101622-50-8 Usage
Uses
Iso-olomoucine is a potent and selective inhibitor of cdc2, cdk and orther cyclin related kinases.
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
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).
Check Digit Verification of cas no
The CAS Registry Mumber 101622-50-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,1,6,2 and 2 respectively; the second part has 2 digits, 5 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 101622-50:
(8*1)+(7*0)+(6*1)+(5*6)+(4*2)+(3*2)+(2*5)+(1*0)=68
68 % 10 = 8
So 101622-50-8 is a valid CAS Registry Number.
InChI:InChI=1/C15H18N6O/c1-21-10-18-14-12(21)13(19-15(20-14)16-7-8-22)17-9-11-5-3-2-4-6-11/h2-6,10,22H,7-9H2,1H3,(H2,16,17,19,20)
101622-50-8Relevant articles and documents
INHIBITORS OF TWO ENZYMES WHICH METABOLIZE CYTOKININS
Parker, Charles W.,Entsch, Barrie,Letham, David S.
, p. 303 - 310 (2007/10/02)
Compounds which inhibit the natural metabolic inactivation of cytokinins are cosiderable physiological significance.In this study, inhibitors have been found for two enzymes which form glucose and alanine conjugates of cytokinin bases, namely, cytokinin 7-glucosyltransferase and β-(9-cytokinin)alanine synthase.The most effective inhibitors found for the former enzyme were the cytokinin analogues 3-methyl-7-n-pentylaminopyrazolopyrimidine, which acted competitively (Ki 22 μM), and the diaminopurine, 6-benzylamino-2-(2-hydroxyethylamino)-9-methylpurine (Ki 3.3 μM).However these compounds were ineffective as inhibitors of the cytokinin-alanine sythase which was inhibited competitively by IAA (Ki 70 μM) and related compounds, especially 5,7-dichloro-IAA (Ki 0.4 μM).Certain urea derivatives were moderately effective inhibitors of the enzymes (Ki ca 100 μM). Key Word Index - Cytokinins; metabolism; cytokinin 7-glucosyltransferase; β-(9-cytokinin)alanine synthase; N6-substituted adenines; auxins; indoleacetic acid.
