| Identification | Back Directory | [Name]
6-BENZYLAMINO-2-(2-HYDROXYETHYLAMINO)-7-METHYLPURINE | [CAS]
101622-50-8 | [Synonyms]
ISO-OLOMOUCINE
OLOMOUCINE, ISO-
6-BENZYLAMINO-2-(2-HYDROXYETHYLAMINO)-7-METHYLPURINE
Ethanol, 2-[[7-Methyl-6-[(phenylMethyl)aMino]-7H-purin-2-yl]aMino]- | [Molecular Formula]
C15H18N6O | [MDL Number]
MFCD00189361 | [MOL File]
101622-50-8.mol | [Molecular Weight]
298.34 |
| Chemical Properties | Back Directory | [density ]
1.36 | [storage temp. ]
Store at -20°C | [solubility ]
≤0.3mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide | [form ]
Off-white solid. |
| Hazard Information | Back Directory | [Uses]
Iso-olomoucine is a potent and selective inhibitor of cdc2, cdk and orther cyclin related kinases. | [Definition]
ChEBI: 2-[[7-methyl-6-[(phenylmethyl)amino]-2-purinyl]amino]ethanol is a thiopurine. | [Biological Activity]
iso-olomoucine is an inactive stereoisomer of the cdk5 inhibitor olomoucine.cyclin-dependent kinases (cdks) are reported to be key regulators of cell cycle progression whose function/dysfunction has been implicated in cancer, human neurodegenerative diseases, as well as the response of addictive drugs through alteration of postsynaptic dopamine receptor signaling. | [in vitro]
in a previous study, rat dorsal striatal synaptosomes were incubation with the cdk5 inhibitors roscovitine, olomoucine, and gw8510 or the inactive congener iso-olomoucine, which led to a rapid, concentration-dependent inhibition of specific [3h]da uptake. however, roscovitine was the only inhibitor that did not decrease [3h]2beta-carbomethoxy-3beta-(4-fluorophenyl)tropane binding to dstr dats. roscovitine-induced inhibition of dstr [3h]da uptake was demonstrated by decreased maximal uptake velocity, without a change in cell-surface dat levels. moreover, roscovitine did not enhance [3h]da release mediated by either dat reverse-transport. instead, roscovitine could enhance spontaneous [3h]da outflow and inhibit dat-mediated [3h]da reaccumulation into dstr slices. additionally, in a cdk5-independent manner, iso-olomoucine was able to rapidly inhibit dopamine transporter activity in rat dorsal striatal synaptosomes with a potency similar to that of olomoucine (ic50 ~37 μm) [1] | [IC 50]
≥ 1 mm for cdk5 | [storage]
Store at -20°C | [References]
[1] price, d. a.,sorkin, a. and zahniser, n.r. cyclin-dependent kinase 5 inhibitors: inhibition of dopamine transporter activity. molecular pharmacology 76(4), 812-823 (2009). |
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