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MW 391.4 Da, Purity >98%. Cell-permeable, ATP-competitive p90 ribosomal S6 kinase (RSK) inhibitor (RSK1 IC50 = 31 nM; RSK2 IC50 = 24 nM; RSK3 IC50 = 18 nM; RSK4 IC50 = 15 nM). Selective (10 to 100-fold) over MST2, GSK-3 beta, MARK3, CK1 and Aurora B. Inhibits RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in cell models. May have RSK-independent effects on mTORC1-p70S6K and p21WAF1/CIP1 pathways.

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Key facts

CAS number
501437-28-1
Purity
> 98
Form
Solid
Molecular weight
391.4 Da
Molecular formula
C19H23F2N5O2
PubChem identifier
25023738
Nature
Synthetic

Target data

Alternative names

CK-1, CK1A, CKI-alpha, CKIa, Casein kinase 1 alpha 1, Casein kinase I isoform alpha, Clock regulator kinase, Csnk1a1, Down regulated in lung cancer, HLCDGP1, KC1A_HUMAN, PRO2975

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MW 391.4 Da, Purity >98%. Cell-permeable, ATP-competitive p90 ribosomal S6 kinase (RSK) inhibitor (RSK1 IC50 = 31 nM; RSK2 IC50 = 24 nM; RSK3 IC50 = 18 nM; RSK4 IC50 = 15 nM). Selective (10 to 100-fold) over MST2, GSK-3 beta, MARK3, CK1 and Aurora B. Inhibits RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in cell models. May have RSK-independent effects on mTORC1-p70S6K and p21WAF1/CIP1 pathways.

Key facts

Purity
> 98
PubChem identifier
25023738
Solubility

Soluble in DMSO to 25 mM.

Biochemical name
2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one
Biological description

Cell-permeable, ATP-competitive p90 ribosomal S6 kinase (RSK) inhibitor (RSK1 IC50 = 31 nM; RSK2 IC50 = 24 nM; RSK3 IC50 = 18 nM; RSK4 IC50 = 15 nM). Selective (10 to 100-fold) over MST2, GSK-3 beta, MARK3, CK1 and Aurora B. Inhibits RSK-mediated phorbol ester- and EGF -induced phosphorylation of glycogen synthase kinase-3β and LKB1 in cell models. May have RSK-independent effects on mTORC1-p70S6K and p21WAF1/CIP1 pathways.

Canonical SMILES
CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
InChI
InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
InChIKey
DTEKTGDVSARYDS-UHFFFAOYSA-N
IUPAC name
2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one

Storage

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C

Notes

Solutions in DMSO may be stored at -20°C for up to 1 month.

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