Art. -Nr.: HY-107778

PF-9366

18 Cited Publications

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Based on 18 publication(s) in Google Scholar

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC₅₀ of 420 nM and a K_d of 170 nM.

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Reinheit: 99.94%
CAS. Nr.: 72882-78-1
Formel: C₂₀H₁₉ClN₄
Molecular Weight:350.84

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF-9366 Chemical Structure

CAS. Nr.: 72882-78-1

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (18)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC₅₀ of 420 nM and a K_d of 170 nM.

IC₅₀ & Target

IC50: 420 nM (Mat2A)^[1]
Kd: 170 nM (Mat2A)^[1]

In Vitro

PF-9366 is a Mat2A inhibitor, with an IC₅₀ of 420 nM and a K_d of 170 nM. PF-9366 displays no substantial off-target activity in GPCRs, neurotransporters, phosphodiesterases, and ion channels. PF-9366 has inhibitory activity against Mat2A in cancer cells. PF-9366 inhibits cellular S-Adenosyl-L-methionine (SAM) production with an IC₅₀ of 1.2 μM in H520 lung carcinoma cells. PF-9366 is more potent in Huh-7 cells against SAM synthesis, with an IC₅₀ of 255 nM, and also suppresses the proliferation of cells with an IC₅₀ of 10 μM.

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

Chemical Information

CAS. Nr. 72882-78-1
Appearance Solid
Molecular Weight 350.84
Formel C₂₀H₁₉ClN₄
Color White to off-white
SMILES

CN(C)CCC1=NN=C2N1C3=CC=C(Cl)C=C3C(C4=CC=CC=C4)=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

All RT-PCRWBCell Proliferation/Viability AssayIFIn Vivo Efficacy Study

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Journal Impact Factor

Cell

Metabolic Regulation of the Epigenome Drives Lethal Infantile Ependymoma. [Abstract]

2020 Jun 11;181(6):1329-1345.e24. PMID: 32445698
Nat Cancer

Loss of MAT2A compromises methionine metabolism and represents a vulnerability in H3K27M mutant glioma by modulating the epigenome. [Abstract]

2022 May;3(5):629-648. PMID: 35422502
Immunity

Multiomics analyses reveal a critical role of selenium in controlling T cell differentiation in Crohn's disease. [Abstract]

2021 Aug 10;54(8):1728-1744.e7. PMID: 34343498
Cancer Commun (Lond)

Unfolded protein response kinase PERK supports survival and metastasis of circulating tumor cell clusters via SAM synthesis and H3K4me3-dependent PDGFB signaling. [Abstract]

2025 Nov 10. PMID: 41212905
Nat Metab

Vitamin B12 is a limiting factor for induced cellular plasticity and tissue repair. [Abstract]

2023 Nov;5(11):1911-1930. PMID: 37973897
Mol Cell

mTORC1 stimulates cell growth through SAM synthesis and m6A mRNA-dependent control of protein synthesis. [Abstract]

2021 May 20;81(10):2076-2093.e9. PMID: 33756106

PF-9366 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]

Relative incorporation of the radiolabel from (C³H3)-methionine into total RNA from wild-type HeLa cells grown in the absence of serum and treated with vehicle, insulin (500 nM), rapamycin (20 nM) or MAT2A inhibitor (PF-9366, 10 μM) for 24 hours.

PF-9366 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]

Cancer cell lines treated with vehicle or MAT2Ai (PF-9366, 10 μM) were grown in 1% serum for 72 hours, and Cell Titer-Glo measurements were performed every 24 hours.

PF-9366 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]

PDX of breast cancer bearing TP53 and PIK3CA^H1047 mutations was subcutaneously injected into the flanks of NOD.Cg-Prkdcscid Il2rgtm1Wj1/SzJ mice. Mice were randomized 1:1 to receive vehicle (PEG/Tween 5%) or MAT2Ai (PF-9366, 50 mg/kg), and tumor volume was monitored over time.
Mol Cell

One-Carbon Metabolism Supports S-Adenosylmethionine and Histone Methylation to Drive Inflammatory Macrophages. [Abstract]

2019 Sep 19;75(6):1147-1160.e5. PMID: 31420217
Nat Commun

Lipoic acid functions in Paneth cells to prevent human intestinal stem cell aging. [Abstract]

2025 Jul 1;16(1):6016. PMID: 40593722
Nat Commun

Epigenome-wide impact of MAT2A sustains the androgen-indifferent state and confers synthetic vulnerability in ERG fusion-positive prostate cancer. [Abstract]

2024 Aug 6;15(1):6672. PMID: 39107274
Sci China Life Sci

Targeting methionine-induced pyroptosis enhances anti-tumor immunity. [Abstract]

2026 May;69(5):1604-1619. PMID: 41793590
EMBO J

Attenuation of SARS-CoV-2 replication and associated inflammation by concomitant targeting of viral and host cap 2'-O-ribose methyltransferases. [Abstract]

2022 Sep 1;41(17):e111608. PMID: 35833542
Cancer Immunol Res

mTOR signaling promotes rapid m6A mRNA methylation to regulate NK-cell activation and effector functions. [Abstract]

2024 Aug 1;12(8):1039-1057. PMID: 38640466
J Orthop Translat

Targeting MAT2A synergistically induces DNA damage in osteosarcoma cells through EZH2-mediated H3K27me3 modification. [Abstract]

2025 Oct 16:55:346-359. PMID: 41146859

PF-9366 purchased from MedChemExpress. Usage Cited in: J Orthop Translat. 2025 Oct 16:55:346-359. [Abstract]

Western blot analysis of MAT2A protein levels in 143B cells treated with PF-9366 at different concentrations (0.5 μM, 1 μM, 2 μM, 4 μM, 6 μM) for 72 h.

PF-9366 purchased from MedChemExpress. Usage Cited in: J Orthop Translat. 2025 Oct 16:55:346-359. [Abstract]

Immunofluorescence staining of DAPI and γH2AX in osteosarcoma cells treated with GSK126 and PF-9366.
PLoS Biol

Dynamic assembly of the mRNA m6A methyltransferase complex is regulated by METTL3 phase separation. [Abstract]

2022 Feb 10;20(2):e3001535. PMID: 35143475
Front Cell Dev Biol

SYVN1-MTR4-MAT2A Signaling Axis Regulates Methionine Metabolism in Glioma Cells. [Abstract]

2021 Mar 30:9:633259. PMID: 33859984
J Biol Chem

Extracellular 5'-methylthioadenosine inhibits intracellular symmetric dimethylarginine protein methylation of FUSE-binding proteins. [Abstract]

2022 Sep;298(9):102367. PMID: 35963436
Cell J

Inhibition of MAT2A-Related Methionine Metabolism Enhances The Efficacy of Cisplatin on Cisplatin-Resistant Cells in Lung Cancer. [Abstract]

2022 Apr;24(4):204-211. PMID: 35674024
SSRN

2024 Jul 02.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 10 mg/mL (28.50 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

2.8503 mL

14.2515 mL

28.5030 mL

5 mM

0.5701 mL

2.8503 mL

5.7006 mL

10 mM

0.2850 mL

1.4252 mL

2.8503 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

The Mat2A and Mat2B proteins are extensively dialyzed into a buffer containing 150 mM KCl, 25 mM HEPES, pH 7.4, 5 mM MgCl₂, 5% (v/v) glycerol, 2 mM TCEP. Concentrations are determined spectrophotometrically using an ɛ280 of 44,350 /M.cm for Mat2A and an ɛ280 of 36,440 /M.cm for Mat2B. Compounds (PF-9366) are diluted from 100% DMSO stocks into a buffer without DMSO. In a typical experiment, nineteen 15 μL injections of 200 μM compound or 30-35 μM Mat2B are made into 10 μM Mat2A on a VP ITC or nineteen 2 μL injections of 200 μM compound into 10 μM Mat2A on an Auto iTC200. Data are analyzed and fit to a simple 1:1 binding model^[1].

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

Cell Assay^[1]

Huh-7 cells are seeded at a concentration of 15,000 cells per well for 6-h incubation with compound (PF-9366) and 4,000 cells per well for 72-h incubation with compound in 96-well plates in 200 μL of growth medium. NCI-H520 MAT2B knockdown cells are seeded at a concentration of 20,000 cells per well for 6 h incubation or 10,000 cells per well for 72 h incubation with compound in 96 well plates in 200 μL of growth medium. Cells are allowed to attach overnight at 37°C with 5% CO₂. A 5× solution of cycloleucine is prepared fresh from powder stock in growth medium. Other compounds (PF-9366) are diluted in 100% DMSO using a three-fold dilution scheme and further diluted in growth medium to give 0.5% DMSO final. Consistency of cellular confluence for each cell line is monitored with the IncuCyte Zoom live cell imager. Proliferation is measured using CellTiterGlo reagent. Growth media is removed from the cell plates following compound treatment and 80 μL/well CellTiter Glo diluted 1:1 in PBS added. Luminescence is measured by an Plate Reader^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

Verweise

[1]. Quinlan CL, et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8503 mL	14.2515 mL	28.5030 mL	71.2576 mL
	5 mM	0.5701 mL	2.8503 mL	5.7006 mL	14.2515 mL
	10 mM	0.2850 mL	1.4252 mL	2.8503 mL	7.1258 mL
	15 mM	0.1900 mL	0.9501 mL	1.9002 mL	4.7505 mL
	20 mM	0.1425 mL	0.7126 mL	1.4252 mL	3.5629 mL
	25 mM	0.1140 mL	0.5701 mL	1.1401 mL	2.8503 mL

Keywords

PF-9366

18 Cited Publications

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PF-9366

Epigenetics Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-9366

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-9366

Epigenetics Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PF-9366

Biologische Aktivität

Chemical Information

Publications (18)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-9366 Related Classifications

HY-107778 Related Classifications