PF-670462

Cat. No.: HY-15490A Purity: 99.24%: Data Sheet
COA

SDS
Handling Instructions
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PF-670462 is a selective CKI ε/δ inhibitor. PF-670462 effectively regulates the phase of the circadian rhythm.

For research use only. We do not sell to patients.

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of PF-670462:

PF-670462 dihydrochloride

Other Forms of PF-670462:

PF-670462 dihydrochloride In-stock

8 Publications Citing Use of MCE PF-670462

Cell Imaging/Staining

: PF-670462 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Jul 16;121(29):e2321647121. [Abstract]; HEK293 cells transfected with indicated constructs were arrested in mitosis with NDZ and treated or not with PF-670462 dihydrochloride (1 µM) for 6 h. Pull-down from cell extracts was performed using GFP-Trap, and binding of tubulin and actin was determined by immunoblotting (n = 2).

: PF-670462 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Jul 16;121(29):e2321647121. [Abstract]; Representative live image sequence of RPE-sAC-GFP cells treated with DMSO or with CK1 inhibitor PF-670462 dihydrochloride (1 µM; 15 min). Cells were imaged every 25 s, time 0 was set to indicate NEB. The results showed that inhibition of CK1 by PF-670462 dihydrochloride impaired organization of the spindle actin in prophase cells. (Scale bar, 10 μm.)

: PF-670462 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Mar 12;523(3):809-815. [Abstract]; Immunoblot analysis of cells treated with IC261 or PF-670462 dihydrochloride for 48 h. GAPDH served as a loading control.

: PF-670462 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]; The recombinant CK1ε phosphorylates Thr1479 of GST-LRP6 mini fragment in vitro, and TPA enhances CK1ε kinase activity. GST-LRP6 mini fragment fusion protein was incubated with recombinant CK1ε in the presence of 200 μM ATP with or without 160 μM TPA or 2 μM PF-670462 dihydrochloride as indicated. The detection of the phosphorylation of Thr1479 was performed by immunoblotting using an anti–phospho-LRP6 (Thr1479) antibody. Thr1479 phosphorylation levels were quantitated by densitometry and normalized to GST-LRP6 mini levels. Quantitated results are displayed (Right). The results showed that PF670462 (specific CK1 inhibitor) markedly suppresses CK1ε-triggered LRP6 phosphorylation at Thr1479. Phosphorylation of Thr1479 is indicated by an asterisk.

: PF-670462 purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]; TPA rescued the inhibitory effect of PF-670462 dihydrochloride on the kinase activity of CK1ε. The GST-LRP6 mini fusion protein was incubated with CK1ε in the absence or presence of 2 μM PF-670462 dihydrochloride or the indicated amounts of TPA. Thr1479 phosphorylation of GST-LRP6 mini was measured by immunoblotting using anti–phospho-LRP6 (Thr1479) antibody, indicated by p-LRP6 (Thr1479). Phosphorylation of Thr1479 is indicated by an asterisk.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

PF-670462 is a selective CKI ε/δ inhibitor. PF-670462 effectively regulates the phase of the circadian rhythm^[1].

IC₅₀ & Target^[1]

CK1δ

CK1ε

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	80.5 nM Compound: 1, PF-670462	Inhibition of human CK1 delta transfected in african green monkey cos7 cells after overnight incubation by whole cell assay Inhibition of human CK1 delta transfected in african green monkey cos7 cells after overnight incubation by whole cell assay	[PMID: 23919824]
Caco-2	CC₅₀	8.24 μM Compound: PF-670462	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	19.23 μM Compound: PF-670462	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1

Molecular Weight

337.39

Formula

C₁₉H₂₀FN₅

CAS No.

950980-98-0

Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCCCC4)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 35 mg/mL (103.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9639 mL	14.8196 mL	29.6393 mL
5 mM	0.5928 mL	2.9639 mL	5.9279 mL
10 mM	0.2964 mL	1.4820 mL	2.9639 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.24%

Select Batch:

Data Sheet (278 KB) SDS (394 KB)

COA (257 KB) HNMR (180 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Sprouse J, et al. Chronic treatment with a selective inhibitor of casein kinase I delta/epsilon yields cumulative phase delays in circadian rhythms. Psychopharmacology (Berl). 2010 Jul;210(4):569-76. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9639 mL	14.8196 mL	29.6393 mL	74.0982 mL
	5 mM	0.5928 mL	2.9639 mL	5.9279 mL	14.8196 mL
	10 mM	0.2964 mL	1.4820 mL	2.9639 mL	7.4098 mL
	15 mM	0.1976 mL	0.9880 mL	1.9760 mL	4.9399 mL
	20 mM	0.1482 mL	0.7410 mL	1.4820 mL	3.7049 mL
	25 mM	0.1186 mL	0.5928 mL	1.1856 mL	2.9639 mL
	30 mM	0.0988 mL	0.4940 mL	0.9880 mL	2.4699 mL
	40 mM	0.0741 mL	0.3705 mL	0.7410 mL	1.8525 mL
	50 mM	0.0593 mL	0.2964 mL	0.5928 mL	1.4820 mL
	60 mM	0.0494 mL	0.2470 mL	0.4940 mL	1.2350 mL
	80 mM	0.0370 mL	0.1852 mL	0.3705 mL	0.9262 mL
	100 mM	0.0296 mL	0.1482 mL	0.2964 mL	0.7410 mL

PF-670462 Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-670462950980-98-0PF670462PF 670462Casein Kinasecircadian rhythmInhibitorinhibitorinhibit

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