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Pifithrin-α hydrobromide

产品编号 T2707 CAS 63208-82-2

别名: Pifithrin hydrobromide, Pifithrin-α (PFTα) HBr, Pifithrin-α, PFTα, PFTα hydrobromide

Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) 是一种 p53 抑制剂，可抑制 p53 反应基因的 p53 依赖性反式激活。它也是芳烃受体的激动剂。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Pifithrin-α hydrobromide Chemical Structure

Pifithrin-α hydrobromide, CAS 63208-82-2

规格	价格/CNY	货期
1 mg	￥ 273	现货
2 mg	￥ 388	现货
5 mg	￥ 628	现货
10 mg	￥ 843	现货
25 mg	￥ 1,680	现货
50 mg	￥ 2,880	现货
100 mg	￥ 4,090	现货
1 mL * 10 mM (in DMSO)	￥ 628	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.
体外活性	小鼠腹腔注射3.6 μg/kg Pifithrin-α,抑制Dex诱导的胸腺退化.Pifithrinα（2 mg/kg）与对照组相比,在大脑中动脉暂时闭塞的大鼠中导致运动障碍程度显著降低.在小鼠大脑中动脉闭塞治疗前30分钟,Pifithrin-α（2 mg/kg i.p.）减少缺血性脑损伤并保护海马神经元免受兴奋毒性损伤.C57BL和Balb/c小鼠腹腔注射2.2 mg/kg Pifithrin-α,使小鼠完全免受60％致死率的γ射线照射造成的损伤.通过Tunel和caspase 3染色,观察到 Pifithrin-α明显降低大鼠的细胞凋亡.当在中风发作后一小时内施用药物时,Pifithrinα处理的动物具有较少的运动障碍和较小的梗塞.与空白对照组相比,Pifithrin-α处理7天后,明显降低大鼠的运动障碍评分.
体内活性	10 μM Pifithrin-α抑制Dox,Etoposide,Taxol和Cytosine arabinoside诱导的C8细胞凋亡。10 μM Pifithrin-α降低热休克转录因子的激活,且增强细胞对热的敏感性。10 μM Pifithrin-α降低HeLa细胞中糖皮质激素受体的激活,且保护小鼠胸腺免受Dexamethasone诱导的凋亡。100–200 nM Pifithrin-α完全抑制海马细胞中Camptothecin诱导的p53 DNA结合水平和p53应答基因Bax的增加。200 nM Pifithrin-α保护培养的海马神经元免受DNA损伤剂诱导的死亡。200 μM Pifithrin-α稳定线粒体功能,抑制caspase活化,保护培养的海马神经元免受谷氨酸和β-淀粉样肽诱导的死亡。 Pifithrin-α抑制人类二倍体成纤维细胞对DNA损伤的p53依赖性生长抑制,但对p53缺陷型成纤维细胞没有影响。Pifithrin-α可调节p53的核输入或输出（或两者同时）,也可降低核p53的稳定性。Pifithrin-α可以抑制热休克和糖皮质激素受体信号,但不影响NF-κB信号。
激酶实验	The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25 mM Hepes, 1 mM EDTA, 1 mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4 mM leupeptin, 4 mg/mL aprotinin, and 0.3 mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120 μg) are incubated at room temperature for 2 h with the indicated concentrations of Pifithrin-α in the presence of 3 nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice, resuspended in 0.2 mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone[2].
细胞实验	At the end of cell treatments, the number of attached cells is estimated by staining with 0.25% crystal violet in 50% methanol, followed by elution of the dye with 1% SDS. Optical density (530 nm) reflecting the number of stained cells is determined with a Bio-Tek EL311 microplate reader. Cell viability in suspension of short term culture of primary thymocytes is determined by their staining with 0.1% of methyl blue and microscopic counting of blue (dead) cells.(Only for Reference)

别名	Pifithrin hydrobromide, Pifithrin-α (PFTα) HBr, Pifithrin-α, PFTα, PFTα hydrobromide
分子量	367.3
分子式	C16H18N2OS·HBr
CAS No.	63208-82-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 36.7 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7226 mL	13.6129 mL	27.2257 mL	68.0643 mL
	5 mM	0.5445 mL	2.7226 mL	5.4451 mL	13.6129 mL
	10 mM	0.2723 mL	1.3613 mL	2.7226 mL	6.8064 mL
	20 mM	0.1361 mL	0.6806 mL	1.3613 mL	3.4032 mL
	50 mM	0.0545 mL	0.2723 mL	0.5445 mL	1.3613 mL
	100 mM	0.0272 mL	0.1361 mL	0.2723 mL	0.6806 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Komarov PG, et al. Science, 1999, 285(5434), 1733-1737. 2. Culmsee C, et al. J Neurochem, 2001, 77(1), 220-228. 3. Komarova EA, et al. J Biol Chem, 2003, 278(18), 15465-15468. 4. Murphy PJ, et al. J Biol Chem, 2004, 279(29), 320195-3201201. 5. Leker RR, et al. Exp Neurol, 2004, 187(2), 478-486. 6. Yu W, et al. Cyclosporine A Suppressed Glucose Oxidase Induced P53 Mitochondrial Translocation and Hepatic Cell Apoptosis through Blocking Mitochondrial Permeability Transition. Int J Biol Sci. 2016 Jan 1;12(2):198-209. 7. Kuang SQ, et al. FOXE3 mutations predispose to thoracic aortic aneurysms and dissections. J Clin Invest. 2016 Mar 1;126(3):948-61. 8. Lu L, Li K, Mao Y H, et al. Gold-chrysophanol nanoparticles suppress human prostate cancer progression through inactivating AKT expression and inducing apoptosis and ROS generation in vitro and in vivo[J]. International journal of oncology. 2017 Oct;51(4):1089-1103. 9. Zhou Y, Yang L, Xiong L, et al. KIF11 is upregulated in colorectal cancer and silencing of it impairs tumor growth and sensitizes colorectal cancer cells to oxaliplatin via p53/GSK3β signaling[J]. Journal of Cancer. 2021, 12(12): 3741.

文献引用

1. Chen L, Zhang L, Jin G, et al.Synergy of 5-aminolevulinate supplement and CX3CR1 suppression promotes liver regeneration via elevated IGF-1 signaling.Cell Reports.2023, 42(8). 2. Lin X, Lin T, Wang X, et al.Sesamol serves as a p53 stabilizer to relieve rheumatoid arthritis progression and inhibits the growth of synovial organoids.Phytomedicine.2023: 155109. 3. Wu Y, Zhou T, Qian D, et al.Z-Guggulsterone Induces Cell Cycle Arrest and Apoptosis by Targeting the p53/CCNB1/PLK1 Pathway in Triple-Negative Breast Cancer.ACS Omega.2023 4. Hussain M, Lu Y, Tariq M, et al. A small-molecule Skp1 inhibitor elicits cell death by p53-dependent mechanism. Iscience. 2022, 25(7): 104591. 5. Yang R, Yang H, Wei J, et al. Mechanisms Underlying the Effects of Lianhua Qingwen on Sepsis-Induced Acute Lung Injury: A Network Pharmacology Approach. Frontiers in Pharmacology. 2021: 2839. 6. Wu X, Han C, Wang L, et al. Iron increases the susceptibility of colorectal cancer cells to compound Kushen Injection via the decrease of TOP2A and p53. Pharmacological Research-Modern Chinese Medicine. 2022, 2: 100058. 7. Luo Y, Gao X, Zou L, et al. Bavachin Induces Ferroptosis through the STAT3/P53/SLC7A11 Axis in Osteosarcoma Cells. Oxidative Medicine and Cellular Longevity. 2021 8. Guo Y, Li Q, Zhao G, et al. Loss of TRIM31 promotes breast cancer progression through regulating K48-and K63-linked ubiquitination of p53. Cell Death & Disease. 2021, 12(10): 1-13. 9. Shang Y, Zhang S, Cheng Y, et al. Tetrabromobisphenol a exacerbates the overall radioactive hazard to zebrafish (Danio rerio). Environmental Pollution. 2022: 120424. 10. Jiang W, Wang X, Su S, et al. Identifying the shared genes and KEGG pathways of Resolvin D1-targeted network and osteoarthritis using bioinformatics. Bioengineered. 2022, 13(4): 9839-9854

11. Zhou Y, Yang L, Xiong L, et al. KIF11 is upregulated in colorectal cancer and silencing of it impairs tumor growth and sensitizes colorectal cancer cells to oxaliplatin via p53/GSK3β signaling. Journal of Cancer. 2021, 12(12): 3741. 12. Lu L, Li K, Mao Y H, et al. Gold-chrysophanol nanoparticles suppress human prostate cancer progression through inactivating AKT expression and inducing apoptosis and ROS generation in vitro and in vivo. International Journal of Oncology. 2017 Oct;51(4):1089-1103 13. Wu X, Wang L, Li Z. Identification of 3-Phenylquinoline Derivative PQ1 as an Antagonist of p53 Transcriptional Activity. ACS Omega. 2022 14. Su Q, Wang J, Ren J, et al.Parkin deficiency promotes liver cancer metastasis by TMEFF1 transcription activation via TGF-β/Smad2/3 pathway.Acta Pharmacologica Sinica.2024: 1-10.

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Pifithrin-α hydrobromide 63208-82-2 Apoptosis Immunology/Inflammation Ferroptosis Aryl Hydrocarbon Receptor p53 inhibit Pifithrin-a (PFTa) HBr Pifithrin α hydrobromide Inhibitor MDM-2/p53 Pifithrin-alpha PFTa Hydrobromide Pifithrin-alpha Hydrobromide Pifithrin-a AhR Pifithrin Pifithrin hydrobromide PFTalpha Hydrobromide Pifithrin-α (PFTα) HBr Pifithrin Hydrobromide PFTalpha Pifithrin-α Pifithrin-a Hydrobromide PFTα Pifithrin-alpha (PFTalpha) HBr Pifithrinα hydrobromide PFTα Hydrobromide Pifithrin-α Hydrobromide PFTα hydrobromide PFTa inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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Pifithrin-α hydrobromide

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords