- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 新產(chǎn)品
- 聯(lián)系我們
SB525334
SB525334是一種有效的，選擇性TGFβ receptor I (ALK5)抑制劑，無細(xì)胞試驗(yàn)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
CAS: 356559-20-1
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
SB525334相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | ALK1 ALK2 ALK3 ALK4 TGFβRI/ALK5 ALK6 TGFβRII TGF-β Smad3 Smad4 Smad5 ALK7 | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | SB431542 LDN-193189 Galunisertib (LY2157299) LY2109761 LDN-193189 2HCl SIS3 HCl RepSox (E-616452) LY364947 DMH1 SB505124 GW788388 A-83-01 SD-208 K02288 Vactosertib (TEW-7197) SIS3 Kartogenin ITD-1 LDN-212854 LY 3200882 ML347 TP0427736 HCl SRI-011381 (C381) LDN-214117 Hesperetin Alantolactone TGFβRI-IN-3 Anti-human/mouse TGF-β-InVivo Phospho-Smad2 (S250) Rabbit Recombinant mAb | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 細(xì)胞周期化合物庫 TGF-beta/Smad信號通路庫 | 點(diǎn)擊展開 |
相關(guān)信號通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 |
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
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(xì)胞試驗(yàn)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(diǎn) |
|
| 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(xì)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(xì)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(dá)。[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(xì)胞(PASMCs)，降低對TGF-β1的敏感性。[2] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 測定SB-525334有效性和選擇性的激酶實(shí)驗(yàn) | |||
| 為了測定SB-525334的有效性, 純化的GST標(biāo)記的ALK5激酶域，純化的GST標(biāo)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(biāo)記的Smad3。為了測定SB-525334的選擇性, 純化的GST標(biāo)記的ALK2和ALK4激酶域，與GST標(biāo)記的全長Smad1和Smad3分別溫育，加入不同濃度SB-525334，測定IC50 值。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | 人腎近曲小管上皮(RPTE)細(xì)胞 | ||
| 濃度 | 1 μM | |||
| 孵育時(shí)間 | 1小時(shí) | |||
| 方法 | RPTE細(xì)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(xì)胞饑餓處理24小時(shí)。用10 ng/mL TGF-β1或1 μM SB-525334或兩者一起處理細(xì)胞。用SB-525334或饑餓培養(yǎng)基預(yù)處理3小時(shí)，然后和TGF-β1或饑餓培養(yǎng)基在37 oC下溫育1小時(shí)。細(xì)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(qiáng)度。 |
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| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot |
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