Pifithrin-α (PFTα) HBr

製品コードS2929 バッチS292903

印刷

化学情報

Chemical Structure Synonyms Pifithrin-α hydrobromide Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H18N2OS.HBr
分子量 367.3 CAS No. 63208-82-2
Solubility (25°C)* 体外 DMSO 73 mg/mL (198.74 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
in vitro Pifithrin-α inhibits p53-dependent transactivation of p53-responsive genes in ConA cells. Pifithrin-α (10 μM) inhibits apoptotic death of C8 cells induced by Dox, etoposide, Taxol, cytosine arabinoside. Pifithrin-α inhibits p53-dependent growth arrest of human diploid fibroblasts in response to DNA damage but has no effect on p53-deficient fibroblasts. Pifithrin-α may modulate the nuclear import or export (or both) of p53 or may decrease the stability of nuclear p53. [1] Pifithrin-α (100-200 nM) completely suppresses the camptothecin-induced increase in the level of p53 DNA binding as well as the p53-responsive gene Bax in hippocampal cell. Pifithrin-α also decreases the basal level of p53 DNA-binding activity. Pifithrin-α (200 nM) protects cultured hippocampal neurons against death induced by DNA-damaging agents. Pifithrin-α (200 μM) stabilizes mitochondrial function, suppresses caspase activation and protects cultured hippocampal neurons against death induced by glutamate and amyloid β-peptide. [2] Pifithrin α, in addition to p53, can suppress heat shock and glucocorticoid receptor signaling but has no effect on nuclear factor-kappaB signaling. Pifithrin α (10 μM) reduces activation of heat shock transcription factor (HSF1) and increases cell sensitivity to heat. Pifithrin α (10 μM) reduces activation of glucocorticoid receptor and rescues mouse thymocytes from apoptotic death after dexamethasone treatment in HeLa cells. [3] PFTalpha blocks p53-mediated induction of p21/Waf-1 in human embryonic kidney cells. PFTalpha does, however, cause a left shift in the dexamethasone dose response curve by increasing intracellular dexamethasone concentration. [4]
in vivo Pifithrin-α (2.2 mg/kg i.p.) treatment completely rescues mice (C57BL and Balb/c) of both strains from 60% killing doses of gamma irradiation (8 Gy for C57BL and 6 Gy for Balb/c). Pifithrin-α-injected mice lost less weight than irradiated mice that are not pretreated with the Pifithrin-α. Pifithrin-α (2.2 mg/kg) abrogates p53-dependent regulation of DNA replication after whole-body gamma irradiation in mice. [1] Pifithrin-α (2 mg/kg i.p.) 30 min prior to middle cerebral artery occlusion treatment of mice reduces ischemic brain injury and protects hippocampal neurons against excitotoxic injury. [2] Pifithrin α (3.6 μg/kg i.p.) inhibits Dex-induced degeneration of the thymus in mice. [3] Pifithrin α (2 mg/kg) results in a significantly lower degree of motor disability in rats receiving transient occlusion of the middle cerebral artery as compared with controls. Pifithrin α-treated animals has less motor disability and smaller infarcts when the drug is administered up to an hour after stroke onset. Pifithrin α results in significantly lower motor disability scores in rats than in the vehicle-treated animals at 7 days post-op. Pifithrin α results in significant reduction of apoptosis in rats as indicated by Tunel and caspase 3 staining. [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116 and Hela cells
濃度 ~10 μM
反応時間 48 hours
実験の流れ 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.
動物実験 動物モデル C57BL and Balb/c mice
投薬量 2.2 mg/kg
投与方法 Intraperitoneal injection

カスタマーフィードバック

, , Cell Prolif, 2017, doi: 10.1111/cpr.12319

Data from [Data independently produced by , , Cell Prolif, 2017, 50(6)]

Data from [Data independently produced by , , J Biol Chem, 2016, 291(9):4462-72]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

BOP1 contributes to the activation of autophagy in polycystic ovary syndrome via nucleolar stress response [ Cell Mol Life Sci, 2024, 81(1):101] PubMed: 38409361
Kidney tubular epithelial cells control interstitial fibroblast fate by releasing TNFAIP8-encapsulated exosomes [ Cell Death Dis, 2023, 14(10):672] PubMed: 37828075
Suppression of TREX1 deficiency-induced cellular senescence and interferonopathies by inhibition of DNA damage response [ iScience, 2023, 26(7):107090] PubMed: 37416470
Proximal Tubular Lats2 Ablation Exacerbates Ischemia/Reperfusion Injury -IRI)-Induced Renal Maladaptive Repair through the Upregulation of P53 [ Int J Mol Sci, 2023, 24(20)15258] PubMed: 37894939
Proximal Tubular Lats2 Ablation Exacerbates Ischemia/Reperfusion Injury (IRI)-Induced Renal Maladaptive Repair through the Upregulation of P53 [ Int J Mol Sci, 2023, 24(20)15258] PubMed: 37894939
Hepatitis B doubly spliced protein (HBDSP) promotes hepatocellular carcinoma cell apoptosis via ETS1/GATA2/YY1-mediated p53 transcription [ J Virol, 2023, 10.1128/jvi.01087-23] PubMed: 37929990
DRP1 Inhibition Enhances Venetoclax-Induced Mitochondrial Apoptosis in TP53-Mutated Acute Myeloid Leukemia Cells through BAX/BAK Activation [ Cancers (Basel), 2023, 15(3)745] PubMed: 36765703
RPS14 promotes the development and progression of glioma via p53 signaling pathway [ Exp Cell Res, 2023, 423(1):113451] PubMed: 36535509
Curcumin Analog, HO-3867, Induces Both Apoptosis and Ferroptosis via Multiple Mechanisms in NSCLC Cells with Wild-Type p53 [ Evid Based Complement Alternat Med, 2023, 2023:8378581] PubMed: 36814470
p53 positively regulates the proliferation of hepatic progenitor cells promoted by laminin-521 [ Signal Transduct Target Ther, 2022, 7(1):290] PubMed: 36042225

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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