MZ-1

製品コードS8889 バッチS888902

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₄₉H₆₀ClN₉O₈S₂

分子量

1002.64

CAS No.

1797406-69-9

Solubility (25°C)*

体外

DMSO

100 mg/mL (99.73 mM)

Ethanol

100 mg/mL (99.73 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml
	5% DMSO 1 95% Corn oil	2.5mg/ml

* <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	MZ-1 is a PROTAC degrader of bromodomain-containing protein 4 (BRD4). MZ-1 binds to the Brd bromodomain with Kd of 62 nM, 60 nM, 21 nM, 13 nM, 39 nM and 15 nM for Brd2^BD1, Brd2^BD2, Brd3^BD1, Brd3^BD2, Brd4^BD1 and Brd4^BD2.
in vitro	MZ-1 induces apoptosis of ovarian cancer cells and inhibits periostin-mediated ovarian cancer cell migration and invasion in vitro. MZ-1 specifically and efficiently inhibits the colony formation of periostin cells in soft agar, which clearly indicates a proproliferation role of periostin.^[2]
in vivo	Our in vivo studies shows significant growth inhibition by MZ-1 on both subcutaneous and intraperitoneal (i.p.) tumors derived from the periostin-expressing ovarian cancer cell line A2780. In addition, MZ-1 treatment leads to a reduction of the metastatic potential of these A2780 i.p. tumors. The in vivo antitumor effects of MZ-1 are linked to its specific inhibition of anchorage-independent growth and survival of periostin-expressing cells, as well as its neutralizing effects on periostin-induced cancer cell migration and invasion.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	A2780, OAW-42, SKOV-3, TOV-112D, ES2, SP2/0 cell line
	濃度	20 μM
	反応時間	2 and 4 days
	実験の流れ	In vitro apoptosis assay: Cells are grown in 24-well plates in serum-free medium (SFM) plus 1% BSA overnight to reach 50% to 60% confluency. A portion of 20 mg/mL of MZ-1 or control antibody is added into the wells. Cell apoptosis is analyzed 2 and 4 days later by using Annexin V-FITC Apoptosis Detection Kit. The cell flow cytometry is carried on Cell LabQuanta SC.
動物実験	動物モデル	Female SCID beige mice (6-8 weeks old) with A2780/TOV-112D xenografts
	投薬量	20 mg/kg
	投与方法	IH/SC, IP

参考

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：

Screening of an epigenetic compound library identifies BRD4 as a potential antiviral target for hepatitis B virus covalently closed circular DNA transcription [ Antiviral Res, 2023, 211:105552]	PubMed: 36737008
Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation [ Int Immunopharmacol, 2023, 117:109929]	PubMed: 36857935
Genomic Mapping of Splicing-Related Genes Identify Amplifications in LSM1, CLNS1A, and ILF2 in Luminal Breast Cancer [ Cancers (Basel), 2021, 13(16)4118]	PubMed: 34439272

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。