1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    PI3K/Akt/mTOR
  2. CDK
    GSK-3

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

Cat. No.: HY-12302 Purity: 98.07%
Handling Instructions

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.

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

Kenpaullone Chemical Structure

Kenpaullone Chemical Structure

CAS No. : 142273-20-9

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10 mM * 1 mL in DMSO USD 92 In-stock
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Estimated Time of Arrival: December 31
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target[1][2]

Cdk1/cyclin B

0.4 μM (IC50)

cdk2/cyclin A

0.68 μM (IC50)

CDK5/p35

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)

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 Ki 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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 35 mg/mL (106.97 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

327.18

Formula

C₁₆H₁₁BrN₂O

CAS No.

142273-20-9

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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× = ×
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Product Name:
Kenpaullone
Cat. No.:
HY-12302
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Kenpaullone

Cat. No.: HY-12302