PF-670462
Based on 8 publication(s) in Google Scholar
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.
- Purity: 99.24%
- CAS No.: 950980-98-0
- Formula: C19H20FN5
- Molecular Weight:337.39
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) PF-670462
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Proc Natl Acad Sci U S A. 2024 Jul 16;121(29):e2321647121. [Abstract]
- Proc Natl Acad Sci U S A. 2018 Aug 7;115(32):E7522-E7531. [Abstract]
- Antioxidants (Basel). 2021 Nov 26;10(12):1898. [Abstract]
- EMBO Rep. 2021 Jul 5;22(7):e51847. [Abstract]
- Biochem Biophys Res Commun. 2020 Mar 12;523(3):809-815. [Abstract]
- bioRxiv. 2025 January 15.
- J Pers Med. 2021 Sep 11;11(9):906. [Abstract]
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WB
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Cell Imaging/Staining
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WB
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WB
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WB
Biological Activity
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CK1δ |
CK1ε |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
8.24 μM
Compound: PF-670462
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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
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
19.23 μM
Compound: PF-670462
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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
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10.21203/rs.3.rs-23951/v1 |
| COS-7 | IC50 |
80.5 nM
Compound: 1, PF-670462
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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
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[PMID: 23919824] |
Chemical Information
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CAS No. 950980-98-0
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Appearance Solid
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Molecular Weight 337.39
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Formula C19H20FN5
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Color White to off-white
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SMILES
NC1=NC=CC(C2=C(C3=CC=C(F)C=C3)N=CN2C4CCCCC4)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (8)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Proc Natl Acad Sci U S A
FAM110A promotes mitotic spindle formation by linking microtubules with actin cytoskeleton. [Abstract]2024 Jul 16;121(29):e2321647121. PMID: 38995965
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.)
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Proc Natl Acad Sci U S A
Tumor promoter TPA activates Wnt/β-catenin signaling in a casein kinase 1-dependent manner. [Abstract]2018 Aug 7;115(32):E7522-E7531. PMID: 30038030
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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Antioxidants (Basel)
2021 Nov 26;10(12):1898. PMID: 34942999 -
EMBO Rep
CK1-mediated phosphorylation of FAM110A promotes its interaction with mitotic spindle and controls chromosomal alignment. [Abstract]2021 Jul 5;22(7):e51847. PMID: 34080749 -
Biochem Biophys Res Commun
IC261 suppresses progression of hepatocellular carcinoma in a casein kinase 1 δ/ε independent manner. [Abstract]2020 Mar 12;523(3):809-815. PMID: 31954519
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.
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J Pers Med
GPR30 Activation by 17β-Estradiol Promotes p62 Phosphorylation and Increases Estrogen Receptor α Protein Expression by Inducing Its Release from a Complex Formed with KEAP1. [Abstract]2021 Sep 11;11(9):906. PMID: 34575683
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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.
| 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 |