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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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| Related CAS # |
Pifithrin-β hydrobromide;511296-88-1
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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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| Solubility (In Vivo) |
注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。 注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) (Please use freshly prepared in vivo formulations for optimal results.) |
| 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. |
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 NAC treatment induced cell cycle arrest.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. |
 NAC induced apoptotic cell death.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. |
 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. |
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 Neuroprotective effects of compounds4,12, and19.ACS Chem Neurosci. 2014 May 21; 5(5): 390–399. |
 (A) Concentration–response curves of compound12and pifithrin-β.ACS Chem Neurosci. 2014 May 21; 5(5): 3 |
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