557360

Roscovitine

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

• 동의어(들): Roscovitine, 2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine, Cdk7 Inhibitor I
• 실험식(Hill 표기법): C₁₉H₂₆N₆O
• CAS Number: 186692-46-6
• Molecular Weight: 354.45
• MDL number: MFCD02266401
• UNSPSC 코드: 12352202
• NACRES: NA.77

속성

• product name: 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.
• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze
• 색상: white to off-white
• solubility: DMSO: 10 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°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

설명

일반 설명

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34^cdk1 and p33^cdk2 and twenty-fold greater efficacy towards p33^cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34^cdk1/cyclin B (IC₅₀ = 650 nM), p33^cdk2/cyclin A (IC₅₀ = 700 nM), p33^cdk2/cyclin E (IC₅₀ = 700 nM), and p33^cdk5/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 p34^cdk4/cyclin D1 and p40^cdk6/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.

A potent, reversible, and selective inhibitor of cyclin-dependent kinases (cdks). Exhibits greater inhibitory potency compared to olomoucine (Cat. No. 495620). Inhibits p34 ^cdc2/cyclin B (IC₅₀ = 0.65 µM), p33 ^cdk2/cyclin A (IC₅₀ = 0.70 µM), p33 ^cdk2/cyclin E (IC₅₀ = 0.70 µM), and p33 ^cdk5/p35 (IC₅₀ = 0.20 µM) by competing for the ATP binding domain of these kinases. Exhibits very low sensitivity towards related kinases, such as 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 and compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle.

생화학적/생리학적 작용

Cell permeable: no

Primary Target
p34^cdk1/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

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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.

법적 정보

Sold under license of U.S. Patent 6,316,456

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable