1241675-76-2

1241675-76-2 structure

Name: (R)-DRF053 dihydrochloride
Chemical Name: (2R)-2-[(9-Isopropyl-6-{[3-(2-pyridinyl)phenyl]amino}-9H-purin-2-yl)amino]-1-butanol dihydrochloride
CAS Number: 1241675-76-2
Molecular Formula: C₂₃H₂₉Cl₂N₇O
Molecular Weight: 490.429
Catalog: Signaling Pathways Cell Cycle/DNA Damage Casein Kinase
Create Date: 2020-01-14 18:06:09
Modify Date: 2024-04-03 10:45:11
(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.

Name	(2R)-2-[(9-Isopropyl-6-{[3-(2-pyridinyl)phenyl]amino}-9H-purin-2-yl)amino]-1-butanol dihydrochloride
Synonyms	(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)

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)