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View all CDK1 Subfamily (CDK1, CDK2 & CDK3) products.Alsterpaullone is a potent CDK1 and 2 inhibitor (IC50 values are 0.035 and 0.08 μM, respectively). Also inhibits GSK-3β and Lck (IC50 values are 0.11 and 0.47 μM, respectively). Induces apoptosis by activation of caspase-9; inhibits growth of cancer cell lines in vitro. Also glucocorticoid receptor inhibitor.
分子量 | 293.28 |
公式 | C16H11N3O3 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 237430-03-4 |
PubChem ID | 5005498 |
InChI Key | OLUKILHGKRVDCT-UHFFFAOYSA-N |
Smiles | O=C1CC2=C(C3=CC=CC=C3N1)NC4=C2C=C([N+]([O-])=O)C=C4 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Schulz et al (1999) Paullones, a series of cyclin-dependent kinase inhibitors: synthesis, evaluation of CDK1/cyclin B inhibition, and in vitro antitumor activity. J.Med.Chem. 42 2909 PMID: 10425100
Bain et al (2003) The specificities of protein kinase inhibitors: an update. Biochem.J. 371 199 PMID: 12534346
Lahusen et al (2003) Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol.Carcinog. 36 183 PMID: 12669310
Jiang et al (2017) A high-throughput chemical screen identifies novel inhibitors and enhancers of anti-inflammatory functions of the glucocorticoid receptor. Sci.Rep. 7 6405 PMID: 28785063
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