Alsterpaullone (Synonyms: 9-Nitropaullone,NSC 705701) |
| رقم الكتالوجGC15841 |
Alsterpaullone (9-Nitropaullone) هو مثبط قوي لـ CDK ، مع IC50s من 35 نانومتر ، 15 نانومتر ، 200 نانومتر و 40 نانومتر لـ CDK1 / cyclin B ، CDK2 / cyclin A ، CDK2 / cyclin E و CDK5 / p35 ، على التوالييتنافس Alsterpaullone أيضًا مع ATP للربط بـ GSK-3alpha / GSK-3beta مع IC50s لكل من 4 نانومترAlsterpaullone له نشاط مضاد للأورام ، ويمتلك إمكانية الدراسة في الاضطرابات التنكسية العصبية والتكاثريةيستحث Alsterpaullone موت الخلايا المبرمج في خط خلايا سرطان الدم
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 237430-03-4
Sample solution is provided at 25 µL, 10mM.
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Alsterpaullone is a small molecule cyclin-dependent kinase (CDK) inhibitor [1,2].
Cyclin-dependent kinases (CDKs) are protein kinases that play important roles in the control of cell division and modulate transcription in response to several extra- and intracellular cues. Deregulation of CDKs is a hallmark of several diseases, including cancer, and drug-targeted inhibition of specific members has generated very encouraging results in clinical trials [3].
Alsterpaullone (Alp) induced apoptosis and promoted loss in clonogenicity in the Jurkat cell line. Alp activated both caspase-8 and -9, leading to cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP). Alp disrupted the activation of caspase-9 followed mitochondrial perturbation. Alp activated caspase-9 via mitochondrial perturbation [1]. Alsterpaullone regulated the cell cycle progression. Alsterpaullone inhibited HeLa cells in a time-dependent (0–72 h) and dose-dependent (0–30 μM) manner. Alsterpaullone arrested HeLa cells in G2/M prior to undergoing apoptosis via a mechanism that is involved in the regulation of various antiapoptotic genes, DNA-repair, transcription, and cell cycle progression. Alsterpaullone effectively prevented HeLa cells from entering S-phase [2].
References:
[1] Lahusen T, De Siervi A, Kunick C, et al. Alsterpaullone, a novel cyclin‐dependent kinase inhibitor, induces apoptosis by activation of caspase‐9 due to perturbation in mitochondrial membrane potential[J]. Molecular carcinogenesis, 2003, 36(4): 183-194.
[2] Cui C, Wang Y, Wang Y, et al. Alsterpaullone, a cyclin-dependent kinase inhibitor, mediated toxicity in HeLa cells through apoptosis-inducing effect[J]. Journal of analytical methods in chemistry, 2013, 2013.
[3] Malumbres M. Cyclin-dependent kinases[J]. Genome biology, 2014, 15(6): 122.
| Cas No. | 237430-03-4 | SDF | |
| المرادفات | 9-Nitropaullone,NSC 705701 | ||
| Chemical Name | 9-nitro-7,12-dihydrobenzo[2,3]azepino[4,5-b]indol-6(5H)-one | ||
| Canonical SMILES | O=C1CC2=C(C3=CC=CC=C3N1)NC4=C2C=C(C=C4)[N+]([O-])=O | ||
| Formula | C16H11N3O3 | M.Wt | 293.28 |
| الذوبان | DMF: 3 mg/ml,DMSO: 10 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4097 mL | 17.0486 mL | 34.0971 mL |
| 5 mM | 0.6819 mL | 3.4097 mL | 6.8194 mL |
| 10 mM | 0.341 mL | 1.7049 mL | 3.4097 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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