Pifithrin-μ

製品コードS2930 バッチS293001

印刷

化学情報

Synonyms

NSC 303580, PFTμ, 2-Phenylethynesulfonamide

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₈H₇NO₂S

分子量

181.21

CAS No.

64984-31-2

Solubility (25°C)*

体外

DMSO

36 mg/mL (198.66 mM)

Ethanol

36 mg/mL (198.66 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

2.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy.
in vitro	Pifithrin-μ interferes with p53 binding to mitochondria and inhibits rapid p53-dependent apoptosis of primary cell cultures of mouse thymocytes in response to gamma radiation. ^[1] Pifithrin-μ, as an inhibitor of inducible HSP70, significantly inhibited cell viability with IC50 values ranging from 2.5 to 12.7 μM in acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines, as well as in primary AML blasts. Pifithrin-μ is also highly active in primary AML blasts with a median IC50 of 8.9 μ M(range 5.7-37.2 μ M) and induces apoptosis and cell cycle arrest in a dose-dependent fashion. In addition, Pifithrin-μ also increases the active form of caspase-3 and reduces AKT and ERK1/2 in NALM-6 cells. ^[2] Pifithrin-μ increases Annexin V(+) cells in both caspase-dependent and -independent manners and promotes TRAIL-induced apoptosis and arrested cancer cell growth. ^[3]
in vivo	Pifithrin-μ (40 mg/kg, ip) produces protective effect from p53-dependent apoptosis in C57B1/6J mice of 8 or 9 Gy of total body gamma radiation. ^[1] In a xenograft mouse model, Pifithrin-μ significantly enhances the inhibition of TRAIL on MiaPaca-2 tumor growth. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Primary thymocytes
	濃度	0-10 μM
	反応時間	24 hours
	実験の流れ	The number of attached cells is estimated by staining with 0.5% methylene blue and measuring optical density using a Multiscan Ascent microplate reader. Cell viability is determined in suspension of short-term culture of primary thymocytes by staining them with 0.1% trypan blue2 or by analysis of annexin- or propidium iodide (PI)-positive cells by FACScan.
動物実験	動物モデル	C57B1/6J mice.
	投薬量	~40 mg/kg
	投与方法	i.p.

参考

カスタマーフィードバック

: Data from [Data independently produced by Biochim Biophys Acta, 2014, 1842(11), 2204-15]

: , , J Leukoc Biol, 2016, 100(5):1061-1070

: Data from [Data independently produced by , , Oncogene, 2018, 37(8):1041-1048]

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：

Suppression of TREX1 deficiency-induced cellular senescence and interferonopathies by inhibition of DNA damage response [ iScience, 2023, 26(7):107090]	PubMed: 37416470
p53 regulates the effects of DAPT on Rac1 activation and migration of non-small-cell lung cancer cells [ Heliyon, 2023, 9(3):e14169]	PubMed: 36923886
A curcumin analogue GO-Y030 depletes cancer stem cells by inhibiting the interaction between the HSP70/HSP40 complex and its substrates [ FEBS Open Bio, 2023, none]	PubMed: 36648092
Paired box 5 increases the chemosensitivity of esophageal squamous cell cancer cells by promoting p53 signaling activity [ Chin Med J (Engl), 2022, 135(5):606-618]	PubMed: 35191417
Abrogation of Cellular Senescence Induced by Temozolomide in Glioblastoma Cells: Search for Senolytics [ Cells, 2022, 11(16)2588]	PubMed: 36010664
CD44a functions as a regulator of p53 signaling, apoptosis and autophagy in the antibacterial immune response [ Commun Biol, 2022, 5-1:889]	PubMed: 36042265
IMP075 targeting ClpP for colon cancer therapy in vivo and in vitro [ Biochem Pharmacol, 2022, 204:115232]	PubMed: 36030831
Cinobufagin alleviates lipopolysaccharide-induced acute lung injury by regulating autophagy through activation of the p53/mTOR pathway [ Front Pharmacol, 2022, 13:994625]	PubMed: 36518680
Vibrio splendidus flagellin C binds tropomodulin to induce p38 MAPK-mediated p53-dependent coelomocyte apoptosis in Echinodermata [ J Biol Chem, 2022, 298(7):102091]	PubMed: 35654141
Mammalian Ddi2 is a shuttling factor containing a retroviral protease domain that influences binding of ubiquitylated proteins and proteasomal degradation [ J Biol Chem, 2022, 298(5):101875]	PubMed: 35358511

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。