For research use only. Not for therapeutic Use.
CR8（Cat No.:I006293）is a potent and selective inhibitor of cyclin-dependent kinases (CDKs), particularly CDK1, CDK2, CDK5, and CDK9, which are critical for regulating cell cycle progression and transcription. By inhibiting these kinases, CR8 induces cell cycle arrest and apoptosis, making it a valuable tool for cancer research. Its ability to target CDK9 also impacts RNA polymerase II-mediated transcription, contributing to the suppression of oncogene expression. CR8 has demonstrated efficacy in preclinical models of cancer, offering potential therapeutic applications in targeting CDK-driven malignancies and other diseases involving abnormal cell proliferation.
| Catalog Number | I006293 |
| CAS Number | 294646-77-8 |
| Synonyms | CR8; CR-8; CR 8.;(R)-2-((9-isopropyl-6-((4-(pyridin-2-yl)benzyl)amino)-9H-purin-2-yl)amino)butan-1-ol |
| Molecular Formula | C24H29N7O |
| Purity | ≥95% |
| Target | CDCK inhibitor |
| Solubility | Soluble in DMSO, not in water |
| Storage | 2-8°C |
| IUPAC Name | (2R)-2-[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol |
| InChI | InChI=1S/C24H29N7O/c1-4-19(14-32)28-24-29-22(21-23(30-24)31(15-27-21)16(2)3)26-13-17-8-10-18(11-9-17)20-7-5-6-12-25-20/h5-12,15-16,19,32H,4,13-14H2,1-3H3,(H2,26,28,29,30)/t19-/m1/s1 |
| InChIKey | HOCBJBNQIQQQGT-LJQANCHMSA-N |
| SMILES | CC[C@H](CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=C(C=C3)C4=CC=CC=N4 |
| Reference | </br>1:Binding CO2 by a Cr8 Metallacrown. Vitórica-Yrezábal IJ, Sava DF, Timco GA, Brown MS, Savage M, Godfrey HGW, Moreau F, Schröder M, Siperstein F, Brammer L, Yang S, Attfield MP, McDouall JJW, Winpenny REP.Angew Chem Int Ed Engl. 2017 May 8;56(20):5527-5530. doi: 10.1002/anie.201701726. Epub 2017 Apr 13. PMID: 28407353 </br>2:E2F1-CDK1 pathway activation in kanamycin-induced spiral ganglion cell apoptosis and the protective effect of CR8. Liu YY, Wang GP, Peng Z, Guo JY, Wu Q, Xie J, Gong SS.Neurosci Lett. 2016 Mar 23;617:247-53. doi: 10.1016/j.neulet.2016.02.034. Epub 2016 Feb 22. PMID: 26905670 </br>3:Studies of a Large Odd-Numbered Odd-Electron Metal Ring: Inelastic Neutron Scattering and Muon Spin Relaxation Spectroscopy of Cr8 Mn. Baker ML, Lancaster T, Chiesa A, Amoretti G, Baker PJ, Barker C, Blundell SJ, Carretta S, Collison D, Güdel HU, Guidi T, McInnes EJ, Möller JS, Mutka H, Ollivier J, Pratt FL, Santini P, Tuna F, Tregenna-Piggott PL, Vitorica-Yrezabal IJ, Timco GA, Winpenny RE.Chemistry. 2016 Jan 26;22(5):1779-88. doi: 10.1002/chem.201503431. Epub 2016 Jan 8. PMID: 26748964 Free PMC Article</br>4:Antitumoral effects of cyclin-dependent kinases inhibitors CR8 and MR4 on chronic myeloid leukemia cell lines. Troadec S, Blairvacq M, Oumata N, Galons H, Meijer L, Berthou C.J Biomed Sci. 2015 Jul 17;22:57. doi: 10.1186/s12929-015-0163-x. PMID: 26184865 Free PMC Article</br>5:Complete Genome Sequences of Two Citrobacter rodentium Bacteriophages, CR8 and CR44b. Toribio AL, Pickard D, Cerdeño-Tárraga AM, Petty NK, Thomson N, Salmond G, Dougan G.Genome Announc. 2014 May 29;2(3). pii: e00146-14. doi: 10.1128/genomeA.00146-14. PMID: 24874665 Free PMC Article</br>6:CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. Kabadi SV, Stoica BA, Loane DJ, Luo T, Faden AI.J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13. doi: 10.1038/jcbfm.2013.228. Epub 2014 Jan 8. PMID: 24398934 Free PMC Article</br>7:CDK/CK1 inhibitors roscovitine and CR8 downregulate amplified MYCN in neuroblastoma cells. Delehouzé C, Godl K, Loaëc N, Bruyère C, Desban N, Oumata N, Galons H, Roumeliotis TI, Giannopoulou EG, Grenet J, Twitchell D, Lahti J, Mouchet N, Galibert MD, Garbis SD, Meijer L.Oncogene. 2014 Dec 11;33(50):5675-87. doi: 10.1038/onc.2013.513. Epub 2013 Dec 9. PMID: 24317512 Free PMC Article</br>8:Pharmacokinetics and biodistribution of the cyclin-dependent kinase inhibitor -CR8- in mice. Sallam H, El-Serafi I, Meijer L, Hassan M.BMC Pharmacol Toxicol. 2013 Sep 30;14:50. doi: 10.1186/2050-6511-14-50. PMID: 24079553 Free PMC Article</br>9:Inhibition of NF-κB-mediated signaling by the cyclin-dependent kinase inhibitor CR8 overcomes prosurvival stimuli to induce apoptosis in chronic lymphocytic leukemia cells. Cosimo E, McCaig AM, Carter-Brzezinski LJ, Wheadon H, Leach MT, Le Ster K, Berthou C, Durieu E, Oumata N, Galons H, Meijer L, Michie AM.Clin Cancer Res. 2013 May 1;19(9):2393-405. doi: 10.1158/1078-0432.CCR-12-2170. Epub 2013 Mar 26. PMID: 23532892 Free Article</br>10:CDK inhibitors R-roscovitine and S-CR8 effectively block renal and hepatic cystogenesis in an orthologous model of ADPKD. Bukanov NO, Moreno SE, Natoli TA, Rogers KA, Smith LA, Ledbetter SR, Oumata N, Galons H, Meijer L, Ibraghimov-Beskrovnaya O.Cell Cycle. 2012 Nov 1;11(21):4040-6. doi: 10.4161/cc.22375. Epub 2012 Oct 3. PMID: 23032260 Free PMC Article |
