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2mg |
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5mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
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.
Targets |
p53 (IC50 = 23 μM)
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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].
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References |
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Molecular Formula |
C₁₆H₁₆N₂S
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Molecular Weight |
268.38
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Exact Mass |
268.10341969
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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 # |
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
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InChi Key |
IMUKUMUNZJILCG-UHFFFAOYSA-N
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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
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Chemical Name |
2-(4-methylphenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole
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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 |
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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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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.
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): 3 td> |