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) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1075 | SB216763 | <1 mg/mL | 23 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 |
| 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 |
| 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 |
亜型選択性的な製品
GSK-3製品
| 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 |
|---|---|---|---|
| S1075 |
SB216763SB216763 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. |
|
|
| S2745 |
CHIR-98014CHIR-98014 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. |
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 |
TWS119TWS119 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. |
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.
|
|
| S2823 |
TideglusibTideglusib 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. |
(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 |
SB415286SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. |
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 |
BIOBIO 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. |
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. |
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 |
AZD2858AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats. |
(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 |
AZD1080AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. |
||
| S7435 |
AR-A014418AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested. |
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-8TDZD-8 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. |
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 |
LY2090314LY2090314 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. |
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-12IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling. |
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-acetoximeBIO-acetoxime 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. |
Carnosic acid down-regulated SREBPs protein levels and inhibited transcriptional activity in presence of the GSK inhibitor BIO-acetoxime
|
|
| S2386 |
IndirubinIndirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM. |
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.
|
|
| S5439 |
5-Bromoindole5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3). |
||
| S8696 |
2-D082-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, 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. |
||
| S7722 |
BikininBikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling. |
||
| S7193 |
1-Azakenpaullone1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. |
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 |
| 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 |
|---|---|---|---|
| S1075 |
SB216763SB216763 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. |
|
|
| S2745 |
CHIR-98014CHIR-98014 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. |
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 |
TWS119TWS119 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. |
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.
|
|
| S2823 |
TideglusibTideglusib 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. |
(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 |
SB415286SB415286 is a potent GSK3α inhibitor with IC50/Ki of 78 nM/31 nM with equally effective inhibition of GSK-3β. |
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 |
BIOBIO 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. |
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. |
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 |
AZD2858AZD2858 is a selective GSK-3 inhibitor with an IC50 of 68 nM, activating Wnt signaling, increases bone mass in rats. |
(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 |
AZD1080AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. |
||
| S7435 |
AR-A014418AR-A014418 is an ATP-competitive, and selective GSK3β inhibitor with IC50 and Ki of 104 nM and 38 nM in cell-free assays, without significant inhibition on 26 other kinases tested. |
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-8TDZD-8 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. |
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 |
LY2090314LY2090314 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. |
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-12IM-12 is a selective GSK-3β inhibitor with IC50 of 53 nM, and also enhances canonical Wnt signalling. |
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-acetoximeBIO-acetoxime 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. |
Carnosic acid down-regulated SREBPs protein levels and inhibited transcriptional activity in presence of the GSK inhibitor BIO-acetoxime
|
|
| S2386 |
IndirubinIndirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM. |
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.
|
|
| S5439 |
5-Bromoindole5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3). |
||
| S8696 |
2-D082-D08 is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, 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. |
||
| S7722 |
BikininBikinin is an ATP-competitive Arabidopsis GSK-3 inhibitor, and acts as a strong activator of brassinosteroid (BR) signaling. |
||
| S7193 |
1-Azakenpaullone1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. |
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 |
