(R)-CR8 (trihydrochloride)
- CAS号:1786438-30-9
- 英文名:(R)-CR8 (trihydrochloride)
- 中文名:(R)-CR8 (trihydrochloride)
- CBNumber:CB65848911
- 分子式:C24H30ClN7O
- 分子量:468
- MOL File:1786438-30-9.mol
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 62.5 mg/mL (115.54 mM)
- 形态 :Solid
- 颜色 :White to off-white
(R)-CR8 (trihydrochloride)性质、用途与生产工艺
- 生物活性 (R)-CR8 (CR8) trihydrochloride 是 Roscovitine 的第二代类似物，是一种有效的 CDK1/2/5/7/9 抑制剂。(R)-CR8 trihydrochloride 抑制 CDK1/cyclin B (IC50=0.09 μM)、CDK2/cyclin A (0.072 μM)、CDK2/cyclin E (0.041 μM)、CDK5/p25 (0.11 μM)、CDK7/cyclin H (1.1 μM)、CDK9/cyclin T (0.18 μM) 和 CK1δ/ε (0.4 μM)。(R)-CR8 trihydrochloride 诱导细胞凋亡并具有神经保护作用。(R)-CR8 trihydrochloride 作为一种分子胶降解剂来消耗细胞周期蛋白 K。
-
靶点
CDK1/cyclinB1
0.09 μM (IC 50 )
cdk2/cyclin A
0.072 μM (IC 50 )
CDK2/cyclinE
0.041 μM (IC 50 )
Cdk5/p25
0.11 μM (IC 50 )
CDK7/cyclin H
1.1 μM (IC 50 )
CDK9/Cyclin T
0.18 μM (IC 50 )
CK1δ/ε
0.4 μM (IC 50 )
-
体外研究
(R)-CR8 (CR8) trihydrochloride (0.1-100 μM; 48 hours) is a potent inducer of apoptotic cell death with an IC 50 of 0.49 μM for SH-SY5Y cell line.
(R)-CR8 trihydrochloride (0.25-10 μM) induces a dose-dependent induction of poly-(ADP-ribose)polymerase (PARP) cleavage.
The CDK-bound form of (R)-CR8 trihydrochloride has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradationApoptosis Analysis
Cell Line: SH-SY5Y cell line Concentration: 0.1, 1, 10, 100 μM Incubation Time: 24 hours Result: Reduced cell survival in a dose-dependent manner. -
体内研究
(R)-CR8 trihydrochloride (5 mg/Kg; i.p.) results in a significant reduction in lesion size at 28 days in histological assessment.
Animal Model: Adult (10 to 12 weeks old) male Sprague-Dawley rats (310 to 330 g) Dosage: 5 mg/Kg Administration: i.p. Result: Resulted in a significant reduction in lesion size.
- 更新日期：2025/02/08
- 产品编号：HY-18340A
- 产品名称：(R)-CR8 (trihydrochloride) (R)-CR8 trihydrochloride
- CAS编号：1786438-30-9
- 包装：5mg
- 价格：900元
- 更新日期：2025/02/08
- 产品编号：HY-18340A
- 产品名称：(R)-CR8 (trihydrochloride) (R)-CR8 trihydrochloride
- CAS编号：1786438-30-9
- 包装：10mM * 1mLin DMSO
- 价格：1071元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：32161
- 优势度：58
- 公司名称：InvivoChem
- 联系电话：+1-708-310-1919 +1-13798911105
- 电子邮件：sales@invivochem.cn
- 国家：美国
- 产品数：6391
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57505
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
