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Merck

557360

Roscovitine

≥95% (HPLC), solid, Cdk inhibitor, Calbiochem®

Synonyme(s) :

Roscovitine, 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Cdk7 Inhibitor I

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A propos de cet article

Formule empirique (notation de Hill) :
C19H26N6O
Numéro CAS:
186692-46-6
Poids moléculaire :
354.45
UNSPSC Code:
12352202
NACRES:
NA.77
MDL number:
MFCD02266401

Principaux documents

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Nom du produit

Roscovitine, A potent, reversible, and selective inhibitor of Cdks that exhibits about 10-fold greater efficacy towards p34-cdk1 and p33-cdk2 and 20-fold greater efficacy towards p33-cdk5 relative to Olomoucine.

SMILES string

[n]1(c2nc(nc(c2nc1)NCc3ccccc3)N[C@@H](CO)CC)C(C)C

InChI

1S/C19H26N6O/c1-4-15(11-26)22-19-23-17(20-10-14-8-6-5-7-9-14)16-18(24-19)25(12-21-16)13(2)3/h5-9,12-13,15,26H,4,10-11H2,1-3H3,(H2,20,22,23,24)/t15-/m1/s1

InChI key

BTIHMVBBUGXLCJ-OAHLLOKOSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

white to off-white

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Catégories apparentées

Legal Information

Sold under license of U.S. Patent 6,316,456
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Biochem/physiol Actions

Cell permeable: no
Primary Target
p34cdk1/cyclin B
Product does not compete with ATP.
Reversible: yes
Target IC50: 650 nM, 700 nM, 700 nM, 200 nM, against p34cdk1/cyclin B, p33cdk2/cyclin A, p33cdk2/cyclin E, p33cdk5/p35, respectively

Disclaimer

Toxicity: Standard Handling (A)

General description

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34cdk1 and p33cdk2 and twenty-fold greater efficacy towards p33cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34cdk1/cyclin B (IC50 = 650 nM), p33cdk2/cyclin A (IC50 = 700 nM), p33cdk2/cyclin E (IC50 = 700 nM), and p33cdk5/p35 (IC50 = 200 nM) by competing for the ATP binding domain of the kinases. Exhibits reduced sensitivity towards related kinases including ERK1 and ERK2 (IC50 = 34 µM and 14 µM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 µM, including p34cdk4/cyclin D1 and p40cdk6/cyclin D2. Compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle. A 50 mM (5 mg/282 µl) solution of Roscovitine (Cat. No. 557364) in DMSO is also available.

Other Notes

De Azevedo, W.F., et al. 1997. Eur. J. Biochem.243, 518.
Meijer, L., et al. 1997. Eur. J. Biochem.243, 527.
Meijer, L., et al. 1996. Trends Cell Biol. 6, 393.
Rudolph, B., et al. 1996. EMBO J. 15, 3053.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for at least 6 months at -20°C.

Classe de stockage

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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