Molecular structure of Alsterpaullone, 2-Cyanoethyl, CAS Number: 852529-97-0
Alsterpaullone, 2-Cyanoethyl (CAS 852529-97-0)
Alternate Names:
Alsterpaullone, 2-Cyanoethyl is known as a Alsterpaullone derivative.
Application:
Alsterpaullone, 2-Cyanoethyl is a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β.
CAS Number:
852529-97-0
Purity:
≥97%
Molecular Weight:
346.34
Molecular Formula:
C19H14N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Alsterpaullone, 2-Cyanoethyl is an alsterpaullone derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β (IC50 = 230 pM and 800 pM, respectively [ATP] = 15 µM). It displays ~37-fold greater selectivity for Cdk1/cyclin B over Cdk5/p25 (IC50 = 30 nM). In a commercially available testing screen panel, Alsterpaullone, 2-Cyanoethyl was shown to inhibit other kinases (pIC50 = -logIC50[M] pIC50 ~ 7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D1, GSK-3β, PDGFRβ, Src, VEGFR-2, and VEGFR-3, respectively [ATP] = 1 µM).
Alsterpaullone, 2-Cyanoethyl (CAS 852529-97-0) References
- Structure-aided optimization of kinase inhibitors derived from alsterpaullone. | Kunick, C., et al. 2005. Chembiochem. 6: 541-9. PMID: 15696597
- High-throughput screening reveals alsterpaullone, 2-cyanoethyl as a potent p27Kip1 transcriptional inhibitor. | Walters, BJ., et al. 2014. PLoS One. 9: e91173. PMID: 24646893
- Prediction of kinase inhibitor response using activity profiling, in vitro screening, and elastic net regression. | Tran, TP., et al. 2014. BMC Syst Biol. 8: 74. PMID: 24961498
- Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation. | Horbelt, D., et al. 2015. J Biol Chem. 290: 3390-404. PMID: 25368322
- Nestin phosphorylation at threonines 315 and 1299 correlates with proliferation and metastasis of human pancreatic cancer. | Matsuda, Y., et al. 2017. Cancer Sci. 108: 354-361. PMID: 28002641
- Structure and inhibitor specificity of the PCTAIRE-family kinase CDK16. | Dixon-Clarke, SE., et al. 2017. Biochem J. 474: 699-713. PMID: 28057719
- PKCζ-dependent upregulation of p27kip1 contributes to oxidative stress induced retinal pigment epithelial cell multinucleation. | Rajapakse, D., et al. 2017. Aging (Albany NY). 9: 2052-2068. PMID: 29016360
- p27Kip1 down-regulation as achieved by two clinically feasible means did not induce proliferation of supporting cells in the rat neonatal cochlea in vivo. | Silva, SA. and Maass, JC. 2019. Hear Res. 373: 10-22. PMID: 30578960
- S-Like-Phase Cyclin-Dependent Kinases Stabilize the Epstein-Barr Virus BDLF4 Protein To Temporally Control Late Gene Transcription. | Sato, Y., et al. 2019. J Virol. 93: PMID: 30700607
- Antitumor activity of cyclin-dependent kinase inhibitor alsterpaullone in Epstein-Barr virus-associated lymphoproliferative disorders. | Watanabe, T., et al. 2020. Cancer Sci. 111: 279-287. PMID: 31743514
- Novel anti-flavivirus drugs targeting the nucleolar distribution of core protein. | Tokunaga, M., et al. 2020. Virology. 541: 41-51. PMID: 31826845
- Lytic Induction Therapy against Epstein-Barr Virus-Associated Malignancies: Past, Present, and Future. | Yiu, SPT., et al. 2020. Cancers (Basel). 12: PMID: 32748879
- A kinase inhibitor screen identifies signaling pathways regulating mucosal growth during otitis media. | Noel, J., et al. 2020. PLoS One. 15: e0235634. PMID: 32760078
- Potential for Protein Kinase Pharmacological Regulation in Flaviviridae Infections. | Blázquez, AB. and Saiz, JC. 2020. Int J Mol Sci. 21: PMID: 33333737
Inhibitor of:
Cdc2, cyclin B, and Enzyme.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Alsterpaullone, 2-Cyanoethyl, 1 mg | sc-203815 | 1 mg | $336.00 |