SB216763

目錄號：S1075 Purity: 99.98%

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

SB216763 Chemical Structure

CAS: 280744-09-4

規(guī)格	價格	庫存
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
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

SB216763相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	GSK-3α GSK-3β	點(diǎn)擊展開
相關(guān)產(chǎn)品	CHIR-99021 (Laduviglusib) Laduviglusib (CHIR-99021) Hydrochloride TWS119 CHIR-98014 BIO LY2090314 Tideglusib SB415286 AR-A014418 1-Azakenpaullone IM-12 CP21R7 TDZD-8 AZD2858 Indirubin?(NSC 105327) AZD1080 BIO-acetoxime Bikinin	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫凋亡分子化合物庫細(xì)胞周期化合物庫 NF-κB信號通路庫	點(diǎn)擊展開

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻(xiàn)信息(PMID)
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

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 時保護(hù)神經(jīng)達(dá)到最高值，與10 mM LiCl作用效果形成對比。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,凋亡達(dá)50%,而對HMEC或WI38細(xì)胞系沒有作用效果。^[3]
激酶實驗	GSK-3 活性檢測
激酶實驗	在不同濃度SB 216763存在時,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，測量GSK-3激酶活性。GS-2肽序列對應(yīng)GSK-3使糖原合酶磷酸的地區(qū)。加入0.34 μCi [³³P]γ-ATP開始實驗。全部ATP濃度為 10 μM。實驗在室溫下進(jìn)行30分鐘后，加入含21 mM ATP的1/3實驗體積為2.5%(v/v) H₃PO₄，終止反應(yīng)。樣本在P30磷酸纖維墊上展開，然后在0.5% (v/v) H₃PO₄中沖洗6次。過濾墊密封到Wallac betaplate閃爍液的樣品袋中。在 Wallac microbeta閃爍計數(shù)器中計算測定³³P 滲透到底物肽中的量。
細(xì)胞實驗	細(xì)胞系	BXPC-3, MIA-PaCa2, PANC1, ASPC1, 和CFPAC
	濃度	溶于DMSO, 終濃度為~50 μM
	孵育時間	24, 48, 和72小時
	方法	使用不同濃度SB 216763處理細(xì)胞 24,48和 72小時。通過MTS檢測測量相對細(xì)胞活力。使用 Hoechst染色而測定凋亡細(xì)胞。
實驗圖片	檢測方法	檢測指標(biāo)	實驗圖片	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]
動物實驗	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

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/11033082/ https://pubmed.ncbi.nlm.nih.gov/11279265/ https://pubmed.ncbi.nlm.nih.gov/15781615/ https://pubmed.ncbi.nlm.nih.gov/19959748/ + 展開

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/11033082/
https://pubmed.ncbi.nlm.nih.gov/11279265/
https://pubmed.ncbi.nlm.nih.gov/15781615/

https://pubmed.ncbi.nlm.nih.gov/19959748/

+ 展開

化學(xué)信息&溶解度

分子量	371.22	分子式	C₁₉H₁₂N₂O₂Cl₂
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 23 mg/mL ( (61.95 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 23 mg/mL ( (61.95 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解配方批次：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
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 Corn oil 該配方已經(jīng)過Selleck實驗室實測。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測試。	4.000mg/ml (10.78mM)	以 1 mL 工作液為例，取50μL80mg/ml的澄清DMSO儲備液加到950μL玉米油中，混合均勻。工作液請現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

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）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

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(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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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):