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CDK inhibitor
Potent and selective inhibitor of CDKs. Selective for CDK1/cyclin B kinase (IC50=450nM) [2], CDK2 (IC50=700nM) [4] and CDK5/p35 (IC50=160nM) [4,5]. More potent than olomoucine (Prod. No. BML-CC200). Inhibits M phase promoting factor (MPF) kinase activity. Has effects on calcium channel gating.
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Product Details
| Alternative Name |
6-Benzylamino-2-(R)-[(1-ethyl)-2-hydroxyethylamino]-9-isopropylpurine, 2(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Seliciclib |
|---|---|
| Appearance |
White to off-white solid. |
| CAS |
186692-46-6 |
| Couple Target |
CDK |
| Couple Type |
Inhibitor |
| Formula |
C19H26N6O |
| MW |
354.4 |
| Purity |
≥95% (HPLC, TLC) |
| Solubility |
Soluble in DMSO. |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Stable for at least 1 year after receipt when stored, as supplied, at -20°C. Stock solutions are stable for up to 3 months at -20°C. |
|---|---|
| Short Term Storage |
+4°C |
| Long Term Storage |
-20°C |
| Shipping |
Dry Ice |
| Regulatory Status |
RUO – Research Use Only |
|---|
- The AHR represses nucleotide excision repair and apoptosis and contributes to UV-induced skin carcinogenesis: Pollet, M., Shaik, S., et al.; Cell Death Differ. 25, 1823 (2018), Abstract
- Cdk5 controls IL-2 gene expression via repression of the mSin3a-HDAC complex: Lam, E., Pareek, T. K., et al.; Cell Cycle 14, 1327 (2015), Abstract
- Inhibiting cyclin-dependent kinase 5 in the nucleus accumbens enhances the expression of amphetamine-induced locomotor conditioning: Singer, B. F., Forneris, J., et al.; Behav. Brain Res. 275, 96 (2014), Abstract
- Discovery of thienoquinolone derivatives as selective and ATP non-competitive CDK5/p25 inhibitors by structure-based virtual screening: Chatterjee, A., Cutler, S. J., et al.; Bioorg. Med. Chem. 22, 6409 (2014), Abstract
- Evidence for a novel anti-apoptotic pathway in human keratinocytes involving the aryl hydrocarbon receptor, E2F1, and checkpoint kinase 1: Frauenstein, K., Sydlik, U., et al.; Cell Death Differ. 20, 1425 (2013), Abstract
- Roscovitine differentially affects CaV2 and Kv channels by binding to the open state: Z. Buraei, et al.; Neuropharmacology 52, 883 (2007), Abstract
- 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), Abstract
- E6/E7 oncogenes increase and tumor suppressors decrease the proportion of self-renewing neural progenitor cells: Piltti, K., Kerosuo, L., et al.; Oncogene 25, 4880 (2006), Abstract
- Roscovitine targets, protein kinases and pyridoxal kinase: S. Bach, et al.; J. Biol. Chem. 280, 31208 (2005), Abstract
- Roscovitine, olomoucine, purvalanol: inducers of apoptosis in maturing cerebellar granule neurons: E.A. Monaco, 3rd, et al.; Biochem. Pharmacol. 67, 1947 (2004), Abstract
- Roscovitine and other purines as kinase inhibitors. From starfish oocytes to clinical trials: L. Meijer & E. Raymond; Acc. Chem. Res. 36, 417 (2003), (Review), Abstract
- The specificities of protein kinase inhibitors: an update: J. Bain, et al.; Biochem. J. 371, 199 (2003), Abstract
- Transcription of herpes simplex virus immediate-early and early genes is inhibited by roscovitine, an inhibitor specific for cellular cyclin- dependent kinases: L.M. Schang, et al.; J. Virol. 73, 2161 (1999), Abstract
- Effects of cyclin-dependent kinase inhibitors on transcription and ocular circadian rhythm of Aplysia: N. Sankrithi & A. Eskin; J. Neurochem. 72, 605 (1999), Abstract
- 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), Abstract
- Early inhibition of DNA synthesis in the developing rat cerebral cortex by the purine analogues olomoucine and roscovitine: J.S. Yakisich, et al.; BBRC 243, 674 (1998), Abstract
- 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), Abstract
- Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine: W.F. De Azvedo, et al.; Eur. J. Biochem. 243, 518 (1997), Abstract
- 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), Abstract
- 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), Abstract
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