PF-429242
Based on 13 publication(s) in Google Scholar
PF429242 is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.59%
- No. CAS: 947303-87-9
- Fòrmula: C25H35N3O2
- Peso molecular:409.56
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-429242
More- Nature. 2023 Apr;616(7956):348-356. [Abstract]
- Immunity. 2018 Nov 20;49(5):842-856.e7. [Abstract]
- Autophagy. 2021 Jul;17(7):1592-1613. [Abstract]
- Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]
- Cell Death Dis. 2025 Jul 11;16(1):512. [Abstract]
- Hypertension. 2021 Feb;77(2):405-416. [Abstract]
- Sci China Life Sci. 2022 Feb;65(2):341-361. [Abstract]
- JCI Insight. 2019 Apr 4;4(7):e124174. [Abstract]
- iScience. 2026 Jun 4;29(6):116290. [Abstract]
- J Neurosci Res. 2025 Jun;103(6):e70054. [Abstract]
- Anal Cell Pathol. 2026;2026(1):e6120748. [Abstract]
- Blood Neoplasia. 2026 Aug 11.
- bioRxiv. 2026 Apr 7.
Customer Validation & Images
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Cell Imaging/Staining
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Histological Imaging/Staining
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Histological Imaging/Staining
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ELISA
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WB
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
170 nM
Compound: 1u, PF-429242
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Inhibition of human S1P expressed in CHOK1 cells
Inhibition of human S1P expressed in CHOK1 cells
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[PMID: 17583500] |
| Hepatocyte | EC50 |
0.3 μM
Compound: 1u, PF-429242
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Reduction of HMG-CoA synthase expression in mouse hepatocytes
Reduction of HMG-CoA synthase expression in mouse hepatocytes
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[PMID: 17583500] |
| Hepatocyte | EC50 |
2 μM
Compound: 1u, PF-429242
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Reduction of fatty acid synthase expression in mouse hepatocytes
Reduction of fatty acid synthase expression in mouse hepatocytes
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[PMID: 17583500] |
| HepG2 | EC50 |
600 nM
Compound: 1u, PF-429242
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Inhibition of cholesterol synthesis in HepG2 cells
Inhibition of cholesterol synthesis in HepG2 cells
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[PMID: 17583500] |
In Vitro
10 μM PF-429242 inhibits endogenous SREBP processing in Chinese hamster ovary cells. PF-429242 also down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In HepG2 cells, PF-429242 inhibits cholesterol synthesis, with an IC50 of 0.5 μM[1].
The addition of PF-429242 (30 μM) shows statistically significant suppression of infectious viral titers and viral RNA copies in the cell culture fluids. PF-429242 treatment also shows suppressive effects on DENV2 yields in the cultured fluids of human-derived HEK-293, Hep G2, and non-human-primate derived LLC-MK2 cells[2].
PF-429242 efficiently prevents the processing of GPC from the prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV, which correlates with the compound's potent antiviral activity against LCMV and LASV in cultured cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 947303-87-9
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Appearance Oil
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Peso molecular 409.56
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Fòrmula C25H35N3O2
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Color Colorless to light yellow
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SMILES
O=C(N(CCC1=CC=CC=C1OC)[C@H]2CNCC2)C3=CC=C(CN(CC)CC)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (13)
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Journal Impact Factor
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Most Recent
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Nature
2023 Apr;616(7956):348-356. PMID: 37020026 -
Immunity
Cholesterol Homeostatic Regulator SCAP-SREBP2 Integrates NLRP3 Inflammasome Activation and Cholesterol Biosynthetic Signaling in Macrophages. [Abstract]2018 Nov 20;49(5):842-856.e7. PMID: 30366764
PF-429242 purchased from MedChemExpress. Usage Cited in: Immunity. 2018 Nov 20;49(5):842-856.e7. [Abstract]
PF429242 dihydrochloride (50-200 μM; 1 h) greatly suppressed the NLRP3 inflammasome activity in LPS-primed BMDMs.
PF-429242 purchased from MedChemExpress. Usage Cited in: Immunity. 2018 Nov 20;49(5):842-856.e7. [Abstract]
PF429242 dihydrochloride (200 μM; 1 h) suppressed nigericin-induced SREBP2 maturation in LPS-primed THP1 macrophages.
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Autophagy
Discovery of a potent SCAP degrader that ameliorates HFD-induced obesity, hyperlipidemia and insulin resistance via an autophagy-independent lysosomal pathway. [Abstract]2021 Jul;17(7):1592-1613. PMID: 32432943 -
Cell Death Differ
2021 Jun;28(6):2001-2018. PMID: 33469231
PF-429242 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]
PF429242 dihydrochloride (5-10 μM) significantly inhibited osteoclasts formation in murine BMMs in a dose-dependent manner.
PF-429242 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]
PF429242 dihydrochloride (3 mg/kg; twice a week for 2 months) significantly increased the values of BV/TV and decreased Tb.Sp in OVX-induced osteoporosis mice.
PF-429242 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2021 Jun;28(6):2001-2018. [Abstract]
PF429242 dihydrochloride (3 mg/kg; every two days for 2 weeks) reduced osteolysis and osteoclast activity in LPS-induced calvarial osteolysis mice.
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Cell Death Dis
IFNγ augments TKI efficacy by alleviating protein unfolding stress to promote GSDME-mediated pyroptosis in hepatocellular carcinoma. [Abstract]2025 Jul 11;16(1):512. PMID: 40645933 -
Hypertension
Site-1 Protease-Derived Soluble (Pro)Renin Receptor Contributes to Angiotensin II-Induced Hypertension in Mice. [Abstract]2021 Feb;77(2):405-416. PMID: 33280408 -
Sci China Life Sci
2022 Feb;65(2):341-361. PMID: 34047913 -
JCI Insight
Site-1 protease-derived soluble (pro)renin receptor targets vasopressin receptor 2 to enhance urine concentrating capability. [Abstract]2019 Apr 4;4(7):e124174. PMID: 30944256 -
iScience
Regulation of the endoplasmic reticulum stress sensor ATF6α through multiple oxidoreductases in the ER. [Abstract]2026 Jun 4;29(6):116290. PMID: 42305590 -
J Neurosci Res
Astrocytic HSP60 Deletion Induced Astrocyte Senescence and Inhibited Neuroregeneration via Modulating the S1P/Truncated-BDNF Pathway. [Abstract]2025 Jun;103(6):e70054. PMID: 40448367 -
Anal Cell Pathol
Identification of the Antioxidant Enzyme B166 as a Novel Biomarker for Patients With Glioblastoma Multiforme. [Abstract]2026;2026(1):e6120748. PMID: 41810932 -
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Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (61.04 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. 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. 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.10 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.10 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Korean - KR (537 KB)
- Portuguese - PT (537 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol Exp Ther. 2008 Sep;326(3):801-8. [Content Brief]
[2]. Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. [Content Brief]
[3]. Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803. [Content Brief]
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. 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 | 2.4416 mL | 12.2082 mL | 24.4164 mL | 61.0411 mL |
| 5 mM | 0.4883 mL | 2.4416 mL | 4.8833 mL | 12.2082 mL | |
| 10 mM | 0.2442 mL | 1.2208 mL | 2.4416 mL | 6.1041 mL | |
| 15 mM | 0.1628 mL | 0.8139 mL | 1.6278 mL | 4.0694 mL | |
| 20 mM | 0.1221 mL | 0.6104 mL | 1.2208 mL | 3.0521 mL | |
| 25 mM | 0.0977 mL | 0.4883 mL | 0.9767 mL | 2.4416 mL | |
| 30 mM | 0.0814 mL | 0.4069 mL | 0.8139 mL | 2.0347 mL | |
| 40 mM | 0.0610 mL | 0.3052 mL | 0.6104 mL | 1.5260 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4883 mL | 1.2208 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4069 mL | 1.0174 mL |
PF-429242 Related Classifications
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