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SB525334

SB525334是一種有效的，選擇性TGFβ receptor I (ALK5)抑制劑，無細胞試驗中IC50為14.3 nM，作用于ALK4比作用于ALK5效果低4倍，對ALK2，3，和 6沒有活性。

SB525334 Chemical Structure

SB525334 Chemical Structure

CAS: 356559-20-1

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 647.01 現(xiàn)貨
5mg 580.89 現(xiàn)貨
10mg 991.14 現(xiàn)貨
100mg 7127.74 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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SB525334相關(guān)產(chǎn)品

相關(guān)信號通路圖

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
Sf9 Function assay Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells, IC50 = 0.162 μM. 20472445
ELT-3? Function Assay 0.5/1.0/2.0 μM 1 h inhibits TGF-β signaling in leiomyomas 17505012
AsPC1 Cell Viability Assay 0-10 μM 72 h efficiently reduces the viability with 22399597
PASMCs? Function Assay 1 μM 15 min inhibits TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50?of 295 nmol/L 19116361
rhPOSTN Apoptosis Assay 0.5?μM? 48?h significantly decreases the number of apoptotic cells 24129188
HUVECs Function Assay 10 μM 24/48/72 h leads to a disruption of the HUVEC monolayer after 72 hr 23968981
HUVECs Function Assay 10 μM 72 h blocks signaling 23968981
HUVECs Function Assay 10 μM 72 h reduces the phosphorylation of smad2 23968981
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
MiaPaCa2 Cell Viability Assay 0-10 μM 72 h efficiently reduces the viability with 22399597
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生物活性

產(chǎn)品描述 SB525334是一種有效的，選擇性TGFβ receptor I (ALK5)抑制劑，無細胞試驗中IC50為14.3 nM，作用于ALK4比作用于ALK5效果低4倍，對ALK2，3，和 6沒有活性。
特性 SB-525334有效選擇性抑制TGF-β1受體(ALK5)。
靶點
TGFβR1(ALK5) [1]
(Cell-free assay)
14.3 nM
體外研究(In Vitro)
體外研究活性

SB-525334對ALK2, 3,和6抑制效果不大, IC50 > 10 μM。SB-525334作用于腎臟近曲小管上皮細胞，抑制TGF-β1誘導(dǎo)的Smad2/3磷酸化和核轉(zhuǎn)位；1μM SB-525334作用于A498腎臟上皮癌細胞，抑制TGF-β1誘導(dǎo)的纖溶酶原激活物抑制劑-1(PAI-1)和原膠原α1(I) mRNA增多表達。[1]SB525334 (1 μM)作用于從攜帶遺傳式的特發(fā)性肺動脈高壓(PAH)的病人體內(nèi)獲得的肺動脈平滑肌細胞(PASMCs)，降低對TGF-β1的敏感性。[2]
激酶實驗 測定SB-525334有效性和選擇性的激酶實驗
為了測定SB-525334的有效性, 純化的GST標記的ALK5激酶域，純化的GST標記的全長Smad3,33P-γATP，及不同濃度SB-525334一起溫育。顯示讀數(shù)為放射性標記的Smad3。為了測定SB-525334的選擇性, 純化的GST標記的ALK2和ALK4激酶域，與GST標記的全長Smad1和Smad3分別溫育，加入不同濃度SB-525334，測定IC50 值。
細胞實驗 細胞系 人腎近曲小管上皮(RPTE)細胞
濃度 1 μM
孵育時間 1小時
方法

RPTE細胞接種在顯微鏡載玻片上。第二天，移除表皮生長因子和血清，細胞饑餓處理24小時。用10 ng/mL TGF-β1或1 μM SB-525334或兩者一起處理細胞。用SB-525334或饑餓培養(yǎng)基預(yù)處理3小時，然后和TGF-β1或饑餓培養(yǎng)基在37 oC下溫育1小時。細胞混合，通透處理。用BSA阻斷載玻片,和鼠Smad2/3抗體溫育，然后和鼠IgG熒光二抗溫育。用聚焦顯微鏡觀察載玻片，分析核信號強度。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot

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