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

Kenpaullone/肯帕罗酮 {[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增强大鼠和人类神经前体细胞培养物中的神经分化，促进小鼠胚胎干细胞 (ES 细胞)及肌萎缩性侧索硬化症 (ALS)患者诱导多能干细胞 (iPS 细胞)衍生的运动神经元的存活。

Kenpaullone/肯帕罗酮化学结构
CAS号：142273-20-9

Kenpaullone/肯帕罗酮 3D分子结构
CAS号：142273-20-9

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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 HCl	++++ 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											ERK,SGK	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(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 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 HCl	++++ 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 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/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ 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			98%
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												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 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				✔		Sirtuin,PKC	95%
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/肯帕罗酮生物活性

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/肯帕罗酮细胞实验

Cell Line Mouse embryonic fibroblasts (MEFs) ReNcell VM cells Mouse cochlear explants SOD1G93A/HB9::GFP mouse motor neurons HB9::GFP mouse motor neurons Neural progenitor cells (NPCs) Mouse cochlear explants Primary cortical neurons HT22 cells HEK293 cells SH-SY5Y cells Neural progenitor cells (NPCs) Mouse embryonic fibroblasts (MEFs) Chick embryonic atrial myocytes Adult human skin fibroblasts P3 mouse cochlear explants HEI-OC1 cells SGHPL-4 cells ReNcell VM cells HEI-OC1 cells SOD1G93A mutant mouse motor neurons (SOD1G93A/HB9::GFP) Wild-type mouse motor neurons (HB9::GFP) BHK cells HEK293 MSR GripTite cells Human primary fetal cortical neurons Rat primary cortical neurons 4T1 cells	Concentration	Treated Time	Description	References
Mouse embryonic fibroblasts (MEFs)	5 µM	10 days	To functionally replace Klf4 in reprogramming, activating Nanog expression and inducing iPS cell formation	Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.
ReNcell VM cells	2 µM	15 days	To study the effect of kenpaullone on the differentiation of ReNcell VM cells, results showed that kenpaullone promoted neurite extension and neural differentiation.	Sci Data. 2019 Feb 19;6:190016.
Mouse cochlear explants	5 µM	24 hours	Evaluating the protective effect of kenpaullone against cisplatin-induced hair cell death, results showed kenpaullone significantly reduced hair cell loss.	J Exp Med. 2018 Apr 2;215(4):1187-1203.
SOD1G93A/HB9::GFP mouse motor neurons	0.1 µM, 1 µM, 10 µM	72 hours	Promoted motor neuron survival and preserved cell morphology	Cell Stem Cell. 2013 Jun 6;12(6):713-26.
HB9::GFP mouse motor neurons	0.1 µM, 1 µM, 10 µM	72 hours	Promoted motor neuron survival and preserved cell morphology	Cell Stem Cell. 2013 Jun 6;12(6):713-26.
Neural progenitor cells (NPCs)	5 µM	8 days	To replace Klf4 in the presence of Oct4 and c-Myc, inducing NPCs reprogramming into iPS cells	Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.
Mouse cochlear explants	5 µM	24 hours	Evaluating the protective effect of Kenpaullone against cisplatin-induced hair cell death, results showed Kenpaullone significantly reduced hair cell loss.	J Exp Med. 2018 Apr 2;215(4):1187-1203.
Primary cortical neurons	0.25–2 μM	36 hours	KEN enhanced ADAM10 protein levels	Adv Sci (Weinh). 2024 Mar;11(11):e2305260.
HT22 cells	0.25–2 μM	36 hours	KEN enhanced ADAM10 protein levels	Adv Sci (Weinh). 2024 Mar;11(11):e2305260.
HEK293 cells	0.25–2 μM	36 hours	KEN enhanced ADAM10 protein levels	Adv Sci (Weinh). 2024 Mar;11(11):e2305260.
SH-SY5Y cells	0.25–2 μM	36 hours	KEN significantly increased m-ADAM10 protein levels	Adv Sci (Weinh). 2024 Mar;11(11):e2305260.
Neural progenitor cells (NPCs)	5 μM	8 days	Replace Klf4 to induce iPS cell formation in the presence of Oct4 and c-Myc	Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.
Mouse embryonic fibroblasts (MEFs)	5 μM	10 days	Activate Nanog expression, replace Klf4 in reprogramming	Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.
Chick embryonic atrial myocytes	2-5 μmol/L	24 hours	Kenpaullone, by inhibiting GSK3β activity, increases the expression of nSREBP-1 and GIRK4, thereby modulating the response of atrial myocytes to parasympathetic stimulation.	Diabetes. 2014 Jun;63(6):2097-113.
Adult human skin fibroblasts	1 µM	treatment starting at 14 dpi and continued	Kenpaullone significantly promoted the survival of ALS-hiMNs, enhanced dendritic outgrowth, and restored soma size. Electrophysiological recordings showed that Kenpaullone completely normalized the excitability of ALS-hiMNs and restored their ability to form neuromuscular junctions and control muscle activity.	Cell Rep. 2016 Jan 5;14(1):115-128.
P3 mouse cochlear explants	0.150 μM	24 hours	To evaluate the protective effect of Kenpaullone against cisplatin-induced damage in cochlear explants, results showed Kenpaullone significantly protected outer hair cells from cisplatin toxicity.	J Med Chem. 2018 Sep 13;61(17):7700-7709.
HEI-OC1 cells	0.349 μM	22 hours	To evaluate the protective effect of Kenpaullone against cisplatin-induced cytotoxicity, results showed Kenpaullone significantly reduced cisplatin-induced caspase-3/7 activity.	J Med Chem. 2018 Sep 13;61(17):7700-7709.
SGHPL-4 cells	20 and 50 nM	6 hours	To investigate the effect of 1-azakenpaullone on SGHPL-4 cell motility, results showed that activation of β-catenin alone was insufficient to stimulate cell motility.	Hum Reprod. 2008 Aug;23(8):1733-41.
ReNcell VM cells	2 μM	15 days	To study the effect of kenpaullone on the differentiation of ReNcell VM cells, results showed that kenpaullone accelerated neural differentiation and promoted neurite extension and branching.	Sci Data. 2019 Feb 19;6:190016.
HEI-OC1 cells	8 µM	22 hours	Screening for protective compounds, Kenpaullone showed protective effects against cisplatin-induced apoptosis.	J Exp Med. 2018 Apr 2;215(4):1187-1203.
SOD1G93A mutant mouse motor neurons (SOD1G93A/HB9::GFP)	0.1 μM, 1 μM, 10 μM	72 hours	Kenpaullone significantly prolonged the healthy survival of both wild-type and mutant motor neurons, attributed to its dual inhibition of GSK3 and HGK kinases.	Cell Stem Cell. 2013 Jun 6;12(6):713-26.
Wild-type mouse motor neurons (HB9::GFP)	0.1 μM, 1 μM, 10 μM	72 hours	Kenpaullone significantly prolonged the healthy survival of both wild-type and mutant motor neurons, attributed to its dual inhibition of GSK3 and HGK kinases.	Cell Stem Cell. 2013 Jun 6;12(6):713-26.
BHK cells	10 μM	48 hours	Flow cytometry detected increased cell-surface /H9004F508-CFTR expression in Kenpaullone-treated groups.	Mol Cell Proteomics. 2012 Sep;11(9):745-57.
HEK293 MSR GripTite cells	10 μM	48 hours	Evaluated correction of /H9004F508-CFTR function via Cellomics halide exchange assay, showing fluorescence intensity difference ≥0.10, indicating partial rescue of trafficking defect by Kenpaullone.	Mol Cell Proteomics. 2012 Sep;11(9):745-57.
Human primary fetal cortical neurons	50, 100, 400 nM	2-4 days	Dose-dependently enhanced KCC2 mRNA expression	Nat Commun. 2021 Oct 27;12(1):6208.
Rat primary cortical neurons	10-1000 nM	48 hours	Enhanced Kcc2 gene expression and function	Nat Commun. 2021 Oct 27;12(1):6208.
4T1 cells	5 µg KEN	24 hours	Kenpaullone combined with Paclitaxel significantly reduced tumor volume and induced cell death	Oncogene. 2018 Dec;37(49):6299-6315.

Cell Line

Concentration

Treated Time

Description

References

Mouse embryonic fibroblasts (MEFs)

5 µM

10 days

To functionally replace Klf4 in reprogramming, activating Nanog expression and inducing iPS cell formation

Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.

ReNcell VM cells

2 µM

15 days

To study the effect of kenpaullone on the differentiation of ReNcell VM cells, results showed that kenpaullone promoted neurite extension and neural differentiation.

Sci Data. 2019 Feb 19;6:190016.

Mouse cochlear explants

5 µM

24 hours

Evaluating the protective effect of kenpaullone against cisplatin-induced hair cell death, results showed kenpaullone significantly reduced hair cell loss.

J Exp Med. 2018 Apr 2;215(4):1187-1203.

SOD1G93A/HB9::GFP mouse motor neurons

0.1 µM, 1 µM, 10 µM

72 hours

Promoted motor neuron survival and preserved cell morphology

Cell Stem Cell. 2013 Jun 6;12(6):713-26.

HB9::GFP mouse motor neurons

0.1 µM, 1 µM, 10 µM

72 hours

Promoted motor neuron survival and preserved cell morphology

Cell Stem Cell. 2013 Jun 6;12(6):713-26.

Neural progenitor cells (NPCs)

5 µM

8 days

To replace Klf4 in the presence of Oct4 and c-Myc, inducing NPCs reprogramming into iPS cells

Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.

Mouse cochlear explants

5 µM

24 hours

Evaluating the protective effect of Kenpaullone against cisplatin-induced hair cell death, results showed Kenpaullone significantly reduced hair cell loss.

J Exp Med. 2018 Apr 2;215(4):1187-1203.

Primary cortical neurons

0.25–2 μM

36 hours

KEN enhanced ADAM10 protein levels

Adv Sci (Weinh). 2024 Mar;11(11):e2305260.

HT22 cells

0.25–2 μM

36 hours

KEN enhanced ADAM10 protein levels

Adv Sci (Weinh). 2024 Mar;11(11):e2305260.

HEK293 cells

0.25–2 μM

36 hours

KEN enhanced ADAM10 protein levels

Adv Sci (Weinh). 2024 Mar;11(11):e2305260.

SH-SY5Y cells

0.25–2 μM

36 hours

KEN significantly increased m-ADAM10 protein levels

Adv Sci (Weinh). 2024 Mar;11(11):e2305260.

Neural progenitor cells (NPCs)

5 μM

8 days

Replace Klf4 to induce iPS cell formation in the presence of Oct4 and c-Myc

Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.

Mouse embryonic fibroblasts (MEFs)

5 μM

10 days

Activate Nanog expression, replace Klf4 in reprogramming

Proc Natl Acad Sci U S A. 2009 Jun 2;106(22):8912-7.

Chick embryonic atrial myocytes

2-5 μmol/L

24 hours

Kenpaullone, by inhibiting GSK3β activity, increases the expression of nSREBP-1 and GIRK4, thereby modulating the response of atrial myocytes to parasympathetic stimulation.

Diabetes. 2014 Jun;63(6):2097-113.

Adult human skin fibroblasts

1 µM

treatment starting at 14 dpi and continued

Kenpaullone significantly promoted the survival of ALS-hiMNs, enhanced dendritic outgrowth, and restored soma size. Electrophysiological recordings showed that Kenpaullone completely normalized the excitability of ALS-hiMNs and restored their ability to form neuromuscular junctions and control muscle activity.

Cell Rep. 2016 Jan 5;14(1):115-128.

P3 mouse cochlear explants

0.150 μM

24 hours

To evaluate the protective effect of Kenpaullone against cisplatin-induced damage in cochlear explants, results showed Kenpaullone significantly protected outer hair cells from cisplatin toxicity.

J Med Chem. 2018 Sep 13;61(17):7700-7709.

HEI-OC1 cells

0.349 μM

22 hours

To evaluate the protective effect of Kenpaullone against cisplatin-induced cytotoxicity, results showed Kenpaullone significantly reduced cisplatin-induced caspase-3/7 activity.

J Med Chem. 2018 Sep 13;61(17):7700-7709.

SGHPL-4 cells

20 and 50 nM

6 hours

To investigate the effect of 1-azakenpaullone on SGHPL-4 cell motility, results showed that activation of β-catenin alone was insufficient to stimulate cell motility.

Hum Reprod. 2008 Aug;23(8):1733-41.

ReNcell VM cells

2 μM

15 days

To study the effect of kenpaullone on the differentiation of ReNcell VM cells, results showed that kenpaullone accelerated neural differentiation and promoted neurite extension and branching.

Sci Data. 2019 Feb 19;6:190016.

HEI-OC1 cells

8 µM

22 hours

Screening for protective compounds, Kenpaullone showed protective effects against cisplatin-induced apoptosis.

J Exp Med. 2018 Apr 2;215(4):1187-1203.

SOD1G93A mutant mouse motor neurons (SOD1G93A/HB9::GFP)

0.1 μM, 1 μM, 10 μM

72 hours

Kenpaullone significantly prolonged the healthy survival of both wild-type and mutant motor neurons, attributed to its dual inhibition of GSK3 and HGK kinases.

Cell Stem Cell. 2013 Jun 6;12(6):713-26.

Wild-type mouse motor neurons (HB9::GFP)

0.1 μM, 1 μM, 10 μM

72 hours

Kenpaullone significantly prolonged the healthy survival of both wild-type and mutant motor neurons, attributed to its dual inhibition of GSK3 and HGK kinases.

Cell Stem Cell. 2013 Jun 6;12(6):713-26.

BHK cells

10 μM

48 hours

Flow cytometry detected increased cell-surface /H9004F508-CFTR expression in Kenpaullone-treated groups.

Mol Cell Proteomics. 2012 Sep;11(9):745-57.

HEK293 MSR GripTite cells

10 μM

48 hours

Evaluated correction of /H9004F508-CFTR function via Cellomics halide exchange assay, showing fluorescence intensity difference ≥0.10, indicating partial rescue of trafficking defect by Kenpaullone.

Mol Cell Proteomics. 2012 Sep;11(9):745-57.

Human primary fetal cortical neurons

50, 100, 400 nM

2-4 days

Dose-dependently enhanced KCC2 mRNA expression

Nat Commun. 2021 Oct 27;12(1):6208.

Rat primary cortical neurons

10-1000 nM

48 hours

Enhanced Kcc2 gene expression and function

Nat Commun. 2021 Oct 27;12(1):6208.

4T1 cells

5 µg KEN

24 hours

Kenpaullone combined with Paclitaxel significantly reduced tumor volume and induced cell death

Oncogene. 2018 Dec;37(49):6299-6315.

Kenpaullone/肯帕罗酮动物实验

Species Nude mice Zebrafish Mice Mice Nude mice	Animal Model Breast cancer xenograft model Zebrafish lateral-line neuromasts APP/PS1 mouse model Nerve constriction injury and bone cancer pain models Breast cancer xenograft model	Administration	Dosage	Frequency	Description	References
Nude mice	Breast cancer xenograft model	Intratumoral injection	200 µg KEN per mouse	Every five days	To evaluate the therapeutic effect of KLF4 inhibitor Kenpaullone on breast cancer xenograft model	Oncogene. 2018 Dec;37(49):6299-6315.
Zebrafish	Zebrafish lateral-line neuromasts	Water bath exposure	30–50 µM	20 hours	Evaluating the protective effect of Kenpaullone against cisplatin-induced hair cell loss in zebrafish, results showed Kenpaullone provided 30–50% protection.	J Exp Med. 2018 Apr 2;215(4):1187-1203.
Mice	APP/PS1 mouse model	Intraperitoneal injection	7 mg/kg	Every other day for 2 months	KEN promoted ADAM10 expression and improved cognitive functions	Adv Sci (Weinh). 2024 Mar;11(11):e2305260.
Mice	Nerve constriction injury and bone cancer pain models	Intraperitoneal or intrathecal injection	10 or 30 mg/kg	Daily injections for 7 days	KP exhibited analgesic effects in nerve constriction injury and bone cancer pain models	Nat Commun. 2021 Oct 27;12(1):6208.
Nude mice	Breast cancer xenograft model	Intratumoral injection	200 µg per mouse	Every five days, continuous treatment	Combination therapy of Kenpaullone and Paclitaxel significantly improved survival and reduced lung metastasis	Oncogene. 2018 Dec;37(49):6299-6315.

Species

Nude mice Zebrafish Mice Mice Nude mice

Animal Model

Breast cancer xenograft model Zebrafish lateral-line neuromasts APP/PS1 mouse model Nerve constriction injury and bone cancer pain models Breast cancer xenograft model

Administration

Dosage

Frequency

Description

References

Nude mice

Breast cancer xenograft model

Intratumoral injection

200 µg KEN per mouse

Every five days

To evaluate the therapeutic effect of KLF4 inhibitor Kenpaullone on breast cancer xenograft model

Oncogene. 2018 Dec;37(49):6299-6315.

Zebrafish

Zebrafish lateral-line neuromasts

Water bath exposure

30–50 µM

20 hours

Evaluating the protective effect of Kenpaullone against cisplatin-induced hair cell loss in zebrafish, results showed Kenpaullone provided 30–50% protection.

J Exp Med. 2018 Apr 2;215(4):1187-1203.

Mice

APP/PS1 mouse model

Intraperitoneal injection

7 mg/kg

Every other day for 2 months

KEN promoted ADAM10 expression and improved cognitive functions

Adv Sci (Weinh). 2024 Mar;11(11):e2305260.

Mice

Nerve constriction injury and bone cancer pain models

Intraperitoneal or intrathecal injection

10 or 30 mg/kg

Daily injections for 7 days

KP exhibited analgesic effects in nerve constriction injury and bone cancer pain models

Nat Commun. 2021 Oct 27;12(1):6208.

Nude mice

Breast cancer xenograft model

Intratumoral injection

200 µg per mouse

Every five days, continuous treatment

Combination therapy of Kenpaullone and Paclitaxel significantly improved survival and reduced lung metastasis

Oncogene. 2018 Dec;37(49):6299-6315.

Kenpaullone/肯帕罗酮参考文献

Kenpaullone/肯帕罗酮实验方案

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/肯帕罗酮技术信息

CAS号	142273-20-9
分子式	C₁₆H₁₁BrN₂O
分子量	327.18
SMILES Code	O=C(NC1=CC=CC=C12)CC3=C2NC4=C3C=C(Br)C=C4
MDL No.	MFCD02683595

别名	NSC-664704; 9-Bromopaullone; 1-azakenpaullone
运输	蓝冰
InChI Key	QQUXFYAWXPMDOE-UHFFFAOYSA-N
Pubchem ID	3820

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

溶解方案

细胞实验：

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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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

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

Kenpaullone/肯帕罗酮纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Kenpaullone/肯帕罗酮质控信息

Kenpaullone/肯帕罗酮生物活性

Kenpaullone/肯帕罗酮细胞实验

Kenpaullone/肯帕罗酮动物实验

Kenpaullone/肯帕罗酮参考文献

Kenpaullone/肯帕罗酮实验方案

Kenpaullone/肯帕罗酮技术信息

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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

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

Kenpaullone/肯帕罗酮 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/肯帕罗酮 质控信息

Kenpaullone/肯帕罗酮 生物活性

Kenpaullone/肯帕罗酮 细胞实验

Kenpaullone/肯帕罗酮 动物实验

Kenpaullone/肯帕罗酮 参考文献

Kenpaullone/肯帕罗酮 实验方案

Kenpaullone/肯帕罗酮 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/肯帕罗酮纯度/质量文件产品仅供科研

Kenpaullone/肯帕罗酮质控信息

Kenpaullone/肯帕罗酮生物活性

Kenpaullone/肯帕罗酮细胞实验

Kenpaullone/肯帕罗酮动物实验

Kenpaullone/肯帕罗酮参考文献

Kenpaullone/肯帕罗酮实验方案

Kenpaullone/肯帕罗酮技术信息