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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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500mg |
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Purity: ≥98%
Kenpaullone (NSC-664704) is a novel, potent and ATP competitive 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 inhibits ATP binding competitively. Kenpaullone can bind in the ATP binding site of CDK2 with residue contacts resembling those found in the crystal structures of other CDK2-bound inhibitors, according to molecular modeling.
Targets |
Cdk1/cyclin B (IC50 = 0.4 μM); cdk2/cyclin A (IC50 = 0.68 μM); CDK5/p35 (IC50 = 0.85 μM); CDK2/cyclinE (IC50 = 7.5 μM); GSK-3β (IC50 = 0.023 μM); erk1 (IC50 = 20 μM); erk2 (IC50 = 9 μM); c-raf (IC50 = 38 μM)
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ln Vitro |
Prolonged incubation with kenpaullone significantly reduces the amount of phosphorylation of the endogenous GSK3α on Tyr279 in HEK-293 cells. Moreover, although less dramatically, the endogenous GSK3β's phosphorylation also drops. In PC12 and SH-SY5Y cells, kenpaullone also causes the dephosphorylation of both GSK3 isoforms. Whether GSK3 is expressed in Sf21 cells or E. coli, kenpaullone (20µM) strongly suppresses the autophosphorylation of GSK3β at Tyr216 in vitro[2][3].
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Enzyme Assay |
The kinase assay is conducted for 10 minutes at 30°C with 1 mg/mL histone H1, in a final volume of 30 ml, and 15 μM [g-32P]ATP (3000 Ci/μmol; 1 mCi/mL). It is done through purification, assays, or inhibition of other kinases. The ATP concentration ranged from 50 to 400 μM, the kenpaullone concentration ranged from 1 to 4 μM, and the histone H1 concentration was lowered to 3.5 mg/mL in kinetic experiments.
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References |
Molecular Formula |
C16H11BRN2O
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Molecular Weight |
327.1753
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Exact Mass |
326.01
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Elemental Analysis |
C, 58.74; H, 3.39; Br, 24.42; N, 8.56; O, 4.89
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CAS # |
142273-20-9
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Related CAS # |
237430-03-4 (Alsterpaullone)
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Appearance |
White to off-white solid powder
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SMILES |
C1C2=C(C3=CC=CC=C3NC1=O)NC4=C2C=C(C=C4)Br
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InChi Key |
QQUXFYAWXPMDOE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H11BrN2O/c17-9-5-6-14-11(7-9)12-8-15(20)18-13-4-2-1-3-10(13)16(12)19-14/h1-7,19H,8H2,(H,18,20)
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Chemical Name |
9-bromo-7,12-dihydro-5H-indolo[3,2-d][1]benzazepin-6-one
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Synonyms |
1-azakenpaullone; Kenpaullone; NSC664704; NSC 664704; NSC-664704; 9-Bromopaullone
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~65 mg/mL (~198.7 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2% DMSO+50% PEG 300+5% Tween 80+ddH2O: 2.5mg/mL  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
![]() Inhibition of CDK1/cyclin B by paullones.A, dose-response curves for several paullones.B, kinetic analysis of inhibition by kenpaullone.Cancer Res.1999 Jun 1;59(11):2566-9. th> |
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![]() Effect of kenpaullone and 10-bromo-paullone on cell cycle progression.Cancer Res.1999 Jun 1;59(11):2566-9. td> |
![]() Schematic drawing of CDK2-kenpaullone interactions. td> |