Pifithrin-α hydrobromide
Based on 102 publication(s) in Google Scholar
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
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- Reinheit: 99.94%
- CAS. Nr.: 63208-82-2
- Formel: C16H19BrN2OS
- Molecular Weight:367.30
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Pifithrin-α hydrobromide
More- Signal Transduct Target Ther. 2025 May 9;10(1):150. [Abstract]
- Cell. 2026 Jun 11;189(12):3541-3552.e18. [Abstract]
- Mol Cancer. 2024 Oct 30;23(1):242. [Abstract]
- Adv Mater. 2025 Oct 17:e08245. [Abstract]
- ACS Nano. 2023 Nov 28;17(22):22901-22915. [Abstract]
- Nat Commun. 2026 Feb 13;17(1):2737. [Abstract]
- Nat Commun. 2024 Oct 4;15(1):8624. [Abstract]
- Adv Sci (Weinh). 2025 May 20:e2416489. [Abstract]
- Adv Sci (Weinh). 2024 Aug 9:e2402329. [Abstract]
- J Adv Res. 2025 Jan:67:217-229. [Abstract]
- Biomark Res. 2024 Jan 25;12(1):13. [Abstract]
- J Hazard Mater. 2021 Mar 15;406:124316. [Abstract]
- Environ Int. 2026 Apr:210:110254. [Abstract]
- Cell Death Dis. 2026 Jan 24;17(1):165. [Abstract]
- Cell Death Dis. 2022 Sep 6;13(9):770. [Abstract]
- Cell Death Dis. 2022 Apr 13;13(4):343. [Abstract]
- Cell Death Dis. 2020 Jan 22;11(1):44. [Abstract]
- Cell Death Dis. 2019 May; 10(5): 329. [Abstract]
- Dev Cell. 2025 Apr 21;60(8):1182-1198.e8. [Abstract]
- Phytomedicine. 2026 Mar:152:157865. [Abstract]
- Phytomedicine. 2025 Nov:147:157215. [Abstract]
- Phytomedicine. 2025 Jun 8:144:156958. [Abstract]
- EMBO J. 2022 Mar 15;41(6):e108946. [Abstract]
- Free Radic Biol Med. 2026 Mar 25:250:174-188. [Abstract]
- Apoptosis. 2022 Aug;27(7-8):545-560. [Abstract]
- Sci Total Environ. 2024 Dec 10:955:177073. [Abstract]
- Biomed Pharmacother. 2026 Feb:195:118974. [Abstract]
- Cell Death Discov. 2024 Oct 13;10(1):436. [Abstract]
- Cell Death Discov. 2023 Nov 14;9(1):414. [Abstract]
- Cell Rep. 2026 Mar 15;45(3):117084. [Abstract]
- Phytother Res. 2020 Dec;34(12):3298-3310. [Abstract]
- Cell Biosci. 2022 Feb 25;12(1):20. [Abstract]
- Ecotoxicol Environ Saf. 2026 Mar 1:312:119946. [Abstract]
- Biochem Pharmacol. 2025 Jan 31:116790. [Abstract]
- Biochem Pharmacol. 2018 Feb:148:64-74. [Abstract]
- J Ethnopharmacol. 2026 Aug 10:367:121659. [Abstract]
- J Ethnopharmacol. 2025 Aug 29:352:120227. [Abstract]
- J Ethnopharmacol. 2024 Aug 20:118721. [Abstract]
- Commun Biol. 2025 Dec 13. [Abstract]
- Commun Biol. 2025 Aug 23;8(1):1275. [Abstract]
- Mech Ageing Dev. 2019 Sep:182:111124. [Abstract]
- Inflammation. 2025 Jan 10. [Abstract]
- Eur J Pharmacol. 2025 Oct 10:1007:178233. [Abstract]
- Int Immunopharmacol. 2025 Sep 23:166:115554. [Abstract]
- Eur J Pharmacol. 2022 Jun 15;925:175002. [Abstract]
- Toxicology. 2024 Jan:501:153707. [Abstract]
- Toxicology. 2020 Dec 15;446:152611. [Abstract]
- Clin Epigenetics. 2024 Jul 23;16(1):97. [Abstract]
- Exp Gerontol. 2026 Jan:213:112994. [Abstract]
- J Cell Mol Med. 2020 Mar;24(6):3611-3624. [Abstract]
- J Cell Mol Med. 2019 May;23(5):3538-3548. [Abstract]
- Mol Nutr Food Res. 2018 Aug;62(16):e1800164. [Abstract]
- J Funct Foods. 2026 Jan 31.
- J Cell Physiol. 2021 Nov;236(11):7356-7375. [Abstract]
- Fish Shellfish Immunol. 2022 Jan:120:648-657. [Abstract]
- Oncol Rep. 2019 Jun;41(6):3475-3487. [Abstract]
- Microbiol Spectr. 2022 Apr 27;10(2):e0272721. [Abstract]
- Mol Cell Biochem. 2025 Jul;480(7):4483-4497. [Abstract]
- Cell Signal. 2020 Feb;66:109445. [Abstract]
- Biochim Biophys Acta Mol Cell Res. 2019 Aug;1866(8):1272-1281. [Abstract]
- Biochim Biophys Acta. 2018 Apr 26;1865(8):1034-1045. [Abstract]
- Development. 2022 Jul 1;149(13):dev200205. [Abstract]
- Food Chem Toxicol. 2025 Jun 4:203:115592. [Abstract]
- Food Chem Toxicol. 2023 Jan:171:113531. [Abstract]
- Exp Cell Res. 2021 Oct 1;407(1):112799. [Abstract]
- BMC Cancer. 2024 Jun 14;24(1):729. [Abstract]
- J Immunol. 2024 Jun 15;212(12):1932-1944. [Abstract]
- BMC Cancer. 2024 Jan 2;24(1):25. [Abstract]
- Eur J Med Res. 2023 Nov 8;28(1):503. [Abstract]
- Stem Cells Int. 2021 Dec 24:2021:4968649. [Abstract]
- Mol Carcinog. 2023 Apr;62(4):464-478. [Abstract]
- Front Biosci (Landmark Ed). 2025 Dec 18;30(12):45389. [Abstract]
- Arch Biochem Biophys. 2024 Mar:753:109905. [Abstract]
- Toxicol Lett. 2020 Jun 15;326:114-122. [Abstract]
- Am J Cancer Res. 2018 Sep 1;8(9):1697-1711. [Abstract]
- Mol Biol Rep. 2025 Jun 24;52(1):633. [Abstract]
- J Cancer Res Clin Oncol. 2024 Oct 16;150(10):463. [Abstract]
- Front Genet. 2018 Aug 31:9:320. [Abstract]
- J Cell Biochem. 2018 May;119(5):4009-4020. [Abstract]
- Toxicol In Vitro. 2020 Dec;69:104971. [Abstract]
- Clin Transl Oncol. 2025 Dec 19. [Abstract]
- Am J Reprod Immunol. 2025 Oct;94(4):e70163. [Abstract]
- Biochem Biophys Res Commun. 2025 Nov 1:787:152767. [Abstract]
- J Fish Dis. 2019 Apr;42(4):585-595. [Abstract]
- Cancer Biother Radiopharm. 2025 Aug 8. [Abstract]
- Neurosci Lett. 2023 Mar 13:800:137125. [Abstract]
- Biomed Chromatogr. 2026 Jun;40(6):e70452. [Abstract]
- Neuroreport. 2022 Jul 6;33(10):437-444. [Abstract]
- J Obstet Gynaecol Res. 2023 Aug;49(8):2126-2134. [Abstract]
- bioRxiv. 2026 Apr 7:2026.04.04.716514. [Abstract]
- SSRN. 2025 Nov 6.
- Res Sq. 2025 Aug 08.
- Res Sq. 2025 May 13.
- Res Sq. 2024 Nov 19.
- Res Sq. 2024 Aug 14:rs.3.rs-4603170. [Abstract]
- Research Square Preprint. 2024 Mar 28.
- Research Square Preprint. 2023 Sep 21.
- Research Square Print. 2023 Feb 14.
- Oxid Med Cell Longev. 2022 Oct 4:2022:2353115. [Abstract]
- Research Square Preprint. 2021 Aug.
- bioRxiv. 2020 Jun.
- Patent. US20180263995A1.
Customer Validation & Images
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Biologische Aktivität
Pifithrin-α (PFT-α) hydrobromideis a water-soluble compound that could suppress p53 protein transcription. Pifithrin-α can suppress glucose oxidase (GOX)-induced p53 protein increase in whole cell lysates, but cyclosporine A (CsA) fails to show such an inhibition effect. Notably, Pifithrin-α is able to block the GOX-induced Bcl-2 protein reduction. Similarly, it is Pifithrin-α rather than CsA that able to prevent the Bax increasing in whole cell lysates[1]. Pifithrin-α inhibits p53-dependent apoptosis through an undetermined mechanism. Pifithrin-α also acts as an aryl hydrocarbon receptor (AhR) agonist and. Pifithrin-α is a potent AhR agonist as determined by its ability to bind the AhR, induce formation of its DNA binding complex, activate reporter activity, and up-regulate the classic AhR target gene CYP1A1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 63208-82-2
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Appearance Solid
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Molecular Weight 367.30
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Formel C16H19BrN2OS
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Color White to light yellow
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SMILES
N=C1SC2=C(CCCC2)N1CC(C3=CC=C(C)C=C3)=O.[H]Br
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Synonyms
Pifithrin hydrobromide; PFTα hydrobromide
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Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (102)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Myeloid but not hepatocytic CD38 is a key driver for hepatic ischemia/reperfusion injury. [Abstract]2025 May 9;10(1):150. PMID: 40341132 -
Cell
2026 Jun 11;189(12):3541-3552.e18. PMID: 41999746 -
Mol Cancer
Tumour-intrinsic PDL1 signals regulate the Chk2 DNA damage response in cancer cells and mediate resistance to Chk1 inhibitors. [Abstract]2024 Oct 30;23(1):242. PMID: 39478560 -
Adv Mater
Ultrasound-Activated Sonophage Synergizes Sonodynamic Therapy and Saltoptosis for Solid Tumor Eradication. [Abstract]2025 Oct 17:e08245. PMID: 41104711 -
ACS Nano
MicroRNA-200 Loaded Lipid Nanoparticles Promote Intestinal Epithelium Regeneration in Canonical MicroRNA-Deficient Mice. [Abstract]2023 Nov 28;17(22):22901-22915. PMID: 37939210 -
Nat Commun
Engineered exosome nanovesicles for delivery of antibodies to treat inflammatory bowel disease. [Abstract]2026 Feb 13;17(1):2737. PMID: 41688436 -
Nat Commun
MDM2 induces pro-inflammatory and glycolytic responses in M1 macrophages by integrating iNOS-nitric oxide and HIF-1α pathways in mice. [Abstract]2024 Oct 4;15(1):8624. PMID: 39366973 -
Adv Sci (Weinh)
2025 May 20:e2416489. PMID: 40390546 -
Adv Sci (Weinh)
CircUGP2 Suppresses Intrahepatic Cholangiocarcinoma Progression via p53 Signaling Through Interacting With PURB to Regulate ADGRB1 Transcription and Sponging miR-3191-5p. [Abstract]2024 Aug 9:e2402329. PMID: 39120980 -
J Adv Res
HSPA12A acts as a scaffolding protein to inhibit cardiac fibroblast activation and cardiac fibrosis. [Abstract]2025 Jan:67:217-229. PMID: 38219869 -
Biomark Res
Simultaneous inhibition of FAK and ROS1 synergistically repressed triple-negative breast cancer by upregulating p53 signalling. [Abstract]2024 Jan 25;12(1):13. PMID: 38273343 -
J Hazard Mater
Multiple transcriptomic profiling: p53 signaling pathway is involved in DEHP-induced prepubertal testicular injury via promoting cell apoptosis and inhibiting cell proliferation of Leydig cells. [Abstract]2021 Mar 15;406:124316. PMID: 33162236 -
Environ Int
From phthalate exposure to venous thrombotic risk: Decoding the DEHP-ROS mediated OTUD1- p53 stabilization loop in endothelium. [Abstract]2026 Apr:210:110254. PMID: 41967174 -
Cell Death Dis
2026 Jan 24;17(1):165. PMID: 41580425 -
Cell Death Dis
Histone methyltransferase MLL1 drives renal tubular cell apoptosis by p53-dependent repression of E-cadherin during cisplatin-induced acute kidney injury. [Abstract]2022 Sep 6;13(9):770. PMID: 36068197 -
Cell Death Dis
Downregulation of REST in the cochlea contributes to age-related hearing loss via the p53 apoptosis pathway. [Abstract]2022 Apr 13;13(4):343. PMID: 35418568 -
Cell Death Dis
TNAP inhibition attenuates cardiac fibrosis induced by myocardial infarction through deactivating TGF-β1/Smads and activating P53 signaling pathways. [Abstract]2020 Jan 22;11(1):44. PMID: 31969558 -
Cell Death Dis
S-nitrosylation of the Peroxiredoxin-2 promotes S-nitrosoglutathione-mediated lung cancer cells apoptosis via AMPK-SIRT1 pathway. [Abstract]2019 May; 10(5): 329. PMID: 30988280 -
Dev Cell
2025 Apr 21;60(8):1182-1198.e8. PMID: 39765233 -
Phytomedicine
Tripterygium glycosides reverse cisplatin resistance in epithelial ovarian cancer by activating ferroptosis via two different pathways. [Abstract]2026 Mar:152:157865. PMID: 41619560 -
Phytomedicine
Dendrobin A inhibits gastric cancer: Mechanistic insights supported by integrated evidence. [Abstract]2025 Nov:147:157215. PMID: 40913985 -
Phytomedicine
Targeting tumor metabolism: The dual attack of emodin on glycolysis and oxidative phosphorylation in esophageal squamous cell carcinoma. [Abstract]2025 Jun 8:144:156958. PMID: 40513325 -
EMBO J
Pharmacological CDK4/6 inhibition reveals a p53-dependent senescent state with restricted toxicity. [Abstract]2022 Mar 15;41(6):e108946. PMID: 34985783 -
Free Radic Biol Med
Hypothermic machine perfusion attenuates DCD liver ischemia reperfusion injury via the YAP1/P53-mediated micromitophagy pathway. [Abstract]2026 Mar 25:250:174-188. PMID: 41895416 -
Apoptosis
ML323, a USP1 inhibitor triggers cell cycle arrest, apoptosis and autophagy in esophageal squamous cell carcinoma cells. [Abstract]2022 Aug;27(7-8):545-560. PMID: 35654870 -
Sci Total Environ
Naringin alleviates fluoride-induced neurological impairment: A focus on the regulation of energy metabolism mediated by mitochondrial permeability transition pore. [Abstract]2024 Dec 10:955:177073. PMID: 39447898 -
Biomed Pharmacother
Dihydroartemisinin enhances NKG2D CAR-T cell therapy against solid tumors by inducing NKG2D ligands and remodeling the tumor microenvironment. [Abstract]2026 Feb:195:118974. PMID: 41529511 -
Cell Death Discov
2024 Oct 13;10(1):436. PMID: 39397009 -
Cell Death Discov
LASS2 enhances p53 protein stability and nuclear import to suppress liver cancer progression through interaction with MDM2/MDMX. [Abstract]2023 Nov 14;9(1):414. PMID: 37963859 -
Cell Rep
Loss of p53 exacerbates autoimmunity by reprogramming propionyl-CoA metabolism and histone modifications in Treg cells. [Abstract]2026 Mar 15;45(3):117084. PMID: 41838722 -
Phytother Res
Triptolide enhances lipolysis of adipocytes by enhancing ATGL transcription via upregulation of p53. [Abstract]2020 Dec;34(12):3298-3310. PMID: 32614500 -
Cell Biosci
2022 Feb 25;12(1):20. PMID: 35216629 -
Ecotoxicol Environ Saf
Integrative network toxicology and single-cell transcriptomics reveal TP53 as a key mediator of PCBs-induced microglial dysfunction in diabetic retinopathy. [Abstract]2026 Mar 1:312:119946. PMID: 41740555 -
Biochem Pharmacol
WWOX-mediated p53/SAT1 and NRF2/FPN1 axis contribute to toosendanin-induced ferroptosis in hepatocellular carcinoma. [Abstract]2025 Jan 31:116790. PMID: 39894307 -
Biochem Pharmacol
Ginsenoside Rh4 induces apoptosis and autophagic cell death through activation of the ROS/JNK/p53 pathway in colorectal cancer cells. [Abstract]2018 Feb:148:64-74. PMID: 29225132 -
J Ethnopharmacol
Xin Jia congrong tusizi decoction reverses ferroptosis in granulosa cells to rescue ovarian function decline via p53/Nrf2/SLC7A11/GPX4 signaling pathway. [Abstract]2026 Aug 10:367:121659. PMID: 42000005 -
J Ethnopharmacol
Erchen decoction alleviates silicosis by attenuating ferroptosis and fibrosis in alveolar macrophages via modulating the P53/HMOX1 pathway. [Abstract]2025 Aug 29:352:120227. PMID: 40617365 -
J Ethnopharmacol
Naoxintong capsule accelerates mitophagy in cerebral ischemia-reperfusion injury via TP53/PINK1/PRKN pathway based on network pharmacology analysis and experimental validation. [Abstract]2024 Aug 20:118721. PMID: 39173723 -
Commun Biol
P38α MAPK-induced senescence in cranial suture progenitor cells promotes craniosynostosis. [Abstract]2025 Dec 13. PMID: 41390905 -
Commun Biol
NAD+-dependent Sirt6 is a key regulator involved in telomere shortening of in vitro-cultured preimplantation embryos. [Abstract]2025 Aug 23;8(1):1275. PMID: 40849514 -
Mech Ageing Dev
The synergistic action of phosphate and interleukin-6 enhances senescence-associated calcification in vascular smooth muscle cells depending on p53. [Abstract]2019 Sep:182:111124. PMID: 31376399 -
Inflammation
Dnmt3a-mediated DNA Methylation Regulates P. gingivalis-suppressed Cementoblast Mineralization Partially Via Mitochondria-dependent Apoptosis Pathway. [Abstract]2025 Jan 10. PMID: 39789287 -
Eur J Pharmacol
Exendin-4 improves mitochondrial integrity against cisplatin-induced cardiac damage: Targeting p53 and NF-κB pathways. [Abstract]2025 Oct 10:1007:178233. PMID: 41075914 -
Int Immunopharmacol
Six1 promotes alveolar epithelium senescence in pulmonary fibrosis through regulating Tp53. [Abstract]2025 Sep 23:166:115554. PMID: 40991995 -
Eur J Pharmacol
Sampsonione F suppresses adipogenesis via activating p53 pathway during the mitotic clonal expansion progression of adipocyte differentiation. [Abstract]2022 Jun 15;925:175002. PMID: 35526567 -
Toxicology
DON induced DNA damage triggers absence of p53-mediated G2 arrest and apoptosis in IPEC-1 cells. [Abstract]2024 Jan:501:153707. PMID: 38104654 -
Toxicology
Cadmium induces apoptosis via generating reactive oxygen species to activate mitochondrial p53 pathway in primary rat osteoblasts. [Abstract]2020 Dec 15;446:152611. PMID: 33031904 -
Clin Epigenetics
DNA methylation-mediated suppression of TUSC1 expression regulates the malignant progression of esophagogastric junction cancer. [Abstract]2024 Jul 23;16(1):97. PMID: 39044262 -
Exp Gerontol
Hepcidin inhibits osteoclast differentiation to alleviate osteoporosis by modulating the p53/miR-34a/Trem2 axis. [Abstract]2026 Jan:213:112994. PMID: 41386388 -
J Cell Mol Med
P53/PANK1/miR-107 signalling pathway spans the gap between metabolic reprogramming and insulin resistance induced by high-fat diet. [Abstract]2020 Mar;24(6):3611-3624. PMID: 32048816 -
J Cell Mol Med
Inhibition of P53/miR-34a improves diabetic endothelial dysfunction via activation of SIRT1. [Abstract]2019 May;23(5):3538-3548. PMID: 30793480 -
Mol Nutr Food Res
Frataxin-Mediated PINK1-Parkin-Dependent Mitophagy in Hepatic Steatosis: The Protective Effects of Quercetin. [Abstract]2018 Aug;62(16):e1800164. PMID: 29935106
Pifithrin-α hydrobromide purchased from MedChemExpress. Usage Cited in: Mol Nutr Food Res. 2018 Aug;62(16):e1800164. [Abstract]
PFT-α, a pharmacological p53 inhibitor, inhibits the expression of frataxin in HepG2 cells. Under the treatment of free fatty acids (FFAs), the frataxin are further decreased by PFT-α.
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J Cell Physiol
NOXA-mediated degradation of MCL1 and BCL2L1 causes apoptosis of daunorubicin-treated human acute myeloid leukemia cells. [Abstract]2021 Nov;236(11):7356-7375. PMID: 33982799 -
Fish Shellfish Immunol
PI3K/AKT/p53 pathway inhibits infectious spleen and kidney necrosis virus infection by regulating autophagy and immune responses. [Abstract]2022 Jan:120:648-657. PMID: 34968710 -
Oncol Rep
JS‑K induces G2/M phase cell cycle arrest and apoptosis in A549 and H460 cells via the p53/p21WAF1/CIP1 and p27KIP1 pathways. [Abstract]2019 Jun;41(6):3475-3487. PMID: 31002373 -
Microbiol Spectr
Mandarin Fish (Siniperca chuatsi) p53 Regulates Glutaminolysis Induced by Virus via the p53/miR145-5p/c-Myc Pathway in Chinese Perch Brain Cells. [Abstract]2022 Apr 27;10(2):e0272721. PMID: 35286150 -
Mol Cell Biochem
TOR1 AIP1 interacts with p53 to enhance cell cycle dysregulation in prostate cancer progression. [Abstract]2025 Jul;480(7):4483-4497. PMID: 40198519 -
Cell Signal
Interleukin-10 induces senescence of activated hepatic stellate cells via STAT3-p53 pathway to attenuate liver fibrosis. [Abstract]2020 Feb;66:109445. PMID: 31730896 -
Biochim Biophys Acta Mol Cell Res
2019 Aug;1866(8):1272-1281. PMID: 30959066 -
Biochim Biophys Acta
2018 Apr 26;1865(8):1034-1045. PMID: 29704532 -
Development
2022 Jul 1;149(13):dev200205. PMID: 35698877 -
Food Chem Toxicol
Mechanisms of aristolochic acid I Hepatotoxicity: Central role of PDK4-Induced mitochondrial dysfunction and hepatic inflammation. [Abstract]2025 Jun 4:203:115592. PMID: 40480416 -
Food Chem Toxicol
DON entry into the nucleus induces DNA damage, apoptosis and cycle arrest in GES-1 cells. [Abstract]2023 Jan:171:113531. PMID: 36427601 -
Exp Cell Res
GRIM-19 inhibits proliferation and induces apoptosis in a p53-dependent manner in colorectal cancer cells through the SIRT7/PCAF/MDM2 axis. [Abstract]2021 Oct 1;407(1):112799. PMID: 34461110 -
BMC Cancer
CSPG4P12 polymorphism served as a susceptibility marker for esophageal cancer in Chinese population. [Abstract]2024 Jun 14;24(1):729. PMID: 38877481 -
J Immunol
IRF7 Exacerbates Candida albicans Infection by Compromising CD209-Mediated Phagocytosis and Autophagy-Mediated Killing in Macrophages. [Abstract]2024 Jun 15;212(12):1932-1944. PMID: 38709167 -
BMC Cancer
2024 Jan 2;24(1):25. PMID: 38166895 -
Eur J Med Res
Activation of the p53 signaling pathway by piRNA-MW557525 overexpression induces a G0/G1 phase arrest thus inhibiting neuroblastoma growth. [Abstract]2023 Nov 8;28(1):503. PMID: 37941038 -
Stem Cells Int
p57 Suppresses the Pluripotency and Proliferation of Mouse Embryonic Stem Cells by Positively Regulating p53 Activation. [Abstract]2021 Dec 24:2021:4968649. PMID: 34976070 -
Mol Carcinog
RBM4 inhibits the growth of clear cell renal cell carcinoma by enhancing the stability of p53 mRNA. [Abstract]2023 Apr;62(4):464-478. PMID: 36585906 -
Front Biosci (Landmark Ed)
SB431542, a Selective Inhibitor of the TGF-β Type I Receptor, Enhances Doxorubicin Antitumor Activity via p63 Activation in Mutant p53 Breast Cancer Cells. [Abstract]2025 Dec 18;30(12):45389. PMID: 41504053 -
Arch Biochem Biophys
Collagen I protects human keratinocytes HaCaT against UVB injury via restoring PINK1/parkin-mediated mitophagy. [Abstract]2024 Mar:753:109905. PMID: 38281543 -
Toxicol Lett
Downregulation of vdac2 inhibits spermatogenesis via JNK and P53 signalling in mice exposed to cadmium. [Abstract]2020 Jun 15;326:114-122. PMID: 32199951 -
Am J Cancer Res
Anti-malarial atovaquone exhibits anti-tumor effects by inducing DNA damage in hepatocellular carcinoma. [Abstract]2018 Sep 1;8(9):1697-1711. PMID: 30323964
Pifithrin-α hydrobromide purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2018 Sep 1;8(9):1697-1711. [Abstract]
Pifithrin-α hydrobromide (PFT) treatment inhibits Atovaquone (ATO)-induced upregulation of p53, p21, and cleavage of PARP, as well as downregulation of CDK2.
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Mol Biol Rep
UBE3C promotes pancreatic ductal adenocarcinoma progression by catalysing p53 ubiquitination. [Abstract]2025 Jun 24;52(1):633. PMID: 40553397 -
J Cancer Res Clin Oncol
AR expression-independent XRCC3 mediates DNA damage-induced p53/Bax signaling pathway activation against prostate cancer. [Abstract]2024 Oct 16;150(10):463. PMID: 39414634 -
Front Genet
Bioinformatics Analysis Identifies p53 as a Candidate Prognostic Biomarker for Neuropathic Pain. [Abstract]2018 Aug 31:9:320. PMID: 30233637
Pifithrin-α hydrobromide purchased from MedChemExpress. Usage Cited in: Front Genet. 2018 Aug 31:9:320. [Abstract]
Western blot analysis of the expression of p53 and caspase-3 after intrathecal administration of Pifithrin-α on day 7 after chronic constriction injury (CCI). The fold change of p53 and caspase-3 levels is normalized to the glyceraldehyde 3-phosphate dehydrogenase (GAPDH) level.
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J Cell Biochem
Halofuginone-induced autophagy suppresses the migration and invasion of MCF-7 cells via regulation of STMN1 and p53. [Abstract]2018 May;119(5):4009-4020. PMID: 29231257 -
Toxicol In Vitro
YAN, a novel microtubule inhibitor, inhibits P-gp and MRP1 function and induces mitotic slippage followed by apoptosis in multidrug-resistant A549/Taxol cells. [Abstract]2020 Dec;69:104971. PMID: 32805372 -
Clin Transl Oncol
Silencing of MAT2A inhibits gastric cancer cell proliferation, migration, and invasion through activation of the p53 pathway. [Abstract]2025 Dec 19. PMID: 41419675 -
Am J Reprod Immunol
The Role of Cryptotanshinone Regulates HTR-8/SVneo Cells Activity Through the p53/STAT3 Pathway in Unexplained Recurrent Spontaneous Abortion. [Abstract]2025 Oct;94(4):e70163. PMID: 41020636 -
Biochem Biophys Res Commun
Macrophage Mertk mediates pressure overload-induced heart failure via type I interferon response. [Abstract]2025 Nov 1:787:152767. PMID: 41076977 -
J Fish Dis
Comparative transcriptome analysis reveals the role of p53 signalling pathway during red-spotted grouper nervous necrosis virus infection in Lateolabrax japonicus brain cells. [Abstract]2019 Apr;42(4):585-595. PMID: 30659619 -
Cancer Biother Radiopharm
Targeting the MCM10/p53/p21/CCND1 Axis in Colorectal Cancer: Evaluating the Therapeutic Potential of Ultrasound. [Abstract]2025 Aug 8. PMID: 40779443 -
Neurosci Lett
2023 Mar 13:800:137125. PMID: 36780942
Pifithrin-α hydrobromide purchased from MedChemExpress. Usage Cited in: Neurosci Lett. 2023 Mar 13:800:137125. [Abstract]
Pifithrin-α hydrobromide (PFT-α; 0.5 μM; 0, 24, 48 h) reverses the inhibition of NSC cell proliferation (SV2A knockdown promotes NSCs apoptosis) (fig C) and reduces cleaved caspase 3 (CC3) expression (fig D) induced by SV2A knockdown.
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Biomed Chromatogr
Haizao Yuhu Decoction Inhibits Goiter via p53 Pathway-Induced Apoptosis: Metabolomic and Cellular Assay Analysis. [Abstract]2026 Jun;40(6):e70452. PMID: 42025629 -
Neuroreport
Duloxetine alleviates oxaliplatin-induced peripheral neuropathy by regulating p53-mediated apoptosis. [Abstract]2022 Jul 6;33(10):437-444. PMID: 35623085 -
J Obstet Gynaecol Res
Rosline promotes p21 expression to inhibit ovarian cancer cell proliferation via p53-independent pathway. [Abstract]2023 Aug;49(8):2126-2134. PMID: 37317483 -
bioRxiv
2026 Apr 7:2026.04.04.716514. PMID: 41993559 -
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Res Sq
SET8 inhibition preserves PTEN to attenuate kidney cell apoptosis in cisplatin nephrotoxicity. [Abstract]2024 Aug 14:rs.3.rs-4603170. PMID: 39184108 -
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Oxid Med Cell Longev
Energy-Stress-Mediated AMPK Activation Promotes GPX4-Dependent Ferroptosis through the JAK2/STAT3/P53 Axis in Renal Cancer. [Abstract]2022 Oct 4:2022:2353115. PMID: 36246395 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (136.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.81 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 (6.81 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protokoll
The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25 mM Hepes, 1 mM EDTA, 1 mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4 mM leupeptin, 4 mg/mL aprotinin, and 0.3 mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120 μg) are incubated at room temperature for 2 h with the indicated concentrations of Pifithrin-α in the presence of 3 nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice, resuspended in 0.2 mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The human hepatoma cell lines HepG2 (p53++) are cultured in RMPI 1640 medium with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin at 37°C in an atmosphere containing 5% CO2. Cells are exposed to GOX (0-5 0U) for 0-8 hours with or without Pifithrin-α (20 μM/L), Pifithrin-μ (5 μM/L), CsA (10 μM/L), Sanglifehrin A (20 μM/L) and NAC (5 mM/L) for 1 hour, respectively. After treatment, cells are collected and processed for further experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[3]
The Foxe3-null (Foxe3-/-) mice are used. To investigate the role of p53 in Foxe3-related apoptosis, Pifithrin-α is administered by i.p. injection at a dosage of 2.2 mg/kg, then dissolved in PBS 1 hour before TAC and then every 48 hours. Animals are euthanized 2 weeks after the surgery, and the ascending aortic tissues are harvested for either RNA, total protein, histomorphometric analysis, or TUNEL assay.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (285 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)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Yu W, et al. Cyclosporine A Suppressed Glucose Oxidase Induced P53 Mitochondrial Translocation and Hepatic Cell Apoptosis through Blocking Mitochondrial Permeability Transition. Int J Biol Sci. 2016 Jan 1;12(2):198-209. [Content Brief]
[2]. Hoagland MS, et al. The p53 Inhibitor Pifithrin-α Is a Potent Agonist of the Aryl Hydrocarbon Receptor. J Pharmacol Exp Ther. 2005 Aug;314(2):603-10. [Content Brief]
[3]. Kuang SQ, et al. FOXE3 mutations predispose to thoracic aortic aneurysms and dissections. J Clin Invest. 2016 Mar 1;126(3):948-61. [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 (sealed storage, away from moisture). 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 | 2.7225 mL | 13.6127 mL | 27.2254 mL | 68.0635 mL |
| 5 mM | 0.5445 mL | 2.7225 mL | 5.4451 mL | 13.6127 mL | |
| 10 mM | 0.2723 mL | 1.3613 mL | 2.7225 mL | 6.8064 mL | |
| 15 mM | 0.1815 mL | 0.9075 mL | 1.8150 mL | 4.5376 mL | |
| 20 mM | 0.1361 mL | 0.6806 mL | 1.3613 mL | 3.4032 mL | |
| 25 mM | 0.1089 mL | 0.5445 mL | 1.0890 mL | 2.7225 mL | |
| 30 mM | 0.0908 mL | 0.4538 mL | 0.9075 mL | 2.2688 mL | |
| 40 mM | 0.0681 mL | 0.3403 mL | 0.6806 mL | 1.7016 mL | |
| 50 mM | 0.0545 mL | 0.2723 mL | 0.5445 mL | 1.3613 mL | |
| 60 mM | 0.0454 mL | 0.2269 mL | 0.4538 mL | 1.1344 mL | |
| 80 mM | 0.0340 mL | 0.1702 mL | 0.3403 mL | 0.8508 mL | |
| 100 mM | 0.0272 mL | 0.1361 mL | 0.2723 mL | 0.6806 mL |
Pifithrin-α hydrobromide Related Classifications
HY-15484 Related Classifications
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