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Pifithrin-β HBr (QB-102; Cyclic-Pifithrin-α), the hydrobromide salt of Pifithrin-β, is a potent p53 inhibitor (IC50 of 23 μM) and a cell-permeable Cyclized analog of Pifithrin-α with higher stability and reduced cytotoxicity. Neuroprotective properties of Pifithrin-β HBr.
Targets |
p53 (IC50 = 23 μM)
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ln Vitro |
Pifithrin-α hydrobromide (PFT β hydrobromide), an inhibitor of the p53 protein, is thought to be a promising drug candidate for the treatment of cancer and neurodegenerative diseases. The N-acetyl derivative of pifithrin, Pifithrin-α, is produced quickly from the extremely unstable precursor pifithrin-β, which is very unstable in culture medium[2]. The viability assay demonstrates, after 24 hours, that pretreatments with 1 and 10 μM pifithrin-β exert neuroprotective effects[3].
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Cell Assay |
For 24 hours, the H460 and IGROV-1 cell lines were subjected to either PFT or paclitaxel treatment alone or in combination. Following a PBS wash, the cells were fixed for 30 minutes in 2% paraformaldehyde before being permeabilized for 20 minutes at 20°C in ice-cold methanol. Anti-p53 antibody was incubated for 1 hour at room temperature after blocking with PBA (PBS containing 1% bovine serum albumin), and then for 1 hour with Alexa Fluor 488 goat antimouse IgG secondary antibody. Confocal microscopy was used to view and examine images.
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References |
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Molecular Formula |
C16H17BRN2S
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Molecular Weight |
349.29
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Exact Mass |
349.29
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Elemental Analysis |
C, 55.02; H, 4.91; Br, 22.88; N, 8.02; S, 9.18
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CAS # |
511296-88-1
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Related CAS # |
Pifithrin-β;60477-34-1
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Appearance |
Solid powder
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SMILES |
CC1=CC=C(C=C1)C2=CN3C4=C(CCCC4)SC3=N2.Br
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InChi Key |
SGNCOAOESGSEOP-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C16H16N2S.BrH/c1-11-6-8-12(9-7-11)13-10-18-14-4-2-3-5-15(14)19-16(18)17-13;/h6-10H,2-5H2,1H3;1H
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Chemical Name |
2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole;hydrobromide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8630 mL | 14.3148 mL | 28.6295 mL | |
5 mM | 0.5726 mL | 2.8630 mL | 5.7259 mL | |
10 mM | 0.2863 mL | 1.4315 mL | 2.8630 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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
NAC increased the level of p53 target gene transcription.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. th> |
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NAC treatment induced cell cycle arrest.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. td> |
NAC induced apoptotic cell death.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. td> |
Cytotoxic effects of the tested compounds and pifithrin-β at 1 (A) and 10 μM (B) on SH-SY5Y cells.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. th> |
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Neuroprotective effects of compounds4,12, and19.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. td> |
(A) Concentration–response curves of compound12and pifithrin-β.ACS Chem Neurosci. 2014 May 21; 5(5): 390– td> |