Pifithrin-β HBr (QB102; Cyclic Pifithrin-α)

Alias: Pifithrin-β HBr; Pifithrin-beta HBr; PFTβ HBr; PFT-β HBr; QB102 HBr; QB 102; QB-102; Cyclic-Pifithrin-α
Cat No.:V0092 Purity: ≥98%
Pifithrin-βHBr (QB-102; Cyclic-Pifithrin-α), the hydrobromide salt ofPifithrin-β, is a potentp53inhibitor (IC50of 23 μM) andacell-permeable Cyclized analog of Pifithrin-α with higher stability and reduced cytotoxicity.
Pifithrin-β HBr (QB102; Cyclic Pifithrin-α) Chemical Structure CAS No.: 511296-88-1
Product category: p53
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Pifithrin-β HBr (QB102; Cyclic Pifithrin-α):

  • Pifithrin-β (QB-102 and Cyclic-Pifithrin-α)
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Top Publications Citing lnvivochem Products
Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
p53 (IC50 = 23 μM)
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].
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.
References

[1]. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg Med Chem. 2011 Mar 1;19(5):1649-57.

[2]. Biological and chemical studies on aryl hydrocarbon receptor induction by the p53 inhibitor pifithrin-α and its condensation productpifithrin-β. Life Sci. 2011 Apr 25;88(17-18):774-83.

[3]. p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. ACS Chem Neurosci. 2014 May 21;5(5):390-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H17BRN2S
Molecular Weight
349.29
Exact Mass
349.29
Elemental Analysis
C, 55.02; H, 4.91; Br, 22.88; N, 8.02; S, 9.18
CAS #
511296-88-1
Appearance
Solid powder
SMILES
CC1=CC=C(C=C1)C2=CN3C4=C(CCCC4)SC3=N2.Br
InChi Key
SGNCOAOESGSEOP-UHFFFAOYSA-N
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
Chemical Name
2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole;hydrobromide
Synonyms
Pifithrin-β HBr; Pifithrin-beta HBr; PFTβ HBr; PFT-β HBr; QB102 HBr; QB 102; QB-102; Cyclic-Pifithrin-α
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: >10 mM
Water: N/A
Ethanol: N/A
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.

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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.
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Biological Data
  • Pifithrin-β HBr


    NAC increased the level of p53 target gene transcription.. 2014 May 21; 5(5): 390–399.

  • Pifithrin-β HBr


    NAC treatment induced cell cycle arrest.. 2014 May 21; 5(5): 390–399.

  • Pifithrin-β HBr


    NAC induced apoptotic cell death.. 2014 May 21; 5(5): 390–399.

  • Pifithrin-β HBr


    Cytotoxic effects of the tested compounds and pifithrin-β at 1 (A) and 10 μM (B) on SH-SY5Y cells.. 2014 May 21; 5(5): 390–399.

  • Pifithrin-β HBr


    Neuroprotective effects of compounds4,12, and19.. 2014 May 21; 5(5): 390–399.

  • Pifithrin-β HBr


    (A) Concentration–response curves of compound12and pifithrin-β.. 2014 May 21; 5(5): 390–

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