(R)-DRF053 dihydrochloride|DRF 053;DRF053

Cas No.:	1241675-76-2
Chemical Name:	(R)-2-((9-isopropyl-6-((3-(pyridin-2-yl)phenyl)amino)-9H-purin-2-yl)amino)butan-1-ol dihydrochloride
Synonyms:	DRF 053;DRF053
SMILES:	C(O)[C@@H](NC1=NC(NC2=CC=CC(C3=NC=CC=C3)=C2)=C2C(=N1)N(C(C)C)C=N2)CC.[H]Cl.[H]Cl
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC46935	SR-1277	SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer.
DC44833	CK2/PIM1-IN-1	CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1, with IC50s of 3.787 μM and 4.327 μM for CK2 and PIM1, respectively. CK2/PIM1-IN-1 is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.
DC40122	TBCA	TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases.
DC28717	CKI-7	CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
DC11789	VU-WS113	VU-WS113 is a potent inhibitor of Wnt signaling with EC50 of 80 nM that selectively potentiates CK1α kinase activity..
DC11791	SSTC3	SSTC3 is a novel small-molecule CK1α activator with EC50 of 30 nM (WNT-driven reporter gene assay), Kd of 32 nM.
DC11252	BTX161	BTX161 is a thalidomide analog that mediates degradation of CKIα better than lenalidomide in human AML cells and activates DDR and p53, while stabilizing the p53 antagonist MDM2.
DC11787	Pyrvinium	An anthelmintic effective for pinworms that shows to be a potent inhibitor of Wnt signaling with EC50 of 10 nM, binds to all CK1 family members in vitro at low nanomolar concentrations and selectively potentiates CK1α kinase activity.
DC11788	Pyrvinium Iodide	An anthelmintic effective for pinworms that shows to be a potent inhibitor of Wnt signaling with EC50 of 10 nM, binds to all CK1 family members in vitro at low nanomolar concentrations and selectively potentiates CK1α kinase activity.
DC11949	SR-653234	A purine scaffold casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 of 160/540 nM, respectively..