Y-27632

Y-27632 是口服有效的，ATP 競爭性的 ROCK-I 和 ROCK-II 抑制劑，Ki 分別為 220 nM 和 300 nM。Y-27632 減弱阿霉素誘導的人心臟干細胞凋亡 (apoptosis)。Y-27632 還抑制分離誘導的小鼠前列腺干/祖細胞凋亡。Y-27632 通過上皮-間充質(zhì)過渡樣調(diào)節(jié)引發(fā)人誘導多能干細胞 (hIPSCs) 選擇性地分化為間胚層譜系。

貨號：HY-10071
CAS：146986-50-7

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-10071

起訂量：1

規(guī)格:：10mg

價格:：￥900

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15906629305

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產(chǎn)品詳情

Y-27632 是口服有效的，ATP 競爭性的 ROCK-I 和 ROCK-II 抑制劑，K_i 分別為 220 nM 和 300 nM。Y-27632 減弱阿霉素誘導的人心臟干細胞凋亡 (apoptosis)。Y-27632 還抑制分離誘導的小鼠前列腺干/祖細胞凋亡。Y-27632 通過上皮-間充質(zhì)過渡樣調(diào)節(jié)引發(fā)人誘導多能干細胞 (hIPSCs) 選擇性地分化為間胚層譜系。

生物活性

Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with K_is of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation

體外研究(In Vitro)

Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively^[1].
Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 μM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 μM Y-27632 induced group^[2].
Extracellular matrix (ECM) molecules decreases apoptosis markers and inhibiting the ROCK pathway blocks ECM stimulated actin cortical mat reformation and increases apoptosis in embryonic corneal epithelial cells

體內(nèi)研究(In Vivo)

Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group^[3]. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group)

分子量：247.34

Formula：C₁₄H₂₁N₃O

CAS 號：146986-50-7

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性數(shù)據(jù)

DMSO : 50 mg/mL (202.15 mM; Need ultrasonic)

H₂O : 1 mg/mL (4.04 mM; ultrasonic and warming and heat to 60°C)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	4.0430 mL	20.2151 mL	40.4302 mL
5 mM	0.8086 mL	4.0430 mL	8.0860 mL
10 mM	0.4043 mL	2.0215 mL	4.0430 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
4.

請依序添加每種溶劑： Saline
Solubility: 2 mg/mL (8.09 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

參考文獻

[1]. Ishizaki T, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.

[2]. Xue ZW, et al. Rho-associated coiled kinase inhibitor Y-27632 promotes neuronal-like differentiation of adult human adipose tissue-derived stem cells.Chin Med J (Engl). 2012 Sep;125(18):3332-5.

[3]. Tada S, et al. A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats. J Hepatol. 2001 Apr;34(4):529-36.

[4]. Inan S, et al. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br J Pharmacol. 2008 Sep;155(1):44-51.

[5]. Maldonado M, et al. ROCK inhibitor primes human induced pluripotent stem cells to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymal transition-like modulation. Stem Cell Res. 2016 Sep;17(2):222-227.

[6]. Kan L, et al. Rho-Associated Kinase Inhibitor (Y-27632) Attenuates Doxorubicin-Induced Apoptosis of Human Cardiac Stem Cells. PLoS One. 2015;10(12):e0144513. Published 2015 Dec 8.

[7]. Zhang L, et al. ROCK inhibitor Y-27632 suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells and increases their cloning efficiency. PLoS One. 2011;6(3):e18271. Published 2011 Mar 28.

[8]. Svoboda KK, et al. ROCK inhibitor (Y27632) increases apoptosis and disrupts the actin cortical mat in embryonic avian corneal epithelium. Dev Dyn. 2004;229(3):579-590.

Y-27632

Y-27632 是口服有效的，ATP 競爭性的 ROCK-I 和 ROCK-II 抑制劑，Ki 分別為 220 nM 和 300 nM。Y-27632 減弱阿霉素誘導的人心臟干細胞凋亡 (apoptosis)。Y-27632 還抑制分離誘導的小鼠前列腺干/祖細胞凋亡。Y-27632 通過上皮-間充質(zhì)過渡樣調(diào)節(jié)引發(fā)人誘導多能干細胞 (hIPSCs) 選擇性地分化為間胚層譜系。

貨號：HY-10071
CAS：146986-50-7

品牌：MCE

型號：HY-10071

起訂量：1

規(guī)格:：10mg

價格:：￥900

15906629305

在線客服

客服一

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產(chǎn)品詳情

Y-27632 是口服有效的，ATP 競爭性的 ROCK-I 和 ROCK-II 抑制劑，K_i 分別為 220 nM 和 300 nM。Y-27632 減弱阿霉素誘導的人心臟干細胞凋亡 (apoptosis)。Y-27632 還抑制分離誘導的小鼠前列腺干/祖細胞凋亡。Y-27632 通過上皮-間充質(zhì)過渡樣調(diào)節(jié)引發(fā)人誘導多能干細胞 (hIPSCs) 選擇性地分化為間胚層譜系。

生物活性

Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with K_is of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation

體外研究(In Vitro)

Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively^[1].
Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 μM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 μM Y-27632 induced group^[2].
Extracellular matrix (ECM) molecules decreases apoptosis markers and inhibiting the ROCK pathway blocks ECM stimulated actin cortical mat reformation and increases apoptosis in embryonic corneal epithelial cells

體內(nèi)研究(In Vivo)

Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group^[3]. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group)

分子量：247.34

Formula：C₁₄H₂₁N₃O

CAS 號：146986-50-7

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式：

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性數(shù)據(jù)

DMSO : 50 mg/mL (202.15 mM; Need ultrasonic)

H₂O : 1 mg/mL (4.04 mM; ultrasonic and warming and heat to 60°C)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	4.0430 mL	20.2151 mL	40.4302 mL
5 mM	0.8086 mL	4.0430 mL	8.0860 mL
10 mM	0.4043 mL	2.0215 mL	4.0430 mL

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.11 mM); Clear solution
4.

請依序添加每種溶劑： Saline
Solubility: 2 mg/mL (8.09 mM); Clear solution; Need ultrasonic and warming and heat to 60°C