Kenpaullone

Catalog No.S7917 Batch:S791701

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Technical Data

Formula

C16H11BrN2O
Molecular Weight 327.18 CAS No. 142273-20-9
Solubility (25°C)* In vitro DMSO 65 mg/mL (198.66 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2%DMSO 50%PEG300 5%Tween80 43%ddH2O
2.5mg/ml Taking the 1 mL working solution as an example, add 20 μL of 125 mg/ml clarified DMSO stock solution to 500 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 430 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Kenpaullone (9-Bromopaullone, NSC-664704) is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It also inhibit glycogen synthase kinase 3β (GSK3β) with IC50 of 0.23 µM.
Targets
GSK-3β [1]
(Cell-free assay)		 CDK1/CyclinB [1]
(Cell-free assay)		 CDK2/CyclinA [1]
(Cell-free assay)		 CDK5/p35 [1]
(Cell-free assay)		 CDK2/CyclinE [1]
(Cell-free assay)		 View More
0.23μM 0.4μM 0.68μM 0.85μM 7.5μM
In vitro In HEK-293 cells, phosphorylation of the endogenous GSK3α on Tyr279 is greatly decreased after prolonged incubation with Kenpaullone. Also, the Phosphorylation of the endogenous GSK3β also decreases, although less markedly. Kenpaullone also induces the dephosphorylation of both GSK3 isoforms in SH-SY5Y cells and PC12 cells. Kenpaullone (20µM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro whether GSK3 is expressed in Sf21 cells or in E. coli[2][3].

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Biochem Biophys Res Commun, 2013, 435(3):378-84. ]

Selleck's Kenpaullone has been cited by 6 publications

KLF4-mediated upregulation of the NKG2D ligand MICA in acute myeloid leukemia: a novel therapeutic target identified by enChIP [ Cell Commun Signal, 2023, 21(1):94] PubMed: 37143070
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
Aurora kinase A promotes hepatitis B virus replication and expression. [ Antiviral Res, 2019, 170:104572] PubMed: 31376425
GSK3β Controls mTOR and Prosurvival Signaling in Neurons [ Mol Neurobiol, 2018, 55(7):6050-6062] PubMed: 29143288
CDK inhibitors suppress Th17 and promote iTreg differentiation, and ameliorate experimental autoimmune encephalomyelitis in mice [Yoshida H, et al. Biochem Biophys Res Commun, 2013, 435(3):378-84] PubMed: 23665028

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.