Monastrol

製品コードS8439 バッチS843902

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	69 mg/mL (236.01 mM)
		Ethanol	15 mg/mL (51.3 mM)
		Water	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	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 monastrol is also rapidly reversible. Monastrol also inhibits bipolar spindle formation in Xenopus egg extracts. Monastrol 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 monastrol 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, monastrol 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 monastrol is also rapidly reversible. Monastrol also inhibits bipolar spindle formation in Xenopus egg extracts. Monastrol 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 monastrol 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, monastrol 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 monastrol 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 monastrol 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

[4] Mayer TU, et al. Science. 1999, 286(5441):971-4.

+ 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：

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
Genetic instability from a single S phase after whole-genome duplication [ Nature, 2022, 604(7904):146-151]	PubMed: 35355016
Pathogenic mutations in the chromokinesin KIF22 disrupt anaphase chromosome segregation [ Elife, 2022, 11e78653]	PubMed: 35730929
SCFFBXW7 regulates G2-M progression through control of CCNL1 ubiquitination [ EMBO Rep, 2022, e55044]	PubMed: 36278408
The deubiquitinating enzyme complex BRISC regulates Aurora B activation via lysine-63-linked ubiquitination in mitosis [ Commun Biol, 2022, 5(1):1335]	PubMed: 36473924
Inhibitor library screening identifies ispinesib as a new potential chemotherapeutic agent for pancreatic cancers [ Cancer Sci, 2021, 112(11):4641-4654]	PubMed: 34510663
The Aurora-A/TPX2 Axis Directs Spindle Orientation in Adherent Human Cells by Regulating NuMA and Microtubule Stability [ Curr Biol, 2020, S0960-9822(20)31673-0]	PubMed: 33275894
The kinesin-5 tail domain directly modulates the mechanochemical cycle of the motor domain for anti-parallel microtubule sliding. [ Elife, 2020, 9]	PubMed: 31958056
Phosphorylation of CENP-A on serine 7 does not control centromere function. [ Nat Commun, 2019, 10(1):175]	PubMed: 30635586

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。