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SB216763

SB216763 是一種有效的，選擇性GSK-3α抑制劑，IC50為34.3 nM；對(duì)GSK-3β具有同樣的抑制作用。SB216763 可激活自噬。

SB216763 Chemical Structure

SB216763 Chemical Structure

CAS: 280744-09-4

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 1351.27 現(xiàn)貨
5mg 1218.72 現(xiàn)貨
50mg 7122.58 現(xiàn)貨
100mg 8763.3 現(xiàn)貨
1g 20229.3 現(xiàn)貨
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SB216763相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

GSK-3 Signaling Pathways

GSK-3信號(hào)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
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
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生物活性

產(chǎn)品描述 SB216763 是一種有效的，選擇性GSK-3α抑制劑，IC50為34.3 nM；對(duì)GSK-3β具有同樣的抑制作用。SB216763 可激活自噬。
靶點(diǎn)
GSK-3α [1]
(Cell-free assay)		 GSK-3β [1]
(Cell-free assay)
34.3 nM ~34.3 nM
體外研究(In Vitro)
體外研究活性 除了抑制GSK-3α,SB 216763也同樣有效作用于 GSK-3β，按10 μM 處理，抑制達(dá)96%， 作用于24 種其他蛋白激酶包括 PKBα 和PDK1時(shí)具有最小活性，IC50>10 μM。SB-216763作用于人肝臟細(xì)胞，刺激糖原合成，EC50為3.6 μM, 且作用于HEK293 細(xì)胞，誘導(dǎo)β-catenin-LEF/TCF相關(guān)報(bào)告基因的轉(zhuǎn)錄，這種作用存在劑量依賴性，按 5 μM處理，誘導(dǎo)達(dá)到最大值，增大2.5倍。[1]與劑量依賴性顯著抑制GSK-3 活性一致，SB 216763 保護(hù)小腦顆粒神經(jīng)元免受 LY-294002或鉀喪失而誘導(dǎo)的細(xì)胞凋亡，這種作用具有濃度依賴性，3 μM 時(shí)保護(hù)神經(jīng)達(dá)到最高值，與10 mM LiCl作用效果形成對(duì)比。3 μM SB 216763完全抑制 LY-294002誘導(dǎo)的 雞背根神經(jīng)節(jié)感覺(jué)神經(jīng)元死亡。5 μM SB 216763 作用于HEK293細(xì)胞，顯著抑制小腦顆粒神經(jīng)元中GSK-3依賴的神經(jīng)元特異性微管相關(guān)蛋白的磷酸化，且提高β-catenin細(xì)胞質(zhì)水平，與Wnt調(diào)節(jié)的 GSK-3抑制效果差不多。[2] 25-50 μM SB 216763作用于前列腺癌細(xì)胞系，包括BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC, 降低細(xì)胞活力，這種作用存在劑量依賴性，且顯著促進(jìn)凋亡，處理72小時(shí),凋亡達(dá)50%,而對(duì)HMEC或WI38細(xì)胞系沒(méi)有作用效果。[3]
激酶實(shí)驗(yàn) GSK-3 活性檢測(cè)
在不同濃度SB 216763存在時(shí),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-巰基乙醇,5% (w/v)甘油,0.01% (w/v) Tween-20, 10% (v/v) DMSO, 及28 μM GS-2 肽底物的反應(yīng)混合物中，測(cè)量GSK-3激酶活性。GS-2肽序列對(duì)應(yīng)GSK-3使糖原合酶磷酸的地區(qū)。加入0.34 μCi [33P]γ-ATP開(kāi)始實(shí)驗(yàn)。全部ATP濃度為 10 μM。實(shí)驗(yàn)在室溫下進(jìn)行30分鐘后，加入含21 mM ATP的1/3實(shí)驗(yàn)體積為2.5%(v/v) H3PO4，終止反應(yīng)。樣本在P30磷酸纖維墊上展開(kāi)，然后在0.5% (v/v) H3PO4中沖洗6次。過(guò)濾墊密封到Wallac betaplate閃爍液的樣品袋中。在 Wallac microbeta閃爍計(jì)數(shù)器中計(jì)算測(cè)定33P 滲透到底物肽中的量。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC
濃度 溶于DMSO, 終濃度為~50 μM
孵育時(shí)間 24, 48, 和72小時(shí)
方法 使用不同濃度SB 216763處理細(xì)胞 24,48和 72小時(shí)。通過(guò)MTS檢測(cè)測(cè)量相對(duì)細(xì)胞活力。使用 Hoechst染色而測(cè)定凋亡細(xì)胞。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot c-Myb pGSK-3β / GSK-3β / E2F1 / β-catenin 21795403
Growth inhibition assay Cell viability 24779365
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 SB 216763 按20 mg/kg 劑量處理患Bleomycin (BLM)誘導(dǎo)肺部炎癥和纖維化的小鼠，通過(guò)顯著抑制炎癥細(xì)胞因子MCP-1和TNF-α的產(chǎn)量，顯著抑制肺部炎癥和纖維化，且顯著提高BLM處理小鼠的壽命。SB 216763 處理，通過(guò)抑制肺泡上皮細(xì)胞損傷，而顯著降低 BLM誘導(dǎo)的肺泡。[4]
動(dòng)物實(shí)驗(yàn) Animal Models 患Bleomycin (BLM)誘導(dǎo)的肺部炎癥和纖維化的C57BL/6N小鼠
Dosages 20 mg/kg
Administration 靜脈注射

化學(xué)信息&溶解度

分子量 371.22 分子式

C19H12N2O2Cl2
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 23 mg/mL ( (61.95 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(jìn)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。

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