μM

描述

(S) 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^[3]. Kenpaullone efficiently suppressed activity of glycogen synthase kinase (GSK) 3β. Combination therapy with kenpaullone and TMZ (temozolomide) suppressed stem cell phenotype and viability of both GSCs (glioma stem cell) and glioma cell lines. Combination therapy in mouse models significantly prolonged survival time compared with TMZ monotherapy^[4]. KLF4 inhibitor Kenpaullone sensitizes breast cancer cells and xenograft tumors to Paclitaxel and improves therapeutic effects^[5]. Moreover, kenpaullone plays a role in protecting cardiomyocytes from oxidative stress and that the turnover of Cx43 through SGSM3(small G protein signaling modulator 3)-induced lysosomal degradation underlies the anti-apoptotic effect of kenpaullone^[6].

Kenpaullone 参考文献

[1]Cole A, Frame S, Cohen P. Further evidence that the tyrosine phosphorylation of glycogen synthase kinase-3 (GSK3) in mammalian cells is an autophosphorylation event. Biochem J. 2004 Jan 1;377(Pt 1):249-55.

[2]Zaharevitz DW, Gussio R, 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.

[3]Zaharevitz DW, Gussio R, Leost M, Senderowicz AM, Lahusen T, Kunick C, Meijer L, Sausville EA. 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

[4]Kitabayashi T, Dong Y, Furuta T, Sabit H, Jiapaer S, Zhang J, Zhang G, Hayashi Y, Kobayashi M, Domoto T, Minamoto T, Hirao A, Nakada M. Identification of GSK3β inhibitor kenpaullone as a temozolomide enhancer against glioblastoma. Sci Rep. 2019 Jul 11;9(1):10049

[5]Shi L, Tang X, Qian M, Liu Z, Meng F, Fu L, Wang Z, Zhu WG, Huang JD, Zhou Z, Liu B. A SIRT1-centered circuitry regulates breast cancer stemness and metastasis. Oncogene. 2018 Dec;37(49):6299-6315

[6]Joo HC, Choi JW, Moon H, Lee CY, Yoo KJ, Kim SW, Hwang KC. Protective effects of kenpaullone on cardiomyocytes following H2O2-induced oxidative stress are attributed to inhibition of connexin 43 degradation by SGSM3. Biochem Biophys Res Commun. 2018 May 5;499(2):368-373

Kenpaullone 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.06mL

0.61mL

0.31mL

15.28mL

3.06mL

1.53mL

30.56mL

6.11mL

3.06mL

Kenpaullone 技术信息

CAS号	142273-20-9
分子式	C₁₆H₁₁BrN₂O
分子量	327.175

别名	NSC-664704;9-Bromopaullone;1-azakenpaullone
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解度

DMSO: 35 mg/mL(106.98 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

2% DMSO+50% PEG 300+5% Tween 80+water 2.5 mg/mL

肯帕罗酮 /Kenpaullone {[allProObj[0].p_purity_real_show]}

Kenpaullone 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Kenpaullone 质控信息

Kenpaullone 生物活性

Kenpaullone 参考文献

Kenpaullone 实验方案

Kenpaullone 技术信息

最近浏览的产品

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摩尔计算器

靶点

总药量计算器

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细胞研究

临床研究

确认信息

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CDK5	CDK5/p35, IC50:0.85μM
CDK2	CDK2/CyclinA, IC50:0.68μM CDK2/CyclinE, IC50:7.5μM
CDK1	CDK1/CyclinB, IC50:0.4μM

肯帕罗酮 /Kenpaullone {[allProObj[0].p_purity_real_show]}

Kenpaullone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Kenpaullone 质控信息

Kenpaullone 生物活性

Kenpaullone 参考文献

Kenpaullone 实验方案

Kenpaullone 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Kenpaullone 纯度/质量文件产品仅供科研