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

Name: Kenpaullone
Brand: MedChemExpress
SKU: HY-12302
Rating: 5.0 (13 reviews)

Cat. No.: HY-12302 Purity: 98.20%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

CAS No. : 142273-20-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

13 Publications Citing Use of MCE Kenpaullone

Cell Imaging/Staining

Cell Proliferation/Viability Assay

RT-PCR

IHC

: 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).

: 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.

: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

View All GSK-3 Isoform Specific Products:

View All Isoforms

GSK-3 GSK-3α GSK-3β

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

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	0.4 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: 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: 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]

In Vitro

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.

Molecular Weight

327.18

Formula

C₁₆H₁₁BrN₂O

CAS No.

142273-20-9

Appearance

Solid

Color

Off-white to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.20%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (257 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[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.

References

[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]

Complete Stock Solution Preparation Table

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

Kenpaullone Related Classifications

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-664704NSC664704NSC 664704NSC-664704CDKGSK-3Cyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

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

Customer Review

Kenpaullone Related Antibodies

13 Publications Citing Use of MCE Kenpaullone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

View All GSK-3 Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Kenpaullone Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Kenpaullone Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report