SB-431542

SB-431542 是一種有效，選擇性的 ALK5/TGF-β type I Receptor 抑制劑，IC50 值為 94 nM。

貨號：HY-10431
CAS：301836-41-9

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-10431

起訂量：1

規(guī)格:：10mg

價格:：￥800

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產(chǎn)品詳情

SB-431542

SB-431542 是一種有效，選擇性的 ALK5/TGF-β type I Receptor 抑制劑，IC₅₀ 值為 94 nM。

生物活性

SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC₅₀ value of 94 nM^[1].

IC₅₀ & Target

ALK5

94 nM (IC₅₀)

體外研究(In Vitro)

SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC₅₀ values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC₅₀ values of 62 and 22 nM, respectively^[1]. SB-431542 (10 μM) is a selective inhibitor of TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells^[2]. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta^[3]. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells^[4].

體內(nèi)研究(In Vivo)

SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft^[5].

分子量：384.39

Formula：C₂₂H₁₆N₄O₃

CAS 號：301836-41-9

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

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (650.38 mM; Need ultrasonic)

Ethanol : 11.17 mg/mL (29.06 mM; Need ultrasonic and warming)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.6015 mL	13.0076 mL	26.0152 mL
5 mM	0.5203 mL	2.6015 mL	5.2030 mL
10 mM	0.2602 mL	1.3008 mL	2.6015 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(fù)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。-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(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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: ≥ 2.08 mg/mL (5.41 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

參考文獻

[1]. N. J. Laping, et al. Inhibition of Transforming Growth Factor (TGF)-β1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF-β Type I Receptor Kinase Activity: SB-431542.

[2]. Inman GJ, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol, 2002, 62(1), 65-74.

[3]. Halder SK, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia, 2005, 7(5), 509-521.

[4]. Matsuyama S, et al. SB-431542 inhibits transforming growth factor-beta-induced proliferation of human osteosarcoma cells. Cancer Res, 2003, 63(22), 7791-7798.

[5]. Sato M, et al. Differential Proteome Analysis Identifies TGF-β-Related Pro-Metastatic Proteins in a 4T1 Murine Breast Cancer Model. PLoS One. 2015 May 18;10(5):e0126483.

[6]. Ma J, et al. Growth differentiation factor 11 improves neurobehavioral recovery and stimulates angiogenesis in rats subjected to cerebral ischemia/reperfusion. Brain Res Bull. 2018 Feb 9;139:38-47

SB-431542

SB-431542 是一種有效，選擇性的 ALK5/TGF-β type I Receptor 抑制劑，IC50 值為 94 nM。

貨號：HY-10431
CAS：301836-41-9

品牌：MCE

型號：HY-10431

起訂量：1

規(guī)格:：10mg

價格:：￥800

15906629305

在線客服

客服一

產(chǎn)品詳情

SB-431542

SB-431542 是一種有效，選擇性的 ALK5/TGF-β type I Receptor 抑制劑，IC₅₀ 值為 94 nM。

生物活性

SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC₅₀ value of 94 nM^[1].

IC₅₀ & Target

ALK5

94 nM (IC₅₀)

體外研究(In Vitro)

SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC₅₀ values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC₅₀ values of 62 and 22 nM, respectively^[1]. SB-431542 (10 μM) is a selective inhibitor of TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells^[2]. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta^[3]. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells^[4].

體內(nèi)研究(In Vivo)

SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft^[5].

分子量：384.39

Formula：C₂₂H₁₆N₄O₃

CAS 號：301836-41-9

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

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

DMSO : 250 mg/mL (650.38 mM; Need ultrasonic)

Ethanol : 11.17 mg/mL (29.06 mM; Need ultrasonic and warming)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.6015 mL	13.0076 mL	26.0152 mL
5 mM	0.5203 mL	2.6015 mL	5.2030 mL
10 mM	0.2602 mL	1.3008 mL	2.6015 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(fù)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。-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(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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: ≥ 2.08 mg/mL (5.41 mM); Clear solution
2.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution