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产地 | 武汉 |
品牌 | Chemstan |
货号 | CS-15484 |
用途 | 科研 |
英文名称 | Pifithrin-α hydrobromide |
包装规格 | 5 mg |
纯度 | 100%% |
CAS编号 | 63208-82-2 |
别名 | PFTα hydrobromide,?Pifithrin hydrobromide,?Pifithrin-α hydrobromide,?Pifithrin-α (PFTα) HBr,?PFTα |
分子式 | C16H18N2OS稨Br? |
是否进口 | 否 |
Description |
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist. |
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IC50 & Target |
p53[1] |
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In Vitro |
Pifithrin-α (PFT-α) hydrobromideis a water-soluble compound that could suppress p53 protein transcription. Pifithrin-α can suppress glucose oxidase (GOX)-induced p53 protein increase in whole cell lysates, but cyclosporine A (CsA) fails to show such an inhibition effect. Notably, Pifithrin-α is able to block the GOX-induced Bcl-2 protein reduction. Similarly, it is Pifithrin-α rather than CsA that able to prevent the Bax increasing in whole cell lysates[1] . Pifithrin-α inhibits p53-dependent apoptosis through an undetermined mechanism. Pifithrin-α also acts as an aryl hydrocarbon receptor (AhR) agonist and. Pifithrin-α is a potent AhR agonist as determined by its ability to bind the AhR, induce formation of its DNA binding complex, activate reporter activity, and up-regulate the classic AhR target gene CYP1A1[2] . MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
When the experiment is performed with Pifthirin-α (PFT-α) hydrobromide, a pharmacological p53 inhibitor, the percentage of annexin V-positive Foxe3-/- SMCs decreases to WT levels. Pifithrin-α (2.2 mg/kg, i.p.) significantly reduces the incidence of aortic rupture and intramural hematomas in Foxe3-/- mice that underwent transverse aortic constriction (TAC) (50% to 17%, P<0.05). After Pifthirin-α treatment, the mean diameter of the ascending aorta and the percentage of TUNEL-positive cells in the aortic media are also normalized to WT levels in surviving Foxe3-/- animals (P<0.05)[3] . MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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Molecular Weight |
367.30 |
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Formula |
C??H??BrN?OS |
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CAS No. |
63208-82-2 |
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SMILES |
N=C1SC2=C(CCCC2)N1CC(C3=CC=C(C)C=C3)=O.[H]Br |
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Shipping |
Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : ≥ 50 mg/mL (136.13 mM) * "≥" means soluble, but saturation unknown.
Preparing
Stock Solutions
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
In Vivo:
请根据您的实验动物和给药方式 选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
*以上所有助溶剂都可在 MCE 网站选购。
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References |
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