| AlsterpaulloneCDKs and GSK3β inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
Alsterpaullone Dilution Calculator
calculate
Alsterpaullone Molarity Calculator
calculate
| Cas No. | 237430-03-4 | SDF | Download SDF |
| Synonyms | 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 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | Yellow to brown powder | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
