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Merck
CN

SML0795

PF-670462

≥98% (HPLC)

Synonym(s):

PF670462, 4-[3-Cyclohexyl-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-ylamine dihydrochloride

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About This Item

Empirical Formula (Hill Notation):
C19H20FN5 · 2HCl
CAS Number:
950912-80-8
Molecular Weight:
410.32
UNSPSC Code:
12352200
NACRES:
NA.77

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Product Name

PF-670462, ≥98% (HPLC)

SMILES string

Fc1ccc(cc1)c2nc[n](c2c4nc(ncc4)N)C3CCCCC3.Cl.Cl

InChI

1S/C19H20FN5.2ClH/c20-14-8-6-13(7-9-14)17-18(16-10-11-22-19(21)24-16)25(12-23-17)15-4-2-1-3-5-15;;/h6-12,15H,1-5H2,(H2,21,22,24);2*1H

InChI key

PSNKGVAXBSAHCH-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

Quality Level

100

Related Categories

Biochem/physiol Actions

PF-670462 is a selective inhibitor of the δ- and ε-isoforms of casein kinase I, with IC50 values of 7.7 and 14 nM respectively, and >30 selectivity relative to 42 other kinases tested. Casein kinase Iε phosphorylates PER proteins, which are involved in setting the period of the circadian pacemaker or clock. PF-670462 is potent (IC50 7.7 nM) and effective in vivo (i.e. it induces profound phase delays in circadian periodicity).
PF-670462 is a selective inhibitor of the δ- and ε-isoforms of casein kinase I.
PF-670462 is also termed as 4-[1-cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine dihydrochloride). It participates in ceramide transfer between Golgi and ER (endoplasmic reticulum) compartments. PF-670462 affects actin filament consolidation. It also hinders the stability at the front edge of cells treated with N-formyl Met-Leu-Phe.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000181510
0000181510
0000063356
0000063357
0000127310

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The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads, 1362-1362 (2017)
Combined Pharmacological and Genetic Manipulations Unlock Unprecedented Temporal Elasticity and Reveal Phase-Specific Modulation of the Molecular Circadian Clock of the Mouse Suprachiasmatic Nucleus.
Patton AP, et al.
The Journal of Neuroscience, 36(36), 9326-9341 (2016)
David A Hicks et al.
Neurochemical research, 45(6), 1354-1364 (2019-07-08)
Motor neuron disease (MND) is a progressive neurodegenerative disease with no effective treatment. One of the principal pathological hallmarks is the deposition of TAR DNA binding protein 43 (TDP-43) in cytoplasmic inclusions. TDP-43 aggregation occurs in both familial and sporadic
Lucian B Tomaz et al.
Journal of cell science, 135(21) (2022-10-12)
The gene mutated in colorectal cancer (MCC) encodes a coiled-coil protein implicated, as its name suggests, in the pathogenesis of hereditary human colon cancer. To date, however, the contributions of MCC to intestinal homeostasis and disease remain unclear. Here, we

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