Iso-Olomoucine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: ≥ 1 mM for Cdk5
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]
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[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).
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 298.3 |
Cas No. | 101622-50-8 |
Formula | C15H18N6O |
Solubility | ≤0.3mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide |
Chemical Name | 2-[[7-methyl-6-[(phenylmethyl)amino]-7H-purin-2-yl]amino]-ethanol |
SDF | Download SDF |
Canonical SMILES | OCCNC1=NC(N=CN2C)=C2C(NCC3=CC=CC=C3)=N1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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