Monastrol

製品コードS8439 バッチS843901

印刷

化学情報

Synonyms

(±)-Monastrol

Storage
(From the date of receipt)

3 years -20°C(in the dark) powder

化学式

C₁₄H₁₆N₂O₃S

分子量

292.35

CAS No.

329689-23-8

Solubility (25°C)*

体外

DMSO

58 mg/mL (198.39 mM)

Ethanol

58 mg/mL (198.39 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	2.900mg/ml (9.92mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.710mg/ml (2.43mM)

* <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	Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.
in vitro	Monastrol does not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to this compound is also rapidly reversible. It also inhibits bipolar spindle formation in Xenopus egg extracts. This chemical arrests cells in mitosis with monoastral spindles comprised of a radial array of microtubules surrounded by a ring of chromosomes while it does not affect microtubules in interphase cells or microtubule polymerization in vitro^[1]. Exposure of cultured sympathetic neurons to this compound for a few hours increases both the number and the growth rate of the axons. With additional time, the overall lengths of the axons are indistinguishable from controls. Sensory neurons shows a similar short-term increase in axonal growth rate. However, prolonged exposure results in shorter axons, suggesting that sensory neurons may be more sensitive to toxic effects of the drug. Nevertheless, the overall health of the cultures is still far more robust than cultures treated with taxol, a drug commonly used for anti-cancer therapy^[2]. In HeLa cells, this compound activates the spindle checkpoint, leading to mitotic arrest and apoptosis^[3].

製品説明

Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.

in vitro

Monastrol does not inhibit progression through S and G2 phases of the cell cycle or centrosome duplication. The mitotic arrest due to this compound is also rapidly reversible. It also inhibits bipolar spindle formation in Xenopus egg extracts. This chemical arrests cells in mitosis with monoastral spindles comprised of a radial array of microtubules surrounded by a ring of chromosomes while it does not affect microtubules in interphase cells or microtubule polymerization in vitro^[1]. Exposure of cultured sympathetic neurons to this compound for a few hours increases both the number and the growth rate of the axons. With additional time, the overall lengths of the axons are indistinguishable from controls. Sensory neurons shows a similar short-term increase in axonal growth rate. However, prolonged exposure results in shorter axons, suggesting that sensory neurons may be more sensitive to toxic effects of the drug. Nevertheless, the overall health of the cultures is still far more robust than cultures treated with taxol, a drug commonly used for anti-cancer therapy^[2]. In HeLa cells, this compound activates the spindle checkpoint, leading to mitotic arrest and apoptosis^[3].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	BS-C-1 (monkey epithelial kidney) cells
	濃度	100 μM
	反応時間	4 h
	実験の流れ	For the double thymidine arrest, exponentially growing BS-C-1 cells are cultured for 16 h in normal growth medium containing 2 mM thymidine. After this, the cells are released into normal growth medium supplemented with 24 μM deoxycytidine for 9 h. The second thymidine block is imposed for 16 h during which the cells were maintained in serum-free medium containing 2 mM thymidine. Finally, the cells are released into normal growth medium containing 24 μM deoxycytidine to which is added either 100 μM monastrol or 0.1% DMSO. To assess the reversibility of the effect of this compound and nocodazole treatment, BS-C-1 cells plated on coverslips are treated for 4 h in normal growth medium containing either 2 μM nocodazole or 100 μM this chemical and then released into normal medium. At the different time points, coverslips are processed for immunofluorescence and the cells in interphase or mitosis are counted and categorized.

参考

https://pubmed.ncbi.nlm.nih.gov/10973989/
https://pubmed.ncbi.nlm.nih.gov/14983520/
https://pubmed.ncbi.nlm.nih.gov/17041103/

https://pubmed.ncbi.nlm.nih.gov/10542155/

+ 展开

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：

EHMT2-mediated R-loop formation promotes the malignant progression of prostate cancer via activating Aurora B [ Clin Transl Med, 2025, 15(1):e70164]	PubMed: 39763034
CENP-C-Mis12 complex establishes a regulatory loop through Aurora B for chromosome segregation [ Life Sci Alliance, 2025, 8(1)e202402927]	PubMed: 39433344
Human REXO4 is Required for Cell Cycle Progression [ bioRxiv, 2025, 2025.01.08.631954]	PubMed: 39829749
Measuring and modeling the dynamics of mitotic error correction [ Proc Natl Acad Sci U S A, 2024, 121(25):e2323009121]	PubMed: 38875144
Simple aneuploidy evades p53 surveillance and promotes niche factor-independent growth in human intestinal organoids [ Mol Biol Cell, 2024, 35(8):br15]	PubMed: 38985518
Harnessing transcriptionally driven chromosomal instability adaptation to target therapy-refractory lethal prostate cancer [ Cell Rep Med, 2023, 4(2):100937]	PubMed: 36787737
Antagonistic interactions among structured domains in the multivalent Bicc1-ANKS3-ANKS6 protein network govern phase transitioning of target mRNAs [ iScience, 2023, 26(6):106855]	PubMed: 37275520
Genome-wide CRISPR Screening in FBXW7-mutant Cells Uncovers Multiple Druggable Synthetic Lethal Interactions Involving Cell Cycle Control [ University of Toronto, 2023, 29994742]	PubMed: None
Genome-Wide CRISPR Screening in FBXW7-Mutant Cells Uncovers Multiple Druggable Synthetic Lethal Interactions Involving Cell Cycle Control [ Graduate Department of Biochemistry University of Toronto, 2023, ]	PubMed: None
Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151]	PubMed: 35355016

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。