所有图片(1)
别名:
(2R)-2-[[9-(1-Methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-butanol-1, (R)-2-(1-Hydroxybut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine, C&R8
经验公式（希尔记法）:
C24H29N7O
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质量水平
检测方案
≥95% (HPLC)
形式
powder
颜色
off-white
溶解性
DMSO: ≥10 mg/mL
储存温度
2-8°C
SMILES字符串
CC[C@H](CO)Nc1nc(NCc2ccc(cc2)-c3ccccn3)c4ncn(C(C)C)c4n1
InChI
1S/C24H29N7O/c1-4-19(14-32)28-24-29-22(21-23(30-24)31(15-27-21)16(2)3)26-13-17-8-10-18(11-9-17)20-7-5-6-12-25-20/h5-12,15-16,19,32H,4,13-14H2,1-3H3,(H2,26,28,29,30)/t19-/m1/s1
InChI key
HOCBJBNQIQQQGT-LJQANCHMSA-N
生化/生理作用
CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. Acts as a molecular glue to induce cyclin K degradation.
特点和优势
This compound is featured on the CDKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
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Nature, 585(7824), 293-297 (2020-06-05)
Molecular glue compounds induce protein-protein interactions that, in the context of a ubiquitin ligase, lead to protein degradation1. Unlike traditional enzyme inhibitors, these molecular glue degraders act substoichiometrically to catalyse the rapid depletion of previously inaccessible targets2. They are clinically
商品
Review properties, activators and inhibitors, and available products for researching cyclin-dependent kinases (CDKs).
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