Home PI3K/Akt/mTOR GSK-3 inhibitor - Autophagy activator SB216763 For research use only.

SB216763

SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.

SB216763 Chemical Structure

SB216763 Chemical Structure

CAS No. 280744-09-4

Purity & Quality Control

SB216763 Related Products

Signaling Pathway

GSK-3 Signaling Pathways

GSK-3 Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
neural precursor cells Function assay Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 17417631
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
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
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 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
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
human HDLM-2 cell Growth inhibition assay Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50=0.20984 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 HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.85256 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 K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability, IC50=1.53698 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 BT-549 cell Growth inhibition assay Inhibition of human BT-549 cell growth in a cell viability assay, IC50=5.29376 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 GAMG cell Growth inhibition assay Inhibition of human GAMG cell growth in a cell viability assay, IC50=6.65409 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 RS4-11 cell Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=8.24141 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 IST-SL1 cell Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=9.0204 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 ESS-1 cell Growth inhibition assay Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=9.59872 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 ALL-PO cell Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=10.3477 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 DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=11.6535 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 RPMI-7951 cell Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay. IC50=11.7864 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 LoVo cell Growth inhibition assay Inhibition of human LoVo cell growth in a cell viability assay, IC50=13.3771 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 D-566MG cell Growth inhibition assay Inhibition of human D-566MG cell growth in a cell viability assay, IC50=13.9481 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 S-117 cell Growth inhibition assay Inhibition of human S-117 cell growth in a cell viability assay, IC50=16.4022 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 IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=17.2001 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 MKN45 cell Growth inhibition assay Inhibition of human MKN45 cell growth in a cell viability assay, IC50=18.4128 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 U-266 cell Growth inhibition assay Inhibition of human U-266 cell growth in a cell viability assay, IC50=20.8797 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 BxPC-3 cell Growth inhibition assay Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50=21.3554 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 SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=22.0198 μM SANGER
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
Click to View More Cell Line Experimental Data

Biological Activity

Description SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.
Targets
GSK-3α [1]
(Cell-free assay)		 GSK-3β [1]
(Cell-free assay)
34.3 nM ~34.3 nM
In vitro
In vitro SB 216763 displays similar potency for GSK-3β with 96% inhibition at 10 μM while exhibiting minimal activity against 24 other protein kinases including PKBα and PDK1 with IC50 of >10 μM. SB 216763 stimulates glycogen synthesis in human liver cells with EC50 of 3.6 μM, and induces dose-dependent transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells with a maximum 2.5-fold induction at 5 μM. [1] SB 216763 protects the cerebellar granule neurones from apoptotic cell death induced by LY-294002 or potassium-deprivation in a concentration-dependent manner, with a maximal neuroprotection at 3 μM in contrast with the effect of lithium chloride at which 10 mM is required. SB 216763 at 3 μM also completely prevents death of chicken dorsal root ganglion sensory neurones induced by LY-294002 regardless of NGF. SB 216763 treatment at 5 μM markedly inhibits the GSK-3-dependent phosphorylation of neuronal-specific microtubule-associated protein tau in cerebellar granule neurones or recombinant tau in HEK293 cells, and induces increased levels of cytoplasmic β-catenin in both cells mimicking the effect of Wnt-mediated inhibition of GSK-3. [2] In pancreatic cancer cell lines including BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC, SB 216763 treatment at 25-50 μM reduces cell viability in a dose-dependent manner, and leads to significant increase in apoptosis by 50% at 72 hours due to the specific down regulation of GSK-3β, while has no effect in HMEC or WI38 cell lines. [3]
Kinase Assay GSK-3 activity assay
GSK-3 kinase activity is measured, in the presence of various concentrations of SB 216763, in a reaction mixture containing final concentrations of 1 nM human GSK-3α, 50 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM Mg-acetate, 7.5 mM β-mercaptoethanol, 5% (w/v) glycerol, 0.01% (w/v) Tween-20, 10% (v/v) DMSO, and 28 μM GS-2 peptide substrate. The GS-2 peptide sequence corresponds to a region of glycogen synthase that is phosphorylated by GSK-3. The assay is initiated by the addition of 0.34 μCi [33P]γ-ATP. The total ATP concentration is 10 μM. Following 30 minutes incubation at room temperature the assay is stopped by the addition of one third assay volume of 2.5% (v/v) H3PO4 containing 21 mM ATP. Samples are spotted onto P30 phosphocellulose mats and washed six times in 0.5% (v/v) H3PO4. The filter mats are sealed into sample bags containing Wallac betaplate scintillation fluid. 33P incorporation into the substrate peptide is determined by counting the mats in a Wallac microbeta scintillation counter.
Cell Research Cell lines BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC cells
Concentrations Dissolved in DMSO, final concentrations ~50 μM
Incubation Time 24, 48, and 72 hours
Method Cells are exposed to various concentrations of SB 216763 for 24, 48 and 72 hours. Relative cell viability is measured using the MTS assay. Apoptotic cells are determined by staining with Hoechst.
Experimental Result Images Methods Biomarkers Images PMID
Western blot c-Myb pGSK-3β / GSK-3β / E2F1 / β-catenin 21795403
Growth inhibition assay Cell viability 24779365
In Vivo
In vivo Administration of SB 216763 at 20 mg/kg significantly prevents lung inflammation and the subsequent fibrosis in bleomycin (BLM)-induced pulmonary inflammation and fibrosis model in mice by significantly blocking the production of inflammatory cytokines MCP-1 and TNF-α by macrophages, and significantly improves the survival of BLM-treated mice. SB 216763 treatment causes a significant reduction in BLM-induced alveolitis by inhibiting alveolar epithelial cell damage. [4]
Animal Research Animal Models C57BL/6N mice with lung inflammation and fibrosis induced by bleomycin (BLM)
Dosages 20 mg/kg
Administration Intravenously

Chemical Information & Solubility

Molecular Weight 371.22 Formula

C19H12N2O2Cl2
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 23 mg/mL ( (61.95 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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