Cat. No.: HY-15490A

PF-670462

Name: PF-670462
Brand: MedChemExpress
SKU: HY-15490A
Price: 85.00 USD
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8 Cited Publications

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Based on 8 publication(s) in Google Scholar

PF-670462 is a selective CK1δ and CK1δε inhibitor (K_i of 10 nM and 50 nM, respectively). PF-670462 is also a ZDHHC8-specific inhibitor (K_d 15.9 μM). PF-670462 inhibits CK1-mediated LRRK2 phosphorylation. PF-670462 blocks PER phosphorylation and CK1δ/ε-dependent TGF-β signaling. PF-670462 reduces GPX4 palmitoylation, sensitizing tumor cells to Ferroptosis inducers. PF-670462 can be used for research on Parkinson's disease, NRAS-mutant melanoma, pulmonary fibrosis, chronic lymphocytic leukemia, diabetic nephropathy, and melanoma.

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Pureté : 99.24%
CAS No.: 950980-98-0
Formule: C₁₉H₂₀FN₅
Masse moléculaire:337.39

Stockage:

-20°C, protect from light

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

PF-670462 Chemical Structure

CAS No.: 950980-98-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]^[8]

CK1δ

10 nM (Ki)

CK1ε

50 nM (Ki)

GPX4

Voir tous les produits spécifiques à Isoform Casein Kinase :

Voir tous les produits spécifiques à Isoform TGF-beta/Smad :

Smad1
Smad3

Voir tous les produits spécifiques à Isoform Glutathione Peroxidase :

GPX1
GPX4

Cellular Effect

Cell Line	Type	Value	Description	References
SK-MEL-103	IC50	2.37 μM	Antiproliferative activity against human SK-MEL-103 NRASQ61R melanoma cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human SK-MEL-103 NRASQ61R melanoma cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	5433010
SK-MEL-2	IC50	2.42 μM	Antiproliferative activity against human SK-MEL-2 NRASQ61R melanoma cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Antiproliferative activity against human SK-MEL-2 NRASQ61R melanoma cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	5433010

In Vitro

Anti-cancerCytokines & ChemokinesOthers

Anti-cancer

PF-670462 (1.25-10 μM; 24 h) does not degrade CK1δ in SK-MEL-103 NRAS^Q61R melanoma cells, with a degradation rate of 0% at 5 μM and no degradation across the 1.25-10 μM range^[3].
PF-670462 (72 h) inhibits the proliferation of SK-MEL-103 and SK-MEL-2 NRAS^Q61R melanoma cells, with IC₅₀ values of 2.37 μM and 2.42 μM, respectively^[3].
PF670462 (3-10 μM; 30 min) prevents TGF-β-induced loss of E-cadherin in A549 cells^[4].

Anti-cancer

Cytokines & Chemokines

PF670462 (0.1-10 μM) completely prevents TGF-β-induced changes in EMT markers in A549 cells^[4].

Others

PF670462 (3 μM; 30 min) reduces the stiffness of spheroids derived from primary lung fibroblasts from IPF^[4].
PF670462 (1 μM) inhibits TGF-β-induced COL1A, CTGF, and αSMA mRNA expression in primary lung fibroblast cultures^[4].
PF670462 (10 μM) only slightly reduces bFGF-induced mitogenic effects in lung fibroblasts^[4].
PF-670462 (10 μM) increases RAD21 protein levels and stability in HK-2 cells while decreasing RAD21 S-palmitoylation^[7].
PF-670462 (10 μM) reverses the HG-induced increase in cytoplasmic RAD21-HSPA8 colocalization in HG-stimulated HK-2 cells^[7].
PF-670462 (5-10 µM; 16 h) selectively reduces zDHHC8 protein abundance in HT-1080 and HEK293T cells^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[3]

Cell Line:

SK-MEL-103 NRASQ61R melanoma cells
Concentration:

1.25, 2.5, 5, and 10 μM (dose-series); 5 μM (degradation-efficiency table)
Incubation Time:

24 h (dose-series); 24 h (degradation-efficiency table)
Result:

Produced 0% CK1δ degradation at 5 μM after 24 h.
No CK1δ degradation was observed at 1.25, 2.5, 5, or 10 μM after 24 h.

Western Blot Analysis^[8]

Cell Line:

HT-1080 cells and HEK293T cells expressing Flag-tagged zDHHC family members
Concentration:

0, 5 and 10 µM (HT-1080); indicated concentrations (HEK293T)
Incubation Time:

16 h
Result:

Decreased zDHHC8 protein levels at 5 and 10 µM.
Among the zDHHC family members tested, selectively reduced zDHHC8 protein abundance, whereas the other zDHHC proteins were not comparably reduced.

In Vivo

Adaptive ImmunityAnti-cancerFerroptosisOthers

Adaptive Immunity

PF-670462 (30 mg/kg/day; intraperitoneal injection; once daily; day 3 to day 13) reduces collagen deposition and immune cell infiltration in the 14-day Bleomycin model^[4].

Adaptive Immunity

Anti-cancer

PF-670462 (10 mg/kg; intraperitoneal injection; once every 2 days; four doses in total) inhibits B16-F10 tumor growth and enhances intratumoral CD8⁺ cytotoxic T cell responses in mice^[8].

Anti-cancer

PF-670462 (30 mg/kg; intraperitoneal injection; once every other day; 18 days) produces time-dependent tumor growth inhibition in the BALB/c nude mouse SK-MEL-103 NRAS^Q61R xenograft model but does not degrade CK1δ in tumor tissue^[3].
PF-670462 (10 mg/kg; intraperitoneal injection; once every 2 days; five doses in total; starting from day 4) inhibits B16-F10 lung metastasis and prolongs in vivo survival in mice^[8].

Anti-cancer

Ferroptosis

PF-670462 (10 mg/kg; intraperitoneal injection; once every 2 days; four doses total) inhibits B16-F10 tumor growth in mice through a ferroptosis-dependent mechanism^[8].

Others

PF-670462 (50 mg/kg; intraperitoneal injection; administered four times within 30 h) reduces lung LRRK2 protein and S935 phosphorylation levels as well as kidney S935 phosphorylation levels in C57Bl/6J wild-type mice, while no brain S935 dephosphorylation is detected^[1].
PF-670462 (10 mg/kg/day; intraperitoneal injection; once daily, 3 days before acute fear conditioning) increases Arc expression in the right amygdala of healthy male C57BL/6J mice after acute aversive learning^[2].
PF-670462 (30 mg/kg/day; intraperitoneal injection; once daily; day -1 to day 3) attenuates early Bleomycin (HY-108345)-induced p38 activation and fibrotic gene induction in mice^[4].
PF-670462 (0.3-3.0 mg/mL; inhalation; once daily for 15 minutes; day 8 to day 20) attenuates established Bleomycin-induced fibrosis and BAL cell infiltration in female mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57Bl/6J (wild-type)^[1]
Dosage:

50 mg/kg
Administration:

i.p.; four injections over 30 h
Result:

In brain, no LRRK2 S935 dephosphorylation was observed.
In lung, LRRK2 S935 phosphorylation and total LRRK2 protein levels were reduced.
In kidney, LRRK2 S935 phosphorylation was reduced, and full-length and truncated LRRK2 protein levels showed a trend toward reduction.

Animal Model:

C57BL/6J (male, wild-type, 2-4 months old)^[2]
Dosage:

10 mg/kg/day
Administration:

i.p.; once daily at ZT10; 3 days before acute fear conditioning
Result:

Left amygdala Arc expression did not differ among groups.
Right amygdala Arc was higher after exposure to the learning paradigm than in either no-learning or learning-only control groups.
In the dorsal hippocampus, the learning paradigm increased Arc expression in control mice, and increased Arc was observed only in the dorsal hippocampus after exposure to learning; there was no difference between the learning and learning-only groups.
In the ventral hippocampus, the learning paradigm increased Arc expression in control mice, but Arc was not increased relative to no-learning controls after exposure to learning, and there was no difference between the learning and learning-only groups.

Animal Model:

BALB/c nude (female, 5-6 weeks old)^[3]
Dosage:

30 mg/kg
Administration:

i.p.; every other day; 18 days
Result:

Time-dependent tumor growth inhibition was observed, with tumor/control ratios comparable to 8u.
Tumor-tissue Western blotting showed that CK1δ was retained without degradation (Figure 7E).

Animal Model:

C57Bl/6 (6-8 weeks, 20-25 g)^[4]
Dosage:

30 mg/kg/day
Administration:

i.p.; once daily; day -1 to day 3
Result:

Prevented the bleomycin-induced increase in p38 MAPK phosphorylation.
Reduced IL-6 and TIMP-1 gene induction and prevented COL-1A and COL-3 induction.
BAL immunoreactive IL-6 was reduced, and ARNTL expression was suppressed.

Animal Model:

C57Bl/6 (6-8 weeks, 20-25 g)^[4]
Dosage:

30 mg/kg/day
Administration:

i.p.; once daily; day 3 to day 13
Result:

Attenuated bleomycin-induced accumulation of lung hydroxyproline and reduced the number of infiltrating immune cells in BAL fluid.

Animal Model:

C57Bl/6 (6-8 weeks, 20-25 g)^[4]
Dosage:

30 mg/kg/day
Administration:

i.p.; once daily; day 7 (Methods states day 8) to day 21
Result:

Reduced bleomycin-induced increases in lung hydroxyproline, lung wet weight, BAL fluid infiltrating cells, and BAL fluid protein.

Animal Model:

C57Bl/6 (female, 6-8 weeks, 20-25 g)^[4]
Dosage:

0.3-3.0 mg/mL
Administration:

inhalation; 15 minutes once daily; day 8 to day 20
Result:

Reduced hydroxyproline content, BALF cell influx, and fibrogenic gene expression at day 21.
Effects did not show dose-related differences across the tested range.

Animal Model:

C57BL/6J^[8]
Dosage:

10 mg/kg
Administration:

i.p.; every 2 days; four doses
Result:

Reduced B16-F10 tumor growth and tumor weight relative to vehicle.
Increased tumor lipid peroxidation and 4-HNE staining.
Increased CD8⁺ cytotoxic T-cell infiltration and the numbers of IFNγ⁺, TNF⁺, and GZMB⁺ CD8⁺ cytotoxic T cells in tumors.

Animal Model:

C57BL/6J^[8]
Dosage:

10 mg/kg
Administration:

i.p.; every 2 days; four doses
Result:

Reduced B16-F10 tumor growth and tumor weight.
Liproxstatin-1 reversed the antitumor effect.

Animal Model:

C57BL/6J^[8]
Dosage:

10 mg/kg
Administration:

i.p.; every 2 days; five doses; starting on day 4
Result:

Reduced the number and size of metastatic lung nodules in B16-F10 tumor-bearing mice and prolonged overall survival.

Animal Model:

Rag2−/−^[8]
Dosage:

10 mg/kg
Administration:

i.p.; every 2 days; five doses; starting on day 6
Result:

Lost antitumor efficacy in Rag2^−/− mice.
Reconstitution with CD8⁺ T cells, but not B cells, restored the antitumor effect.

Related Protocols :

Chemical Information

CAS No. 950980-98-0
Appearance Solid
Masse moléculaire 337.39
Formule C₁₉H₂₀FN₅
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

-20°C, protect from light

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

Publications (8)

All Cell Imaging/StainingWB

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Journal Impact Factor

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.)
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.
Antioxidants (Basel)

Glucose Activates Lysine-Specific Demethylase 1 through the KEAP1/p62 Pathway. [Abstract]

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.
bioRxiv

2025 January 15.
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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (300 KB)
SDS (394 KB)
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- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. De Wit T, et al. Inhibition of LRRK2 or Casein Kinase 1 Results in LRRK2 Protein Destabilization. Molecular neurobiology. 2019 Aug;56(8):5273-5286.

[2]. Mahoney H, et al. Inhibition of casein kinase 1 δ/ε improves cognitive performance in adult C57BL/6J mice. Sci Rep. 2021 Feb 26;11(1):4746. [Content Brief]

[3]. Zhang C, et al. Discovery and Synthesis of Selective Casein Kinase 1δ Degraders for Suppressing Oncogenic NRAS-Mutant Melanoma. Journal of Medicinal Chemistry.

[4]. Keenan CR, et al. Casein kinase 1δ/ε inhibitor, PF670462 attenuates the fibrogenic effects of transforming growth factor-β in pulmonary fibrosis. Frontiers in pharmacology. 2018 Jul 10;9:738. [Content Brief]

[5]. Chan P, et al. Watching the clock in glioblastoma. Neuro-oncology. 2023 Nov 02;25(11):1932-1946. [Content Brief]

[6]. Park S. Identification of Potential Pharmacological Compounds to Promote Healthy Aging and Metabolic Health Through the Circadian Clock Using Neurospora crassa[D]. , 2023.

[7]. Chen W, et al. ZDHHC8-mediated S-palmitoylation of RAD21 causes mitochondrial dysfunction in diabetic nephropathy via inhibiting ACSM3 transcription. Cell death and differentiation. 2026 Jul 15. [Content Brief]

[8]. Zhou L, et al. Palmitoylation of GPX4 via the targetable ZDHHC8 determines ferroptosis sensitivity and antitumor immunity. Nature cancer. 2025 May;6(5):768-785. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

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PF-670462

8 Cited Publications

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PF-670462

Publications Citing Use of MedChemExpress (MCE) PF-670462

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