SB505124
SB505124是一种选择性TGFβR抑制剂，作用于ALK4和ALK5，无细胞试验中IC50分别为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
产品质控
批次：
纯度：
99.99%
99.99
SB505124相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | SB505124是一种选择性TGFβR抑制剂，作用于ALK4和ALK5，无细胞试验中IC50分别为129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。 | ||||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | SB-505124抑制紧密相关的ALK4,IC50为129 nM，选择性比作用于 ALK5低2.5倍。SB-505124浓度高达10 μM时也不抑制ALK2。SB-505124 作用于COS-1细胞，也抑制内源性Smad2磷酸化。加入SB-505124不影响组成型活性 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人类肝癌细胞，C2C12小鼠成肌细胞和Mv1Lu水貂肺细胞，抑制TGF-β诱导的Smad2磷酸化，这种作用存在浓度依赖性。1 μM SB-505124也抑制活化素诱导的Smad2磷酸化。SB-505124有效抑制TGF-β和活化素诱导CAGA12-荧光素酶和ARE-荧光素酶受体结构的活力，这种作用存在浓度依赖性。[1] SB-505124可清除TGF-β1对E-钙粘蛋白启动子, mRNA和蛋白表达的抑制。[2] SB-505124 损害Smad2磷酸化和 CTGF与α-SMA的表达。 [3] |
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|---|---|---|---|---|
| 激酶实验 | 体外蛋白激酶实验 | |||
| 65 nM GST-ALK5和 184 nM GST-Smad3 在50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM 二硫苏糖醇, 和 3 μM ATP，在有或无SB-505124存在时进行激酶实验。反应和 0.5 μCi [33P]γATP在30oC下温育3小时。在 P-81 纸上收集磷酸化的蛋白, 使用0.5% 磷酸冲洗,然后在液体闪烁计数板上测量。另外, Smad3或Smad1蛋白覆盖到 FlashPlate Sterile Basic 微板上。然后在FlashPlates上，在相同实验环境下，使用ALK5激酶域， Smad3作为底物，或者ALK6(BMP 受体)激酶域，Smad1作为底物进行激酶实验。使用磷酸缓冲液冲洗实验板三次，然后在TopCount上计数。 | ||||
| 细胞实验 | 细胞系 | COS-1和HepG2细胞 | ||
| 浓度 | 0.01-5 μM | |||
| 孵育时间 | 30分钟 | |||
| 方法 | 使用修正的四唑盐WST-1测定细胞(如COS-1, HepG2 细胞系)活力。2×103个细胞接种在96孔板上，过夜。板中为无酚红培养基。用50 μL SB-505124 (获得指定终浓度) 处理细胞30分钟，然后使用TGF-β1和TNF-α处理，终体积为200 μL。每孔加入10 μL WST-1，在 37oC下温育3小时，然后在指定时间点测定细胞生长。使用酶联免疫吸附试验酶标仪直接测量代谢活跃的细胞裂解WST-1为水溶性的甲臜。每孔中的细胞系重复处理三次。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-SMAD2 / SMAD2 / Cleaved PARP / ZEB1 / Snail |
|
30401983 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | SB-505124处理青光眼滤过手术中的滤过泡，持续10天以上，没有任何严重的术后并发症，并清楚地观察到滤泡。第一周眼内压 (IOP)低于10 mmHg，然而 SB-505124处理一周后，眼内压涨到10 mmHg。[4] |
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|---|---|---|
| 动物实验 | Animal Models | 雄性Sprague-Dawley大鼠，体重300 g |
| Dosages | 1 μM | |
| Administration | 外用 | |
化学信息&溶解度
| 分子量 | 335.4 | 分子式 | C20H21N3O2 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 67 mg/mL ( (199.76 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 67 mg/mL (199.76 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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