(-)-Blebbistatin

製品コードS7099 バッチS709907

化学情報

	Synonyms	(S)-(-)-Blebbistatin	Storage (From the date of receipt)	3 years -20°C(in the dark) powder
	化学式	C₁₈H₁₆N₂O₂
	分子量	292.33	CAS No.	856925-71-8
Solubility (25°C)*	体外	DMSO	58 mg/mL (198.4 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	(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.
in vitro	Blebbistatin, inhibits cytokinesis, alters the smooth movement of fish keratocytes and inhibits the spontaneous blebbing of a cell line lacking filamin. Blebbistatin is shown to inhibit the enzymatic activities of HMM fragments of nonmuscle myosin IIA, nonmuscle myosin IIB and of rabbit skeletal muscle myosin S1, but not smooth muscle myosin^[1] Blebbistatin rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species, while poorly inhibiting smooth muscle myosin (IC50 = 80 μM). Blebbistatin potently inhibits Dictyostelium myosin II, but poorly inhibits Acanthamoeba myosin II. Blebbistatin does not inhibit representative myosin superfamily members from classes I, V, and X. ^[2] Blebbistatin does not compete with nucleotide binding to the skeletal muscle myosin subfragment-1. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release. Blebbistatin interferes neither with binding of myosin to actin nor with ATP-induced actomyosin dissociation. Instead, it blocks the myosin heads in a products complex with low actin affinity. ^[3]
in vivo	(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase.

製品説明

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.

in vitro

Blebbistatin, inhibits cytokinesis, alters the smooth movement of fish keratocytes and inhibits the spontaneous blebbing of a cell line lacking filamin. Blebbistatin is shown to inhibit the enzymatic activities of HMM fragments of nonmuscle myosin IIA, nonmuscle myosin IIB and of rabbit skeletal muscle myosin S1, but not smooth muscle myosin^[1]

Blebbistatin rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species, while poorly inhibiting smooth muscle myosin (IC50 = 80 μM). Blebbistatin potently inhibits Dictyostelium myosin II, but poorly inhibits Acanthamoeba myosin II. Blebbistatin does not inhibit representative myosin superfamily members from classes I, V, and X. ^[2]

Blebbistatin does not compete with nucleotide binding to the skeletal muscle myosin subfragment-1. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release. Blebbistatin interferes neither with binding of myosin to actin nor with ATP-induced actomyosin dissociation. Instead, it blocks the myosin heads in a products complex with low actin affinity. ^[3]

in vivo

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase.

プロトコル(参考用のみ)

キナーゼアッセイ	Actin-activated MgATPase assay
キナーゼアッセイ	Actin-activated MgATPase activity is measured using an NADH-coupled assay in a Beckman DU 640 spectrophotometer. Blebbistatin [a racemic mixture of the (+) and (-) enantiomers] is added from stocks dissolved in DMSO and the DMSO concentration is maintained at a constant concentration of 5% in all samples.
細胞アッセイ	細胞株	MDCK and U2OS cells
	濃度	25 µM
	反応時間	2-4 h
	実験の流れ	Cells were treated with vlebbistatin for 2-4 hours.
動物実験	動物モデル	Male Sprague–Dawley rats (TBI model)
	投薬量	10 mg/kg
	投与方法	i.p.

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , J Leukoc Biol, 2016, 143-53]

: Data from [Data independently produced by , , Biomed Res Int, 2018, 2018:2174824]

: Data from [Data independently produced by , , J Vasc Res, 2016, 53(3-4):206-215]

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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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