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AdipoGen Life Sciences
(R)-Roscovitine
45
CHF
CHF 45.00
In stock
AG-CR1-0006-M0011 mgCHF 45.00
AG-CR1-0006-M0055 mgCHF 135.00
AG-CR1-0006-M05050 mgCHF 405.00
| Product Details | |
|---|---|
| Synonyms | 6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine |
| Product Type | Chemical |
| Properties | |
| Formula |
C19H26N6O |
| MW | 354.5 |
| CAS | 186692-46-6 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO or 100% ethanol; only moderately soluble in water. |
| Identity | Determined by 1H-NMR. |
| InChi Key | BTIHMVBBUGXLCJ-OAHLLOKOSA-N |
| Smiles | CC[C@H](CO)NC1=NC2=C(N=CN2C(C)C)C(NCC2=CC=CC=C2)=N1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent and selective inhibitor of CDKs [1, 2, 4, 16].
- More potent than olomoucine [3].
- Inhibits CDK1/cyclin B kinase (IC50 = 450 nM) [2], CDK2 (IC50 = 700 nM) [4] and CDK5/p35 (IC50 = 160 nM) [4,5].
- Inhibits M phase promoting factor (MPF) kinase activity [2].
- Arrests human fibroblasts in G1 phase [6].
- Antitumor compound [8].
- Activates the mitogen-activated protein kinase pathway [9].
- Targets both the p53 and NF-κB pathways[10].
- Has effects on calcium channel gating [12, 17, 18].
- Prevents DNA damage-induced cyclin A1 upregulation [13].
- Apoptosis inducer [11, 15, 20].
- As CYC202 in phase I clinical trials [14].
- Reviews [3, 7, 19].
Product References
- Activation of cyclin-dependent kinases by Myc mediates induction of cyclin A, but not apoptosis: B. Rudolph, et al.; EMBO J. 15, 3065 (1996)
- Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5: L. Meijer, et al.; Eur. J. Biochem. 243, 527 (1997)
- Chemical inhibitors of cyclin-dependent kinases: L. Meijer and S.H. Kim; Meth. Enzymol. 283, 113 (1997)
- Cytokinin-derived cyclin-dependent kinase inhibitors: synthesis and cdc2 inhibitory activity of olomoucine and related compounds: L. Havlicek, et al.; J. Med. Chem. 40, 408 (1997)
- Direct in vivo inhibition of the nuclear cell cycle cascade in experimental mesangial proliferative glomerulonephritis with Roscovitine, a novel cyclin-dependent kinase antagonist: J.W. Pippin, et al.; J. Clin. Invest. 100, 2512 (1997)
- The cyclin-dependent kinase inhibitors olomoucine and roscovitine arrest human fibroblasts in G1 phase by specific inhibition of CDK2 kinase activity: F. Alessi, et al.; Exp. Cell Res. 245, 8 (1998)
- The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003)
- In vitro and in vivo antitumor properties of the cyclin dependent kinase inhibitor CYC202 (R-roscovitine): S.J. McClue, et al.; Int. J. Cancer 102, 463 (2002)
- The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway: S.R. Whittaker, et al.; Cancer Res. 64, 262 (2004)
- R-Roscovitine simultaneously targets both the p53 and NF-kappaB pathways and causes potentiation of apoptosis: implications in cancer therapy: A. Dey, et al.; Cell Death Differ. 15, 263 (2008)
- The CDK inhibitor, R-roscovitine, promotes eosinophil apoptosis by down-regulation of Mcl-1: R. Duffin, et al.; FEBS Lett. 583, 2540 (2009)
- (R)-roscovitine prolongs the mean open time of unitary N-type calcium channel currents: N.R. DeStefino, et al.; Neuroscience 167, 838 (2010)
- R-Roscovitine (Seliciclib) prevents DNA damage-induced cyclin A1 upregulation and hinders non-homologous end-joining (NHEJ) DNA repair: M. Federico, et al.; Mol. Cancer 9,208 (2010)
- Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies: C. Le Tourneau, et al.; Eur. J. Cancer 46, 3243 (2010)
- Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004)
- Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005)
- The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction: S. Cho & S.D. Meriney; Eur. J. Neurosci. 23, 3200 (2006)
- Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007)
- Cyclin-dependent kinase inhibitors as anticancer drugs: V. Krystof & S. Uldrijan; Curr. Drug Targets 11, 291 (2010)
- Roscovitine induces cell death and morphological changes indicative of apoptosis in MDA-MB-231 breast cancer cells: O.P. Mgbonyebi, et al.; Cancer Res. 59, 1903 (1999)
- Polo-like kinase 4 transcription is activated via CRE and NRF1 elements, repressed by DREAM through CDE/CHR sites and deregulated by HPV E7 protein: M. Fischer, et al.; Nucleic Acids Res. 42, 163 (2014) (AdipoGen spec.)
- Roscovitine is a proteostasis regulator that corrects the trafficking defect of F508del-CFTR by a CDK-independent mechanism: C. Norez, et al.; Br. J. Pharmacol. 171, 4831 (2014)
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