SB216763

SB216763 是一种有效的,选择性GSK-3α抑制剂,IC50为34.3 nM;对GSK-3β具有同样的抑制作用。SB216763 可激活自噬。

SB216763 Chemical Structure

SB216763 Chemical Structure

CAS: 280744-09-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1351.27 现货
5mg 1218.72 现货
50mg 7122.58 现货
100mg 8763.3 现货
1g 20229.3 现货
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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
HepG2 Function assay 34 uM 12 hrs Inhibition of GSK3beta in human HepG2 cells assessed as decrease in ratio of phosphorylated GS/GS at 34 uM after 12 hrs by Western blot analysis 25467150
3T3L1 Function assay 34 uM 12 hrs Increase in glucose incorporation in mouse 3T3L1 cells at 34 uM after 12 hrs by glucose assay 25467150
HepG2 Function assay 34 uM 12 hrs Increase in glucose incorporation in human HepG2 cells at 34 uM after 12 hrs by glucose assay 25467150
ReNcell VM Antiproliferative assay 3 uM 72 hrs Antiproliferative activity against human ReNcell VM cells assessed as reduction of cell proliferation at 3 uM after 72 hrs 20708937
Sf9 Function assay 30 min Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting, IC50=0.03388μM SANGER
MIAPaCa2 Growth inhibition assay 72 hrs Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay, IC50=25μM 19338355
ST14A Function assay 6 hrs Inhibition of GSK-3-beta-mediated Wnt signaling in human ST14A cells assessed as increase in accumulation of beta-casein around nucleus after 6 hrs by microscopic analysis 20708937
human SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=22.0198 μM SANGER
human NCI-SNU-1 cell Growth inhibition assay Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=21.5558 μM SANGER
human BxPC-3 cell Growth inhibition assay Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=21.3554 μM SANGER
human BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=21.1879 μM SANGER
human U-266 cell Growth inhibition assay Inhibition of human U-266 cell growth in a cell viability assay, IC50=20.8797 μM SANGER
human A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay, IC50=19.4549 μM SANGER
human MKN45 cell Growth inhibition assay Inhibition of human MKN45 cell growth in a cell viability assay, IC50=18.4128 μM SANGER
human BHT-101 cell Growth inhibition assay Inhibition of human BHT-101 cell growth in a cell viability assay, IC50=17.6099 μM SANGER
human IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=17.2001 μM SANGER
human YH-13 cell Growth inhibition assay Inhibition of human YH-13 cell growth in a cell viability assay, IC50=16.6865 μM SANGER
human S-117 cell Growth inhibition assay Inhibition of human S-117 cell growth in a cell viability assay, IC50=16.4022 μM SANGER
human QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=15.6394 μM SANGER
human D-566MG cell Growth inhibition assay Inhibition of human D-566MG cell growth in a cell viability assay, IC50=13.9481 μM SANGER
human A2058 cell Growth inhibition assay Inhibition of human A2058 cell growth in a cell viability assay, IC50=13.469 μM SANGER
human LoVo cell Growth inhibition assay Inhibition of human LoVo cell growth in a cell viability assay, IC50=13.3771 μM SANGER
human NCI-H2009 cell Growth inhibition assay Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=13.2427 μM SANGER
human RPMI-7951 cell Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay. IC50=11.7864 μM SANGER
human NMC-G1 cell Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=11.7264 μM SANGER
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=11.6535 μM SANGER
human NB5 cell Growth inhibition assay Inhibition of human NB5 cell growth in a cell viability assay, IC50=11.2157 μM SANGER
human ALL-PO cell Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=10.3477 μM SANGER
human G-361 cell Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=10.1798 μM SANGER
human ESS-1 cell Growth inhibition assay Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=9.59872 μM SANGER
human SK-OV-3 cell Growth inhibition assay Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=9.1002 μM SANGER
human IST-SL1 cell Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=9.0204 μM SANGER
human NCI-H1993 cell Growth inhibition assay Inhibition of human NCI-H1993 cell growth in a cell viability assay, IC50=8.36534 μM SANGER
human RS4-11 cell Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=8.24141 μM SANGER
human HMV-II cell Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=7.67607 μM SANGER
human GAMG cell Growth inhibition assay Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.65409 μM SANGER
human LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=6.42874 μM SANGER
human BT-549 cell Growth inhibition assay Inhibition of human BT-549 cell growth in a cell viability assay, IC50=5.29376 μM SANGER
human MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=2.69685 μM SANGER
human K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability, IC50=1.53698 μM SANGER
human JAR cell Growth inhibition assay Inhibition of human JAR cell growth in a cell viability assay, IC50=1.21044 μM SANGER
human HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.85256 μM SANGER
human NCI-H1770 cell Growth inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay. IC50=0.29392 μM SANGER
human HDLM-2 cell Growth inhibition assay Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50=0.20984 μM SANGER
neural precursor cells Function assay Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 17417631
HEK293 Function assay Glycogen synthase activity of HEK293 cells, inhibition of GSK3-beta, EC50=0.2μM 12941331
HEK293 Function assay Effective concentration of compound against glycogen synthase kinase-3 in HEK293 cells, EC50=0.2μM 15149684
human VA-ES-BJ cell Growth inhibition assay Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50=22.5763 μM SANGER
human HuO-3N1 cell Growth inhibition assay Inhibition of human HuO-3N1 cell growth in a cell viability assay, IC50=22.6151 μM SANGER
human EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=22.6689 μM SANGER
human T98G cell Growth inhibition assay Inhibition of human T98G cell growth in a cell viability assay, IC50=23.3009 μM SANGER
human SW1783 cell Growth inhibition assay Inhibition of human SW1783 cell growth in a cell viability assay, IC50=23.5243 μM SANGER
human NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=23.8512 μM SANGER
human KOSC-2 cell Growth inhibition assay Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=24.1292 μM SANGER
human SW48 cell Growth inhibition assay Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6067 μM SANGER
human NCI-H28 cell Growth inhibition assay Inhibition of human NCI-H28 cell growth in a cell viability assay, IC50=25.2104 μM SANGER
human 5637 cell Growth inhibition assay Inhibition of human 5637 cell growth in a cell viability assay, IC50=25.8111 μM SANGER
human NB69 cell Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay, IC50=26.1764 μM SANGER
human HT-29 cell Growth inhibition assay Inhibition of human HT-29 cell growth in a cell viability assay, IC50=27.1752 μM SANGER
human PFSK-1 cell Growth inhibition assay Inhibition of human PFSK-1 cell growth in a cell viability assay, IC50=27.593 μM SANGER
human UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=27.743 μM SANGER
human D-423MG cell Growth inhibition assay Inhibition of human D-423MG cell growth in a cell viability assay, IC50=27.9106 μM SANGER
human NH-12 cell Growth inhibition assay Inhibition of human NH-12 cell growth in a cell viability assay, IC50=28.4059 μM SANGER
human DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=29.0474 μM SANGER
human LS-513 cell Growth inhibition assay Inhibition of human LS-513 cell growth in a cell viability assay, IC50=30.1334 μM SANGER
human NBsusSR cell Growth inhibition assay Inhibition of human NBsusSR cell growth in a cell viability assay, IC50=30.5678 μM SANGER
human BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=30.7649 μM SANGER
human A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=30.9784 μM SANGER
human LU-134-A cell Growth inhibition assay Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=31.0238 μM SANGER
human ES3 cell Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50=31.3376 μM SANGER
human NY cell Growth inhibition assay Inhibition of human NY cell growth in a cell viability assay, IC50=32.2965 μM SANGER
human NCI-H1975 cell Growth inhibition assay Inhibition of human NCI-H1975 cell growth in a cell viability assay, IC50=32.3582 μM SANGER
human A704 cell Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay, IC50=34.2059 μM SANGER
human SK-MEL-24 cell Growth inhibition assay Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=34.2523 μM SANGER
human SW1088 cell Growth inhibition assay Inhibition of human SW1088 cell growth in a cell viability assay, IC50=34.3452 μM SANGER
human SK-MEL-1 cell Growth inhibition assay Inhibition of human SK-MEL-1 cell growth in a cell viability, IC50=34.714 μM SANGER
human MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=36.1467 μM SANGER
human T47D cell Growth inhibition assay Inhibition of human T47D cell growth in a cell viability assay, IC50=37.1647 μM SANGER
human SW1710 cell Growth inhibition assay Inhibition of human SW1710 cell growth in a cell viability assay, IC50=37.3608 μM SANGER
human MKN7 cell Growth inhibition assay Inhibition of human MKN7 cell growth in a cell viability assay, IC50=38.0909 μM SANGER
human CAL-72 cell Growth inhibition assay Inhibition of human CAL-72 cell growth in a cell viability assay, IC50=38.1178 μM SANGER
human AGS cell Growth inhibition assay Inhibition of human AGS cell growth in a cell viability assay, IC50=38.2039 μM SANGER
human BE-13 cell Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=38.7783 μM SANGER
human Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=39.6964 μM SANGER
human CAL-27 cell Growth inhibition assay Inhibition of human CAL-27 cell growth in a cell viability assay, IC50=44.0054 μM SANGER
human BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=44.0278 μM SANGER
点击查看更多细胞系数据

生物活性

产品描述 SB216763 是一种有效的,选择性GSK-3α抑制剂,IC50为34.3 nM;对GSK-3β具有同样的抑制作用。SB216763 可激活自噬。
靶点
GSK-3α [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
34.3 nM ~34.3 nM
体外研究(In Vitro)
体外研究活性 除了抑制GSK-3α,SB 216763也同样有效作用于 GSK-3β,按10 μM 处理,抑制达96%, 作用于24 种其他蛋白激酶包括 PKBα 和PDK1时具有最小活性,IC50>10 μM。SB-216763作用于人肝脏细胞,刺激糖原合成,EC50为3.6 μM, 且作用于HEK293 细胞,诱导β-catenin-LEF/TCF相关报告基因的转录,这种作用存在剂量依赖性,按 5 μM处理,诱导达到最大值,增大2.5倍。[1]与剂量依赖性显著抑制GSK-3 活性一致,SB 216763 保护小脑颗粒神经元免受 LY-294002或钾丧失而诱导的细胞凋亡,这种作用具有浓度依赖性,3 μM 时保护神经达到最高值,与10 mM LiCl作用效果形成对比。3 μM SB 216763完全抑制 LY-294002诱导的 鸡背根神经节感觉神经元死亡。5 μM SB 216763 作用于HEK293细胞,显著抑制小脑颗粒神经元中GSK-3依赖的神经元特异性微管相关蛋白的磷酸化,且提高β-catenin细胞质水平,与Wnt调节的 GSK-3抑制效果差不多。[2] 25-50 μM SB 216763作用于前列腺癌细胞系,包括BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC, 降低细胞活力,这种作用存在剂量依赖性,且显著促进凋亡,处理72小时,凋亡达50%,而对HMEC或WI38细胞系没有作用效果。[3]
激酶实验 GSK-3 活性检测
在不同浓度SB 216763存在时,在含1 nM 人GSK-3α, 50 mM MOPS pH 7.0,0.2 mM EDTA, 10 mM Mg(Ac)2,7.5 mM β-巯基乙醇,5% (w/v)甘油,0.01% (w/v) Tween-20, 10% (v/v) DMSO, 及28 μM GS-2 肽底物的反应混合物中,测量GSK-3激酶活性。GS-2肽序列对应GSK-3使糖原合酶磷酸的地区。加入0.34 μCi [33P]γ-ATP开始实验。全部ATP浓度为 10 μM。实验在室温下进行30分钟后,加入含21 mM ATP的1/3实验体积为2.5%(v/v) H3PO4,终止反应。样本在P30磷酸纤维垫上展开,然后在0.5% (v/v) H3PO4中冲洗6次。过滤垫密封到Wallac betaplate闪烁液的样品袋中。在 Wallac microbeta闪烁计数器中计算测定33P 渗透到底物肽中的量。
细胞实验 细胞系 BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC
浓度 溶于DMSO, 终浓度为~50 μM
孵育时间 24, 48, 和72小时
方法 使用不同浓度SB 216763处理细胞 24,48和 72小时。通过MTS检测测量相对细胞活力。使用 Hoechst染色而测定凋亡细胞。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot c-Myb pGSK-3β / GSK-3β / E2F1 / β-catenin 21795403
Growth inhibition assay Cell viability 24779365
体内研究(In Vivo)
体内研究活性 SB 216763 按20 mg/kg 剂量处理患Bleomycin (BLM)诱导肺部炎症和纤维化的小鼠,通过显著抑制炎症细胞因子MCP-1和TNF-α的产量,显著抑制肺部炎症和纤维化,且显著提高BLM处理小鼠的寿命。SB 216763 处理,通过抑制肺泡上皮细胞损伤,而显著降低 BLM诱导的肺泡。[4]
动物实验 Animal Models 患Bleomycin (BLM)诱导的肺部炎症和纤维化的C57BL/6N小鼠
Dosages 20 mg/kg
Administration 静脉注射

化学信息&溶解度

分子量 371.22 分子式

C19H12N2O2Cl2

CAS号 280744-09-4 SDF Download SB216763 SDF
Smiles CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 23 mg/mL ( (61.95 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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