- 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)
- 蛋白實驗
- 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
- 細胞核與細胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 新產(chǎn)品
- 聯(lián)系我們
SB505124
SB505124是一種選擇性TGFβR抑制劑，作用于ALK4和ALK5，無細胞試驗中IC50分別為129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。
SB505124 Chemical Structure
CAS: 694433-59-5
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
SB505124相關產(chǎn)品
相關信號通路圖
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(PMID) |
|---|---|---|---|---|---|
| NMuMG | Function assay | 0.1 to 0.5 uM | 1 hr | Inhibition of ALK5 activity in mouse NMuMG cells assessed as TGFbeta-induced phosphorylation of Smad2 at 0.1 to 0.5 uM after 1 hr by Western blot analysis | 23047226 |
| HaCaT | Function assay | 24 hrs | Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=0.0438μM | 24786585 | |
| 4T1 | Function assay | 24 hrs | Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay, IC50=0.0766μM | 24786585 | |
| Sf9 | Function assay | Inhibition of GST-fused recombinant human ALK5 expressed in baculovirus-infected insect Sf9 cells using casein as substrate by radioisotope-based assay, IC50=0.054μM | 24704197 | ||
| Sf9 | Function assay | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells, IC50=0.054μM | 21435890 | ||
| Sf9 | Function assay | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay, IC50=0.0349μM | 26483198 | ||
| Sf9 | Function assay | Inhibition of human recombinant ALK5 expressed in insect Sf9 cells using casein as substrate by radioisotopic assay, IC50=0.054μM | 24786585 | ||
| Sf9 | Function assay | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells using casein as a substrate by radioisotopic protein kinase assay, IC50=0.0544μM | 23047226 | ||
| Sf9 | Function assay | Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 cells, IC50=0.169μM | 20472445 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 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 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| 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 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | SB505124是一種選擇性TGFβR抑制劑，作用于ALK4和ALK5，無細胞試驗中IC50分別為129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。 | ||||
|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | SB-505124抑制緊密相關的ALK4,IC50為129 nM，選擇性比作用于 ALK5低2.5倍。SB-505124濃度高達10 μM時也不抑制ALK2。SB-505124 作用于COS-1細胞，也抑制內(nèi)源性Smad2磷酸化。加入SB-505124不影響組成型活性 ALK1, ALK2, ALK3, 和 ALK6 磷酸化的Smad1。ALK4和ALK5 激活Smad1和Smad2，加入SB-505124抑制激活。SB-505124作用于HepG2人類肝癌細胞，C2C12小鼠成肌細胞和Mv1Lu水貂肺細胞，抑制TGF-β誘導的Smad2磷酸化，這種作用存在濃度依賴性。1 μM SB-505124也抑制活化素誘導的Smad2磷酸化。SB-505124有效抑制TGF-β和活化素誘導CAGA12-熒光素酶和ARE-熒光素酶受體結(jié)構的活力，這種作用存在濃度依賴性。[1] SB-505124可清除TGF-β1對E-鈣粘蛋白啟動子, mRNA和蛋白表達的抑制。[2] SB-505124 損害Smad2磷酸化和 CTGF與α-SMA的表達。 [3] |
|||
|---|---|---|---|---|
| 激酶實驗 | 體外蛋白激酶實驗 | |||
| 65 nM GST-ALK5和 184 nM GST-Smad3 在50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM 二硫蘇糖醇, 和 3 μM ATP，在有或無SB-505124存在時進行激酶實驗。反應和 0.5 μCi [33P]γATP在30oC下溫育3小時。在 P-81 紙上收集磷酸化的蛋白, 使用0.5% 磷酸沖洗,然后在液體閃爍計數(shù)板上測量。另外, Smad3或Smad1蛋白覆蓋到 FlashPlate Sterile Basic 微板上。然后在FlashPlates上，在相同實驗環(huán)境下，使用ALK5激酶域， Smad3作為底物，或者ALK6(BMP 受體)激酶域，Smad1作為底物進行激酶實驗。使用磷酸緩沖液沖洗實驗板三次，然后在TopCount上計數(shù)。 | ||||
| 細胞實驗 | 細胞系 | COS-1和HepG2細胞 | ||
| 濃度 | 0.01-5 μM | |||
| 孵育時間 | 30分鐘 | |||
| 方法 | 使用修正的四唑鹽WST-1測定細胞(如COS-1, HepG2 細胞系)活力。2×103個細胞接種在96孔板上，過夜。板中為無酚紅培養(yǎng)基。用50 μL SB-505124 (獲得指定終濃度) 處理細胞30分鐘，然后使用TGF-β1和TNF-α處理，終體積為200 μL。每孔加入10 μL WST-1，在 37oC下溫育3小時，然后在指定時間點測定細胞生長。使用酶聯(lián)免疫吸附試驗酶標儀直接測量代謝活躍的細胞裂解WST-1為水溶性的甲臜。每孔中的細胞系重復處理三次。 |
|||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-SMAD2 / SMAD2 / Cleaved PARP / ZEB1 / Snail |
|
30401983 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | SB-505124處理青光眼濾過手術中的濾過泡，持續(xù)10天以上，沒有任何嚴重的術后并發(fā)癥，并清楚地觀察到濾泡。第一周眼內(nèi)壓 (IOP)低于10 mmHg，然而 SB-505124處理一周后，眼內(nèi)壓漲到10 mmHg。[4] |
|
|---|---|---|
| 動物實驗 | Animal Models | 雄性Sprague-Dawley大鼠，體重300 g |
| Dosages | 1 μM | |
| Administration | 外用 | |
|
化學信息&溶解度
| 分子量 | 335.4 | 分子式 | C20H21N3O2 |
| CAS號 | 694433-59-5 | SDF | Download SB505124 SDF |
| Smiles | CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 67 mg/mL ( (199.76 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 67 mg/mL (199.76 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
技術支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術支持郵箱[email protected]，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
