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Pifithrin-α hydrobromide

Catalog No. T2707 CAS 63208-82-2

Synonyms: Pifithrin hydrobromide, PFTα hydrobromide, PFTα, Pifithrin-α, Pifithrin-α (PFTα) HBr

Pifithrin-α is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Pifithrin-α hydrobromide, CAS 63208-82-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 180.00
50 mg	In stock	$ 293.00
100 mg	In stock	$ 438.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 100%

Purity: 98.54%

Purity: 97.71%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pifithrin-α is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.
Kinase Assay	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].
Cell Research	At the end of cell treatments, the number of attached cells is estimated by staining with 0.25% crystal violet in 50% methanol, followed by elution of the dye with 1% SDS. Optical density (530 nm) reflecting the number of stained cells is determined with a Bio-Tek EL311 microplate reader. Cell viability in suspension of short term culture of primary thymocytes is determined by their staining with 0.1% of methyl blue and microscopic counting of blue (dead) cells.(Only for Reference)

Synonyms	Pifithrin hydrobromide, PFTα hydrobromide, PFTα, Pifithrin-α, Pifithrin-α (PFTα) HBr
Molecular Weight	367.3
Formula	C16H18N2OS·HBr
CAS No.	63208-82-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 36.7 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Komarov PG, et al. Science, 1999, 285(5434), 1733-1737. 2. Culmsee C, et al. J Neurochem, 2001, 77(1), 220-228. 3. Komarova EA, et al. J Biol Chem, 2003, 278(18), 15465-15468. 4. Murphy PJ, et al. J Biol Chem, 2004, 279(29), 320195-3201201. 5. Leker RR, et al. Exp Neurol, 2004, 187(2), 478-486. 6. 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. 7. Kuang SQ, et al. FOXE3 mutations predispose to thoracic aortic aneurysms and dissections. J Clin Invest. 2016 Mar 1;126(3):948-61. 8. Lu L, Li K, Mao Y H, et al. Gold-chrysophanol nanoparticles suppress human prostate cancer progression through inactivating AKT expression and inducing apoptosis and ROS generation in vitro and in vivo[J]. International journal of oncology. 2017 Oct;51(4):1089-1103. 9. Zhou Y, Yang L, Xiong L, et al. KIF11 is upregulated in colorectal cancer and silencing of it impairs tumor growth and sensitizes colorectal cancer cells to oxaliplatin via p53/GSK3β signaling[J]. Journal of Cancer. 2021, 12(12): 3741.

Citations

1. Chen L, Zhang L, Jin G, et al.Synergy of 5-aminolevulinate supplement and CX3CR1 suppression promotes liver regeneration via elevated IGF-1 signaling.Cell Reports.2023, 42(8). 2. Lin X, Lin T, Wang X, et al.Sesamol serves as a p53 stabilizer to relieve rheumatoid arthritis progression and inhibits the growth of synovial organoids.Phytomedicine.2023: 155109. 3. Wu Y, Zhou T, Qian D, et al.Z-Guggulsterone Induces Cell Cycle Arrest and Apoptosis by Targeting the p53/CCNB1/PLK1 Pathway in Triple-Negative Breast Cancer.ACS Omega.2023 4. Hussain M, Lu Y, Tariq M, et al. A small-molecule Skp1 inhibitor elicits cell death by p53-dependent mechanism. Iscience. 2022, 25(7): 104591. 5. Yang R, Yang H, Wei J, et al. Mechanisms Underlying the Effects of Lianhua Qingwen on Sepsis-Induced Acute Lung Injury: A Network Pharmacology Approach. Frontiers in Pharmacology. 2021: 2839. 6. Wu X, Han C, Wang L, et al. Iron increases the susceptibility of colorectal cancer cells to compound Kushen Injection via the decrease of TOP2A and p53. Pharmacological Research-Modern Chinese Medicine. 2022, 2: 100058. 7. Luo Y, Gao X, Zou L, et al. Bavachin Induces Ferroptosis through the STAT3/P53/SLC7A11 Axis in Osteosarcoma Cells. Oxidative Medicine and Cellular Longevity. 2021 8. Guo Y, Li Q, Zhao G, et al. Loss of TRIM31 promotes breast cancer progression through regulating K48-and K63-linked ubiquitination of p53. Cell Death & Disease. 2021, 12(10): 1-13. 9. Shang Y, Zhang S, Cheng Y, et al. Tetrabromobisphenol a exacerbates the overall radioactive hazard to zebrafish (Danio rerio). Environmental Pollution. 2022: 120424. 10. Jiang W, Wang X, Su S, et al. Identifying the shared genes and KEGG pathways of Resolvin D1-targeted network and osteoarthritis using bioinformatics. Bioengineered. 2022, 13(4): 9839-9854

Related compound libraries

This product is contained In the following compound libraries：

PPI Inhibitor Library Cell Cycle Compound Library Apoptosis Compound Library Immunology/Inflammation Compound Library Target-Focused Phenotypic Screening Library Anti-Cancer Compound Library Anti-Colorectal Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Lung Cancer Compound Library Kinase Inhibitor Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pifithrin-α hydrobromide 63208-82-2 Apoptosis Immunology/Inflammation p53 Aryl Hydrocarbon Receptor Ferroptosis inhibit Pifithrin α hydrobromide Inhibitor MDM-2/p53 AhR Pifithrin Pifithrin hydrobromide PFTα hydrobromide PFTα Pifithrin-α Pifithrin-α (PFTα) HBr Pifithrinα hydrobromide inhibitor

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