Y16

製品コードS6752 バッチS675201

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₄H₂₀N₂O₃
	分子量	384.43	CAS No.	429653-73-6
Solubility (25°C)*	体外	DMSO	39 mg/mL (101.44 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	Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM).
in vitro	Y16 binds to the junction site of the DH-PH domains of LARG with a ∼80 nM Kd and suppresses LARG catalyzed RhoA activation dose dependently. It is active in blocking the interaction of LARG and related G-protein–coupled Rho GEFs with RhoA without a detectable effect on other DBL family Rho GEFs, Rho effectors, or a RhoGAP. In cells, Y16 selectively inhibits serum-induced RhoA activity and RhoA-mediated signaling, effects that can be rescued by a constitutively active RhoA or ROCK mutant. By suppressing RhoA activity, Y16 inhibits mammary sphere formation of MCF7 breast cancer cells but does not affect the nontransforming MCF10A cells. Y16 works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG–RhoA interaction, RhoA activation, and RhoA-mediated signaling functions. Y16 effectively inhibits the growth, migration, and invasion activities of breast cancer cells^[1].

製品説明

Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM).

in vitro

Y16 binds to the junction site of the DH-PH domains of LARG with a ∼80 nM Kd and suppresses LARG catalyzed RhoA activation dose dependently. It is active in blocking the interaction of LARG and related G-protein–coupled Rho GEFs with RhoA without a detectable effect on other DBL family Rho GEFs, Rho effectors, or a RhoGAP. In cells, Y16 selectively inhibits serum-induced RhoA activity and RhoA-mediated signaling, effects that can be rescued by a constitutively active RhoA or ROCK mutant. By suppressing RhoA activity, Y16 inhibits mammary sphere formation of MCF7 breast cancer cells but does not affect the nontransforming MCF10A cells. Y16 works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG–RhoA interaction, RhoA activation, and RhoA-mediated signaling functions. Y16 effectively inhibits the growth, migration, and invasion activities of breast cancer cells^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PC-3 cells
	濃度	10 μM
	反応時間	36 h
	実験の流れ	PC-3 cells were quiesced in RPMI1640 containing 0.5% FBS for 24 hr. Cells were then trypsinized, resuspended in RPMI1640 containing 0.5% FBS, and counted. A total of 2.5 × 10⁴ cells were loaded into the upper chamber. The lower chamber was filled with RPMI1640 supplemented with 10% FCS. A13 (10 μM), A2 (10 μM), Y16 (10 μM), or DMSO was added both in the upper and lower chambers. The concentration of DMSO in the medium was 0.1% for all experimental conditions. After a 36 hr incubation period, the cell suspension was aspirated, and the membranes were fixed in 70% ethanol at -20℃ for 20 min. Cells that had attached but not migrated were removed, the membranes were rinsed in water, and migrated cells on the underside of the membrane were visualized with staining in 2% crystal violet. Cells were counted on three independent transwell membranes using a light microscope.

参考

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。