Pifithrin-α (PFTα) HBr

Alias: PFT-alpha; Pifithrin-alpha; PFTalpha; Pifithrin alpha; PFT alpha
Cat No.:V0014 Purity: ≥98%
Pifithrin-α HBr ((PFTα hydrobromide; PFT-α) is a novel and potent inhibitor of p53, acting by inhibiting p53 protein transcription and p53-dependent transactivation of p53-responsive genes.
Pifithrin-α (PFTα) HBr Chemical Structure CAS No.: 63208-82-2
Product category: p53
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Pifithrin-HBr (PFT hydrobromide; PFT-) is a brand-new and powerful p53 inhibitor that works by preventing the transcription of the p53 protein and the p53-dependent transactivation of p53-responsive genes. It also has aryl hydrocarbon receptor (AhR) agonist properties. First, it was discovered that pifithrin- inhibited p53-responsive lacZ activation in ConA cells and decreased the activation of endogenous cellular p53-responsive genes. Pifithrin- can also cause embryonic stem cells to experience cell cycle arrest and growth arrest. The protein lever of Nanog (a pluripotency marker) is significantly downregulated after treatment of Pifithrin-. It has been demonstrated that Pifithrin-induced p53 activity inhibition has no impact on the viability of ES cells.

Biological Activity I Assay Protocols (From Reference)
Targets
p53; AhR
ln Vitro
Pifithrin (PFT) hydrobromide is a water-soluble substance that has the potential to inhibit the transcription of the p53 protein. Pifithrin-α can prevent the p53 protein from increasing in whole cell lysates when glucose oxidase (GOX) is activated, but cyclosporine A (CsA) cannot. Notably, Pifithrin-α can prevent the reduction of Bcl-2 protein caused by GOX. In a similar vein, Pifithrin-α rather than CsA, is able to stop the Bax protein from growing in whole cell lysates[1]. Through an unknown mechanism, Pifithrin-α prevents p53-dependent apoptosis. Aryl hydrocarbon receptor (AhR) agonist activity is another function of Pifithrin-α. According to its capacity to bind the AhR, trigger the formation of its DNA binding complex, stimulate reporter activity, and up-regulate the traditional AhR target gene CYP1A1, Pifithrin-α is a potent AhR agonist.
ln Vivo
The experiment's percentage of annexin V-positive Foxe3-/- SMCs drops to WT levels when Pifthirin-α(PFT-α) hydrobromide, a pharmacological p53 inhibitor, is used. In Foxe3-/- mice, transverse aortic constriction (TAC) significantly lowers the incidence of aortic rupture and intramural hematomas (50% to 17%, P<0.05). The average diameter of the ascending aorta and the proportion of TUNEL-positive cells in the aortic media are also normalized to WT levels in surviving Foxe3-/- animals after Pifthirin-α treatment (P<0.05).[3].
Enzyme Assay
Assays for ligand binding competition are carried out. 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 is used to create cytosolic cell extracts from Hepa-1 cells. Aliquots of the supernatant (120 g) are incubated with the indicated concentrations of Pifithrin-α while being exposed to 3 nM [3H]TCDD in HEDG buffer for 2 hours at room temperature. HEDG buffer containing 0.5% Tween 80 is added after 30 minutes of hydroxyapatite incubation on ice. Scintillation counting is performed on the samples after they have been centrifuged, cleaned twice, and resuspended in 0.2 mL of scintillation fluid. A 150-fold molar excess of TCDF is used to calculate nonspecific binding, which is then subtracted from the total binding to get the specific binding. According to [3H]TCDD alone, the precise binding is reported[2].
Cell Assay
The human hepatoma cell lines HepG2 (p53++) are cultured in RMPI 1640 medium with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, and 37°C in a 5% CO2 environment. Cells are exposed to GOX (0–5 0U) for 0–8 hours either with or without Pifithrin-α (20 μM/L), Pifithrin-μ (5 μM/L), CsA (10μM/L), Sanglifehrin A (20μM/L), and NAC (5 mM/L), for an hour each. Cells are gathered and prepared for further experiments after treatment[1].
Animal Protocol
Mice: The Foxe3-null (Foxe3-/-) mice are employed. Pifithrin-α is dissolved in PBS one hour prior to TAC and then given every 48 hours in order to study the role of p53 in Foxe3-related apoptosis. Two weeks after the operation, the animals are put to sleep, and the ascending aortic tissues are collected for RNA, total protein, histomorphometric analysis, or TUNEL assay.
References

[1]. Int J Biol Sci. 2016 Jan 1;12(2):198-209.

[2]. J Pharmacol Exp Ther. 2005 Aug;314(2):603-10.

[3]. J Clin Invest. 2016 Mar 1;126(3):948-61.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H18N2OS.HBR
Molecular Weight
367.3
Exact Mass
366.0401
Elemental Analysis
C, 52.32; H, 5.21; Br, 21.75; N, 7.63; O, 4.36; S, 8.73
CAS #
63208-82-2
Appearance
Solid powder
SMILES
CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br
InChi Key
HAGVCKULCLQGRF-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H18N2OS.BrH/c1-11-6-8-12(9-7-11)14(19)10-18-13-4-2-3-5-15(13)20-16(18)17;/h6-9,17H,2-5,10H2,1H3;1H
Chemical Name
2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-methylphenyl)ethanone;hydrobromide
Synonyms
PFT-alpha; Pifithrin-alpha; PFTalpha; Pifithrin alpha; PFT alpha
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~67 mg/mL (~182.4 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: ~2 mg/mL (~6.1 mM)
Solubility (In Vivo)
30%Propylene glycol, 5%Tween 80, 65% D5W: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7226 mL 13.6129 mL 27.2257 mL
5 mM 0.5445 mL 2.7226 mL 5.4451 mL
10 mM 0.2723 mL 1.3613 mL 2.7226 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
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