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HomeProduct name listOLOMOUCINE

OLOMOUCINE

Synonym(s):2-(Hydroxyethylamino)-6-benzylamino-9-methylpurine;Olomoucine;Olomoucine - CAS 101622-51-9 - Calbiochem

OLOMOUCINE Structural

What is OLOMOUCINE?

Chemical properties

white to off-white solid

The Uses of OLOMOUCINE

A purine derivative which inhibits cyclin-dependent kinases and induces G1 arrest

The Uses of OLOMOUCINE

A purine derivative which inhibits cyclin-dependent kinases and induces G1 arrest.

What are the applications of Application

Olomoucine is a potent and selective inhibitor of Cdc2 and ERK1

Definition

ChEBI: Olomoucine is a 9H-purine that is substituted by a (2-hydroxyethyl)nitrilo, benzylnitrilo and a methyl group at positions 2,6 and 9, respectively. It is a cyclin-dependent kinase inhibitor. It has a role as an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor. It is a member of 2,6-diaminopurines and a member of ethanolamines.

Biological Activity

Cyclin-dependent kinase inhibitor that competes for the ATP binding site of the kinase. Selectively inhibits cdc2/cyclin B (IC 50 = 7 μ M), cdk2/cyclin A (IC 50 = 7 μ M), cdk2/cyclin E (IC 50 = 7 μ M), cdk/p35 kinase (IC 50 = 3 μ M)? and ERK1/MAP kinase (IC 50 = 25 μ M). Arrests human fibroblasts in the G1 phase.

Biochem/physiol Actions

Olomoucine is a purine derivative which inhibits cyclin-dependent kinases and induces G arrest.

Enzyme inhibitor

This ATP site-competitive purine derivative (FW = 298.35 g/mol; CAS 101622-51-9), systematically named 6-benzylamino-2-[2-hydroxyethylamino]- 9-methylpurine, is a potent inhibitor of cyclin-dependent kinases, with an IC50 value of 7 μM for both cdk1 and cdk2 and an IC50 value of 3 μM for cdk5, arresting cells in G1. Olomoucine also inhibits cytokinin 7b-glucosyltransferase.

References

[1]. vesel j, havlicek l, strnad m, et al. inhibition of cyclin-dependent kinases by purine analogues. eur j biochem. 1994 sep 1;224(2):771-86.
[2]. abraham rt, acquarone m, andersen a, et al. cellular effects of olomoucine, an inhibitor of cyclin-dependent kinases. biol cell. 1995;83(2-3):105-20.
[3]. tian ds, xie mj, yu zy, et al. cell cycle inhibition attenuates microglia induced inflammatory response and alleviates neuronal cell death after spinal cord injury in rats. brain res. 2007 mar 2;1135(1):177-85.

Properties of OLOMOUCINE

Melting point: 120-130 °C
Boiling point: 579.6±60.0 °C(Predicted)
Density  1.36
storage temp.  -20°C
solubility  DMSO, Methanol (Slightly)
pka 14.55±0.10(Predicted)
form  Solid
color  White to off-white
CAS DataBase Reference 101622-51-9(CAS DataBase Reference)

Safety information for OLOMOUCINE

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P271:Use only outdoors or in a well-ventilated area.
P280:Wear protective gloves/protective clothing/eye protection/face protection.

Computed Descriptors for OLOMOUCINE

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