製品番号: HY-12302

Kenpaullone

(別名: ケンパウロン；9-Bromopaullone; NSC-664704)

15 Cited Publications

カスタマーレビュー

Based on 15 publication(s) in Google Scholar

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.

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純度: 98.20%
CAS 番号: 142273-20-9
分子式: C₁₆H₁₁BrN₂O
分子量:327.18

保管条件:

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

Kenpaullone 構造式

CAS 番号: 142273-20-9

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
化学情報
Publications (15)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
Bioz

生物活性

製品説明

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)

CDK アイソフォーム固有の製品をすべて表示 :

GSK-3 アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Fibroblast	IC₅₀	10 μM 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	0.4 μM Compound: 4a	In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes. In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes.	[PMID: 10425100]
Oocyte	IC₅₀	0.4 μM Compound: 1	Inhibition of Cyclin-dependent kinase 1-cyclin B from Starfish oocytes Inhibition of Cyclin-dependent kinase 1-cyclin B from Starfish oocytes	[PMID: 10741555]
Oocyte	IC₅₀	0.4 μM Compound: Kenapaullone	Inhibition of Cyclin-dependent kinase 1-cyclin B from M phase starfish (Marthasterias glacialis) oocytes Inhibition of Cyclin-dependent kinase 1-cyclin B from M phase starfish (Marthasterias glacialis) oocytes	[PMID: 12593668]
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	0.023 μM Compound: 1a	Inhibition of GSK3-beta expressed in insect Sf9 cells Inhibition of GSK3-beta expressed in insect Sf9 cells	[PMID: 19906467]
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]

体外実験

Kenpaullone shows much less effect on c-src (IC₅₀, 15 μM), casein kinase 2 (IC₅₀, 20 μM), erk 1 (IC₅₀, 20 μM), and erk 2 (IC₅₀, 9 μM). Kenpaullone acts by competitive inhibition of ATP binding, and the apparent K_i is 2.5 μM. Kenpaullone can inhibit the growth of tumor cells in culture (mean GI₅₀, 43 μM) and causes altered cell cycle progression most clearly revealed under conditions of recovery from serum starvation^[1]. Kenpaullone demonstrates a wide range of biological utility, extending from maintenance of pancreatic β cell survival and proliferation to the induction of apoptosis in cancer cells^[2].

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

化学情報

CAS 番号 142273-20-9
性状 Solid
分子量 327.18
分子式 C₁₆H₁₁BrN₂O
Color Off-white to yellow
SMILES

O=C1NC2=CC=CC=C2C(NC3=C4C=C(Br)C=C3)=C4C1
別名

ケンパウロン；9-Bromopaullone; NSC-664704
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (15)

All WBCell Imaging/StainingIFCell Proliferation/Viability AssayRT-PCRIHC

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Mil Med Res

Direct conversion of human fibroblasts into dopaminergic neuron-like cells using small molecules and protein factors. [Abstract]

2020 Nov 1;7(1):52. PMID: 33129359

Kenpaullone purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2020 Nov 1;7(1):52. [Abstract]

Kenpaullone (3 μmol/L，After 6–8 days replaced 1 μmol/L). Representative microscopy images depicting the morphological changes after chemical induction. Scale bars=100 μm.

Kenpaullone purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2020 Nov 1;7(1):52. [Abstract]

Kenpaullone (3 μmol/L，After 6–8 days replaced 1 μmol/L). Characterization of the cultured IMR-90 fibroblasts by immunostaining assay for the fibroblast marker VIMENTIN, neural markers Class III β-tubulin 1 (TUJ1) and microtubule-associated protein 2 (MAP2), neural progenitor/stem cell markers PAX6, SOX2, and NESTIN, glial cell marker GFAP, and neural crest cell marker p75. Scale bars=25 μm.
Mil Med Res

Efficient and rapid conversion of human astrocytes and ALS mouse model spinal cord astrocytes into motor neuron-like cells by defined small molecules. [Abstract]

2020 Sep 6;7(1):42. PMID: 32892745

Kenpaullone purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2020 Sep 6;7(1):42. [Abstract]

Kenpaullone (5 μM, refreshed every 2 days for 7 days). Microscopic images of the Human astrocytes (HA1800) cells morphological changes after chemical induction.

Kenpaullone purchased from MedChemExpress. Usage Cited in: Mil Med Res. 2020 Sep 6;7(1):42. [Abstract]

Kenpaullone (5 μM), Human astrocytes (HA1800) cells. Expression of class III β-tubulin 1 (TUJ1), microtubule-associated protein 2 (MAP2), and GFAP in the control group and the KFYPR-induced group.
Adv Sci (Weinh)

SHMT2 Mediates Small-Molecule-Induced Alleviation of Alzheimer Pathology Via the 5'UTR-dependent ADAM10 Translation Initiation. [Abstract]

2024 Mar;11(11):e2305260. PMID: 38183387

Kenpaullone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]

Chemical structure of KEN (top), immunoblots (middle), and quantification (bottom) of ADAM10 in SH‐SY5Y cells treated with KEN (0.25–2 µM for 36 h, n = 5).

Kenpaullone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]

Immunoblots (top) and quantification (bottom) of ADAM10 treated with KEN (Kenpaullone, 0.25–2 µM for 36 h) in human HEK293 cell line, murine hippocampal cell line and primary cortical neurons, respectively (n = 5).

Kenpaullone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]

Immunofluorescent images (top) and quantification (bottom) of ADAM10 signals (green) in SH‐SY5Y cells treated with KEN (Kenpaullone, 0.75 µM for 36 h). DAPI is a nuclear marker (blue), scale bar = 25 µm (n > 10).

Kenpaullone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]

Cell viability of SH‐SY5Y cells treated with KEN (Kenpaullone, 0.25 to 2 µM for 36 h) measured by CCK‐8 kit (n = 5).

Kenpaullone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]

Relative mRNA levels of ADAM10 in SH‐SY5Y cells treated with KEN (Kenpaullone, 0.75 µM for 36 h, n = 8).

Kenpaullone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Mar;11(11):e2305260. [Abstract]

Kenpaullone (KEN, 7 mg/kg, every other day for 2 months, administered intraperitoneally). Immunohistochemical images (left) and quantification (right) of Aβ deposition in the brain of APP/PS1 and APP/PS1‐KEN, scale bar = 500 µm (n = 6).
Sci Adv

Chemical conversion of human epidermal stem cells into intestinal goblet cells for modeling mucus-microbe interaction and therapy. [Abstract]

2021 Apr 14;7(16):eabb2213. PMID: 33853767
J Biomed Sci

SARS-CoV-2 membrane protein recruits PP2A to dephosphorylate the nucleocapsid and promote virion production. [Abstract]

2026 May 15;33(1):51. PMID: 42141450
Int J Biol Sci

The KLF4/Galectin-3 cascade is a key determinant of tubular cell death and acute kidney injury. [Abstract]

2025 Sep 20;21(13):5802-5820. PMID: 41079936
J Transl Med

KLF4 regulates trophoblast function and associates with unexplained recurrent spontaneous abortion. [Abstract]

2024 Oct 10;22(1):922. PMID: 39390495
Cell Rep

SETDB2-mediated transcriptional repression of IDE in sensory neurons promotes migraine-like pain behaviors in mice. [Abstract]

2026 Mar 24;45(4):117201. PMID: 41880325
Cell Rep

Hypoxia-sensitive cells trigger NK cell activation via the KLF4-ASH1L-ICAM-1 axis, contributing to impairment in the rat epididymis. [Abstract]

2023 Nov 28;42(11):113442. PMID: 37952156
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
J Neurotrauma

Atorvastatin Regulates the Efferocytosis of Macrophages to Promote Hematoma Absorption and Inflammation Resolution in Experimental Subdural Hematoma. [Abstract]

2026 Jan 29:8977151261415615. PMID: 41609140
Cell Signal

Cell-type specific contribution of KLF4 to fibrotic nephropathy in tubular epithelium and fibroblast. [Abstract]

2026 Jul:143:112459. PMID: 41785980
Eur J Integr Med

2025 Aug 28;78:102545.
bioRxiv

2026 May 7.
Res Sq

2025 Apr 24.

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (305.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass

濃度

体積

分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始)

体積 _(開始)

濃度 _(終了)

体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.64 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

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.

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
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取扱説明書 (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Keywords

Kenpaullone

15 Cited Publications

100 mg お問い合わせ

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Kenpaullone

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Antidepressant Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

MedChemExpress（MCE）の使用を引用している文献 Kenpaullone

CDK アイソフォーム固有の製品をすべて表示

GSK-3 アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (15)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Kenpaullone 関連分類

製品番号: HY-12302