(R)-DRF053 dihydrochloride

Names

[ Name ]:
(R)-DRF053 dihydrochloride

[Synonym ]:
(2R)-2-[(9-Isopropyl-6-{[3-(2-pyridinyl)phenyl]amino}-9H-purin-2-yl)amino]-1-butanol dihydrochloride
(2R)-2-[(9-Isopropyl-6-{[3-(pyridin-2-yl)phenyl]amino}-9H-purin-2-yl)amino]butan-1-ol dihydrochloride
1-Butanol, 2-[[9-(1-methylethyl)-6-[[3-(2-pyridinyl)phenyl]amino]-9H-purin-2-yl]amino]-, (2R)-, hydrochloride (1:2)

Biological Activity

[Description]:

(R)-DRF053 dihydrochloride (DRF053) is a potent, cell-permeable, dual CK1/CDK inhibitor with IC50 of 14 nM, 220 nM and 80 nM for CK1, CDK5/p25 and CDK1/cyclin B, respectively; exhibits antiproliferative activity against human neuroblastoma SH-SY5Y cells with EC50 of 17.2 uM, prevents the CK1-dependent production of amyloid-beta in a cell model; specifically increases the number of duct-derived β-cells without affecting their proliferation.

[References]

References 1. Oumata N, et al. J Med Chem. 2008 Sep 11;51(17):5229-42. 2. Zelenak C, et al. Cell Physiol Biochem. 2012;29(1-2):171-80. 3. Liu KC, et al. Diabetes. 2018 Jan;67(1):58-70. View Related Products by Target Casein Kinase Cyclin-dependent Kinase (CDK)

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₉Cl₂N₇O

[ Molecular Weight ]:
490.429

[ Exact Mass ]:
489.181061

Related Compounds

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