GSK-3

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S2924	CHIR-99021 (CT99021) HCl	<1 mg/mL	93 mg/mL	2 mg/mL
S1075	SB216763	<1 mg/mL	23 mg/mL	<1 mg/mL
S1524	AT7519	<1 mg/mL	10 mg/mL	<1 mg/mL
S2745	CHIR-98014	<1 mg/mL	8 mg/mL	<1 mg/mL
S1590	TWS119	<1 mg/mL	64 mg/mL	<1 mg/mL
S9602	9-ing-41	<1 mg/mL	81 mg/mL	<1 mg/mL
S0765	MAZ51	<1 mg/mL	15 mg/mL	<1 mg/mL
S0354	Alsterpaullone			' mg/mL
S2823	Tideglusib	<1 mg/mL	8 mg/mL	<1 mg/mL
S2729	SB415286	<1 mg/mL	72 mg/mL	72 mg/mL
S7198	BIO	<1 mg/mL	71 mg/mL	'6 mg/mL
S1263	CHIR-99021 (CT99021)	<1 mg/mL	10 mg/mL	<1 mg/mL
S7253	AZD2858	<1 mg/mL	7 mg/mL	<1 mg/mL
S7145	AZD1080	<1 mg/mL	52 mg/mL	<1 mg/mL
S7435	AR-A014418	<1 mg/mL	61 mg/mL	'<1 mg/mL
S2926	TDZD-8	<1 mg/mL	44.5 mg/mL	44.5 mg/mL
S7063	LY2090314	<1 mg/mL	100 mg/mL	2 mg/mL
S7566	IM-12	<1 mg/mL	75 mg/mL	10 mg/mL
S7915	BIO-acetoxime	<1 mg/mL	19 mg/mL	<1 mg/mL
S2386	Indirubin	<1 mg/mL	53 mg/mL	<1 mg/mL
S7954	CP21R7 (CP21)	<1 mg/mL	63 mg/mL	1 mg/mL
S5439	5-Bromoindole	-1 mg/mL	39 mg/mL	-1 mg/mL
S8696	2-D08	<1 mg/mL	54 mg/mL	'<1 mg/mL
S7722	Bikinin	<1 mg/mL	54 mg/mL	<1 mg/mL
S7193	1-Azakenpaullone	<1 mg/mL	66 mg/mL	'<1 mg/mL
S3238	Resibufogenin	-1 mg/mL	100 mg/mL	-1 mg/mL

亜型選択性的な製品

GSK-3製品

All (26) GSK-3阻害剤(25) GSK-3活性剤(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2924	CHIR-99021 (CT99021) HCl CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.	Nat Genet, 2021, 53(4):467-476 Sci Adv, 2021, 7(12)eabf7412 Sci Adv, 2021, 7(7)eabd7605	Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.
S1075	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.	J Clin Invest, 2021, 131(6)136098 Cancers (Basel), 2021, 13(6)1205 Neoplasia, 2021, 23(3):304-325
S1524	AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.	Cell Death Dis, 2020, 11(9):754 Exp Mol Med, 2020, 10.1038/s12276-020-00537-z Biomolecules, 2020, 10(2)	Lysates of MDM treated with five-fold dilutions of the indicated compounds (starting concentration: AT7519, 0.5 mmol/l, roscovitine 4 mmol/l) were subjected to SDS-PAGE, transferred, and immunoblotted with antiphopho-SAMHD1, anti-SAMHD1 and anti-Hsp90 antibodies. MDM, monocyte-derived macrophage; SAMHD1, sterile a motif and HD domain-containing protein-1; SD, standard deviation.
S2745	CHIR-98014 CHIR-98014 (CT98014) is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.	Genomics, 2021, 113(3):1057-1069 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Differentiation of hESCs along the vascular. (B) FACS analysis showing the percentage of cells expressing CD34, PDGFRa, and KDR after 4 days of differentiation using our differentiation protocol in H9 hESC line. Similarly, an analysis was provided for the H1 hESC line using the same protocol but with CHIR98014 as the GSKi.
S1590	TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggers autophagy.	Signal Transduct Target Ther, 2021, 6(1):71 Cells, 2020, 9(7):E1607 Front Immunol, 2020, 11:607543	Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
S9602^新	9-ing-41 9-ING-41 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with antitumor activity. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β.
S0765^新	MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
S0354	Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S2823	Tideglusib Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.	J Virol, 2021, JVI.02393-20 Adv Biol Regul, 2021, S2212-4926(20)30091-9 Mol Cell, 2020, 80(6):1104-1122.e9	(A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs.
S2729	SB415286 SB415286 is a potent GSK3α inhibitor with IC50/K_i of 78 nM/31 nM with equally effective inhibition of GSK-3β. SB415286 causes MM cell growth arrest and apoptosis.	Int J Biol Macromol, 2021, 180:97-111 Toxicol Lett, 2021, 341:68-79 Mol Cell, 2020, 80(6):1104-1122.e9	LGX818 downregulates CyclinD1 dependent of DYRK1B, but not GSK3β. (B) A375 cells were treated with vehicle or an inhibitor of GSK3β (SB415286, 12.5 μM), then they were treated the same as in (A) for 3 and 12 h, IB analysis for β-catenin, Cyclin D1 and GAPDH.
S7198	BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.	Cell Stem Cell, 2020, S1934-5909(20)30541-5 Stem Cells, 2020, 10.1002/stem.3274 Front Immunol, 2020, 27;11:438	Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
S1263	CHIR-99021 (CT99021) CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.	Nat Genet, 2021, 53(4):467-476 Cancer Cell, 2021, 39(3):407-422.e13 Mol Cell, 2021, S1097-2765(20)30989-8	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
S7253	AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.	Carcinogenesis, 2020, 41(7):993-1004 Elife, 2019, 10.7554/eLife.42274 Environ Mol Mutagen, 2019, 60(6):513-533	(C) Macrophages were incubated with cAMP, oxLDL–PON1 alone or in the presence of LXRa inhibitor (SR9243 1 μM), PPARc inhibitor (T0070907, 1 μM), NEM (10 μM), or oxLDL. Data are expressed as means±SEM. P < 0.01, P < 0.0005, ***P < 0.0001.
S7145	AZD1080 AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with K_i of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.	Oncogene, 2020, 39(20):4132-4154 Carcinogenesis, 2020, 41(7):993-1004 Int J Mol Sci, 2020, 21(18)E6826
S7435	AR-A014418 AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and K_i of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.	J Clin Invest, 2020, 130(8):4301-4319 J Neuroinflammation, 2020, 22;17(1):125 Aging (Albany NY), 2020, 12(1):8-34	Protein levels of p-GSK3α/β (Tyr279/Tyr216, Ser21/Ser9) and total GSK3α/β in A549 cells with Lithium chloride, SB216763, TWS119 or ARA014418 treatment were assessed by immunoblotting
S2926	TDZD-8 TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.	Sci Transl Med, 2020, 12(554):eaba3613 FASEB J, 2018, 32(7):3924-3935 Nat Commun, 2017, 1;8(1):1232	The impact of GSK3β inhibitor TDZD-8 (10 μM) on the GSK3β phosphorylation (A), the protein expression (B) and mRNA level (C) of α-SMA and collagen I in acetaldehyde-induced HSCs activation. The data were representative of at least three independent experiments. All values were expressed as mean ± SD. P < 0.01, **P < 0.01 vs. the control group, #P < 0.05, ##P < 0.01, ###P < 0.01 vs. the acetaldehyde group.
S7063	LY2090314 LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.	Cell, 2021, 184(1):243-256.e18 Cell Death Differ, 2020, 7 Oncogene, 2020, 39(20):4132-4154	Western blot of β-catenin, and p62 in FS5 and FS4 melanoma cells upon treatment with the GSK3 inhibitor (LY2090314)) for the indicated doses for 8 hours; loading control: HSP90.
S7566	IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.	Proc Natl Acad Sci U S A, 2020, 117(44):27435-27444 Carcinogenesis, 2020, 41(7):993-1004 Anat Rec (Hoboken), 2020, 303(9):2344-2356	Inhibition of GSK-3β promotes Runx2 induction. Vascularsmoothmusclecells(VSMCs) were treated with or without IM-12(3 μM) for 24h, and cells treated with β-GP (10 mM) were as a positive control. The cell lysates were immunoblotted with antibodies against Runx2 and β-actin, respectively.
S7915	BIO-acetoxime BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.	Cancer Cell, 2017, 32(6):748-760 J Funct Foods, 2017, 10.1016/j.jff.2017.01.040 Sci Rep, 2016, 6:21549	Carnosic acid down-regulated SREBPs protein levels and inhibited transcriptional activity in presence of the GSK inhibitor BIO-acetoxime
S2386	Indirubin Indirubin (NSC 105327) is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.	Carcinogenesis, 2020, 41(7):993-1004 J Med Virol, 2019, 91(8):1440-1447 Int J Mol Sci, 2018, 19(6)	Effect of indirubin on the alterations of actin cytoskeleton in TNF-α-treated RA FLS. F-actin (red) and nucleus (blue) were stained with phalloidin and DAPI, respectively.
S7954	CP21R7 (CP21) CP21R7 (CP21) is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.	Sci Adv, 2020, 6(30):eaba7606 Front Cell Dev Biol, 2020, 15;8:309 Cancer Manag Res, 2020, 12:11773-11782
S5439	5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
S8696	2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.	Cell Res, 2020, 10.1038/s41422-020-00443-z Cell Death Differ, 2020, 10.1038/s41418-020-00641-7
S7722	Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
S7193	1-Azakenpaullone 1-Azakenpaullone (1-Akp) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.	Cancer Lett, 2020, 1;481:1-14 Carcinogenesis, 2020, 41(7):993-1004 Front Oncol, 2020, 10:565225	Wnt activation stimulates proliferation in irradiated neuromasts. Radiated larvae were treated with 2.5 μM Az at 48 h after IR for 2 days. Representative images of YO-PRO1 staining for HCs in radiated neuromasts in larvae treated with DMSO (a) and Az (b). c Two days after 30 Gy IR, larvae treated with 2.5 μM Az for 2 days. Two-tailed t test analysis of the number of HCs in neuromasts revealed a significant increase in Az-treated larvae compared to those treated with DMSO during the two incubation days (eight fish per group; N = 3, two-tailed t test, p < 0.01, p < 0.001). d-e Representative images of BrdU staining for proliferation in radiated neuromasts in larvae treated with DMSO (d) and Az (e). Neuromasts were counterstained by SYTOX. f Two-tailed t test analysis of the number of BrdU+ cells in neuromasts revealed a significantly increase in Az-treated larvae compared to those treated with DMSO during the three incubation days (n = 8 fish per group; N = 3, two-tailed t test, p < 0.05, p < 0.01, *p < 0.001). Scale bar 10 μm
S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S2924	CHIR-99021 (CT99021) HCl CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of the Wnt/beta-catenin signaling pathway. CHIR-99021 significantly rescues light-induced autophagy and augments GR, RORα and autophagy-related proteins.	Nat Genet, 2021, 53(4):467-476 Sci Adv, 2021, 7(12)eabf7412 Sci Adv, 2021, 7(7)eabd7605	Inhibition of GSK3 activity induces an autophagic response in human pancreatic cancer cells. PANC1 cells were treated for 24 h with DMSO, CHIR99021 (CHIR; 5 uM) or the mTOR inhibitor Torin1 (250 nM). Autophagosome (punctate LC3B) (D) and lysosome (E) labeling was visualized with a Zeiss LSM700 confocal microscope. Images were acquired with a 20x (D) or 63x (E) objective. Nuclei were stained with DAPI. Scale bars, 20 祄.
S1075	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.	J Clin Invest, 2021, 131(6)136098 Cancers (Basel), 2021, 13(6)1205 Neoplasia, 2021, 23(3):304-325
S1524	AT7519 AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.	Cell Death Dis, 2020, 11(9):754 Exp Mol Med, 2020, 10.1038/s12276-020-00537-z Biomolecules, 2020, 10(2)	Lysates of MDM treated with five-fold dilutions of the indicated compounds (starting concentration: AT7519, 0.5 mmol/l, roscovitine 4 mmol/l) were subjected to SDS-PAGE, transferred, and immunoblotted with antiphopho-SAMHD1, anti-SAMHD1 and anti-Hsp90 antibodies. MDM, monocyte-derived macrophage; SAMHD1, sterile a motif and HD domain-containing protein-1; SD, standard deviation.
S2745	CHIR-98014 CHIR-98014 (CT98014) is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.	Genomics, 2021, 113(3):1057-1069 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Differentiation of hESCs along the vascular. (B) FACS analysis showing the percentage of cells expressing CD34, PDGFRa, and KDR after 4 days of differentiation using our differentiation protocol in H9 hESC line. Similarly, an analysis was provided for the H1 hESC line using the same protocol but with CHIR98014 as the GSKi.
S1590	TWS119 TWS119 is a GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; capable of inducing neuronal differentiation and may be useful to stem cell biology. GSK-3β inhibition triggers autophagy.	Signal Transduct Target Ther, 2021, 6(1):71 Cells, 2020, 9(7):E1607 Front Immunol, 2020, 11:607543	Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
S9602^新	9-ing-41 9-ING-41 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with antitumor activity. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK3β.
S0765^新	MAZ51 MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines.
S0354	Alsterpaullone Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S2823	Tideglusib Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.	J Virol, 2021, JVI.02393-20 Adv Biol Regul, 2021, S2212-4926(20)30091-9 Mol Cell, 2020, 80(6):1104-1122.e9	(A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs.
S2729	SB415286 SB415286 is a potent GSK3α inhibitor with IC50/K_i of 78 nM/31 nM with equally effective inhibition of GSK-3β. SB415286 causes MM cell growth arrest and apoptosis.	Int J Biol Macromol, 2021, 180:97-111 Toxicol Lett, 2021, 341:68-79 Mol Cell, 2020, 80(6):1104-1122.e9	LGX818 downregulates CyclinD1 dependent of DYRK1B, but not GSK3β. (B) A375 cells were treated with vehicle or an inhibitor of GSK3β (SB415286, 12.5 μM), then they were treated the same as in (A) for 3 and 12 h, IB analysis for β-catenin, Cyclin D1 and GAPDH.
S7198	BIO BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.	Cell Stem Cell, 2020, S1934-5909(20)30541-5 Stem Cells, 2020, 10.1002/stem.3274 Front Immunol, 2020, 27;11:438	Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.
S1263	CHIR-99021 (CT99021) CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs. CHIR99021 functions as a Wnt/β-catenin activator and induces autophagy.	Nat Genet, 2021, 53(4):467-476 Cancer Cell, 2021, 39(3):407-422.e13 Mol Cell, 2021, S1097-2765(20)30989-8	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CHIR-99021 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.
S7253	AZD2858 AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats.	Carcinogenesis, 2020, 41(7):993-1004 Elife, 2019, 10.7554/eLife.42274 Environ Mol Mutagen, 2019, 60(6):513-533	(C) Macrophages were incubated with cAMP, oxLDL–PON1 alone or in the presence of LXRa inhibitor (SR9243 1 μM), PPARc inhibitor (T0070907, 1 μM), NEM (10 μM), or oxLDL. Data are expressed as means±SEM. P < 0.01, P < 0.0005, ***P < 0.0001.
S7145	AZD1080 AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with K_i of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.	Oncogene, 2020, 39(20):4132-4154 Carcinogenesis, 2020, 41(7):993-1004 Int J Mol Sci, 2020, 21(18)E6826
S7435	AR-A014418 AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and K_i of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested.	J Clin Invest, 2020, 130(8):4301-4319 J Neuroinflammation, 2020, 22;17(1):125 Aging (Albany NY), 2020, 12(1):8-34	Protein levels of p-GSK3α/β (Tyr279/Tyr216, Ser21/Ser9) and total GSK3α/β in A549 cells with Lithium chloride, SB216763, TWS119 or ARA014418 treatment were assessed by immunoblotting
S2926	TDZD-8 TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.	Sci Transl Med, 2020, 12(554):eaba3613 FASEB J, 2018, 32(7):3924-3935 Nat Commun, 2017, 1;8(1):1232	The impact of GSK3β inhibitor TDZD-8 (10 μM) on the GSK3β phosphorylation (A), the protein expression (B) and mRNA level (C) of α-SMA and collagen I in acetaldehyde-induced HSCs activation. The data were representative of at least three independent experiments. All values were expressed as mean ± SD. P < 0.01, **P < 0.01 vs. the control group, #P < 0.05, ##P < 0.01, ###P < 0.01 vs. the acetaldehyde group.
S7063	LY2090314 LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 is highly selective towards GSK3 as demonstrated by its fold selectivity relative to a large panel of kinases.	Cell, 2021, 184(1):243-256.e18 Cell Death Differ, 2020, 7 Oncogene, 2020, 39(20):4132-4154	Western blot of β-catenin, and p62 in FS5 and FS4 melanoma cells upon treatment with the GSK3 inhibitor (LY2090314)) for the indicated doses for 8 hours; loading control: HSP90.
S7566	IM-12 IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling.	Proc Natl Acad Sci U S A, 2020, 117(44):27435-27444 Carcinogenesis, 2020, 41(7):993-1004 Anat Rec (Hoboken), 2020, 303(9):2344-2356	Inhibition of GSK-3β promotes Runx2 induction. Vascularsmoothmusclecells(VSMCs) were treated with or without IM-12(3 μM) for 24h, and cells treated with β-GP (10 mM) were as a positive control. The cell lysates were immunoblotted with antibodies against Runx2 and β-actin, respectively.
S7915	BIO-acetoxime BIO-acetoxime (GSK-3 Inhibitor X) is a potent dual GSK3α/β inhibitor with IC50 of 10 nM, >240-fold selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B.	Cancer Cell, 2017, 32(6):748-760 J Funct Foods, 2017, 10.1016/j.jff.2017.01.040 Sci Rep, 2016, 6:21549	Carnosic acid down-regulated SREBPs protein levels and inhibited transcriptional activity in presence of the GSK inhibitor BIO-acetoxime
S2386	Indirubin Indirubin (NSC 105327) is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.	Carcinogenesis, 2020, 41(7):993-1004 J Med Virol, 2019, 91(8):1440-1447 Int J Mol Sci, 2018, 19(6)	Effect of indirubin on the alterations of actin cytoskeleton in TNF-α-treated RA FLS. F-actin (red) and nucleus (blue) were stained with phalloidin and DAPI, respectively.
S7954	CP21R7 (CP21) CP21R7 (CP21) is a potent and selective GSK-3β inhibitor that can potently activate canonical Wnt signalling.	Sci Adv, 2020, 6(30):eaba7606 Front Cell Dev Biol, 2020, 15;8:309 Cancer Manag Res, 2020, 12:11773-11782
S5439	5-Bromoindole 5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
S8696	2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.	Cell Res, 2020, 10.1038/s41422-020-00443-z Cell Death Differ, 2020, 10.1038/s41418-020-00641-7
S7722	Bikinin Bikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling.
S7193	1-Azakenpaullone 1-Azakenpaullone (1-Akp) is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25.	Cancer Lett, 2020, 1;481:1-14 Carcinogenesis, 2020, 41(7):993-1004 Front Oncol, 2020, 10:565225	Wnt activation stimulates proliferation in irradiated neuromasts. Radiated larvae were treated with 2.5 μM Az at 48 h after IR for 2 days. Representative images of YO-PRO1 staining for HCs in radiated neuromasts in larvae treated with DMSO (a) and Az (b). c Two days after 30 Gy IR, larvae treated with 2.5 μM Az for 2 days. Two-tailed t test analysis of the number of HCs in neuromasts revealed a significant increase in Az-treated larvae compared to those treated with DMSO during the two incubation days (eight fish per group; N = 3, two-tailed t test, p < 0.01, p < 0.001). d-e Representative images of BrdU staining for proliferation in radiated neuromasts in larvae treated with DMSO (d) and Az (e). Neuromasts were counterstained by SYTOX. f Two-tailed t test analysis of the number of BrdU+ cells in neuromasts revealed a significantly increase in Az-treated larvae compared to those treated with DMSO during the three incubation days (n = 8 fish per group; N = 3, two-tailed t test, p < 0.05, p < 0.01, *p < 0.001). Scale bar 10 μm

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S3238^新	Resibufogenin Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.

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S3238^新

Resibufogenin

Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.