Pifithrin-β (QB-102 and Cyclic-Pifithrin-α)

Alias: Pifithrin-β; PFTβ; Pifithrin-beta; QB102; QB 102; QB-102; PFT-β; Cyclic-Pifithrin-α
Cat No.:V0091 Purity: ≥98%
Pifithrin-β (also known as QB102 and Cyclic-Pifithrin-α) is anovel and potentp53inhibitor with anIC50of 23 μM.
Pifithrin-β (QB-102 and Cyclic-Pifithrin-α) Chemical Structure CAS No.: 60477-34-1
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 (QB-102 and Cyclic-Pifithrin-α):

  • Pifithrin-β HBr (QB102; Cyclic Pifithrin-α)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Pifithrin-β (also known as QB102 and Cyclic-Pifithrin-α) is a novel and potent p53 inhibitor with an IC50 of 23 μM. It is an analog of Pifithrin-α that is cell-permeable but has greater stability and less cytotoxicity. Pifithrin-β has neuroprotective properties by reversing the effects of Alzheimer peptide non-amyloid component in human SH-SY5Y cells. The TP53 gene in humans is responsible for encoding the protein p53. 53 KD is the molecular weight of p53. The p53 gene controls the cell cycle, acting as a tumor suppressor and preventing the development of cancer. Through the activation of DNA repair proteins, cell growth arrest through holding the cell cycle, and induction of apoptosis, the p53 plays a critical role in apoptosis, the inhibition of angiogenesis, and genomic stability. DNA damage, osmotic shock, oxidative stress, and a variety of other stressors can all cause p53 to become activated. By binding to DNA, including p21, activated p53 activates the expression of numerous genes.

Biological Activity I Assay Protocols (From Reference)
Targets
p53 (IC50 = 23 μM)
ln Vitro
Pifithrin-α, an inhibitor of the p53 protein, is thought to be a promising drug for the treatment of cancer and neurodegenerative diseases. In culture medium, Pifithrin-α is very unstable and quickly transforms into its condensation product, pifithrin-β (PFT), the N-acetyl derivative[2]. Viability testing reveals that pretreatments with 1 and 10 μM pifithrin-β exert neuroprotective effects after 24 hours[3].
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 product pifithrin-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
C₁₆H₁₆N₂S
Molecular Weight
268.38
Exact Mass
268.10341969
Elemental Analysis
C, 55.02; H, 4.91; Br, 22.88; N, 8.02; S, 9.18
CAS #
60477-34-1
Appearance
Solid powder
SMILES
CC1=CC=C(C=C1)C2=CN3C4=C(CCCC4)SC3=N2
InChi Key
IMUKUMUNZJILCG-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H16N2S/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
Chemical Name
2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
Synonyms
Pifithrin-β; PFTβ; Pifithrin-beta; QB102; QB 102; QB-102; PFT-β; 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 3.7261 mL 18.6303 mL 37.2606 mL
5 mM 0.7452 mL 3.7261 mL 7.4521 mL
10 mM 0.3726 mL 1.8630 mL 3.7261 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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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Pifithrin-β


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

  • Pifithrin-β


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

  • Pifithrin-β


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

  • Pifithrin-β


    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


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

  • Pifithrin-β


    (A) Concentration–response curves of compound12and pifithrin-β.. 2014 May 21; 5(5): 3

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