TEAD
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 | ||
| S1786 | Verteporfin (CL 318952) | <1 mg/mL | 100 mg/mL | '''''<1 mg/mL |
| S8951 | TED-347 | ˂1 mg/mL | 69 mg/mL | '25 mg/mL |
| S9735 | MGH-CP1 | <1 mg/mL | 74 mg/mL | ''''74 mg/mL |
| S8554 | Super-TDU | 100 mg/mL | -1 mg/mL | '-1 mg/mL |
| S8950 | MYF-01-37 | <1 mg/mL | 60 mg/mL | ''60 mg/mL |
| S8164 | YAP-TEAD Inhibitor 1 (Peptide 17) | 100 mg/mL | -1 mg/mL | '-1 mg/mL |
| S8661 | CA3 (CIL56) | <1 mg/mL | 97 mg/mL | '<1 mg/mL |
TEAD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 |
|---|---|---|---|
| S1786 |
Verteporfin (CL 318952)Verteporfin (CL 318952, Visudyne) is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis. |
Verteporfin treatment inhibits proliferation and induces apoptosis of Tsc1-null cells in vivo. Mice were administered i.p. with vehicle or verteporfin at a dose of 100 mg/kg every other day for 10 d before sacrifice. Mice were sacrificed at 6 wk of age. Three independent experiments were performed and mice in different treatments were pooled for analysis. Percentage of Ki67 and αSMA double-positive cells in α-SMA+ mesenchymal lesions in the indicated kidneys. Immunofluorescence staining and counting were performed on three sagittal sections from different kidney regions for each mouse.
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| S8951 |
TED-347TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM. |
||
| S9735 |
MGH-CP1MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation. MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively. |
||
| S8554 |
Super-TDUSuper-TDU is an inhibitory peptide targeting YAP-TEADs interaction. |
||
| S8950 |
MYF-01-37MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein. |
||
| S8164 |
YAP-TEAD Inhibitor 1 (Peptide 17)YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM. |
Hippo pathway inhibitors abrogate recombinant LMO3 protein induced HCC cell invasion and anoikis inhibiton. a and b Huh-7 and SNU-423 cells were treated with 50 nM rLMO3 protein, 50 nM rLMO3 protein plus 50 nM Verteporfin (the inhibitor of YAP-TEAD), 50 nM rLMO3 protein plus 50 nM Peptide 17 (the inhibitor of YAP-TEAD) respectively. The invaded Huh-7 (a) and SNU-423 (b) cells were analyzed after 48 h. Scale bars: 10 μm.
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| S8661 |
CA3 (CIL56)CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS). |
| 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 |
|---|---|---|---|
| S1786 |
Verteporfin (CL 318952)Verteporfin (CL 318952, Visudyne) is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis. |
Verteporfin treatment inhibits proliferation and induces apoptosis of Tsc1-null cells in vivo. Mice were administered i.p. with vehicle or verteporfin at a dose of 100 mg/kg every other day for 10 d before sacrifice. Mice were sacrificed at 6 wk of age. Three independent experiments were performed and mice in different treatments were pooled for analysis. Percentage of Ki67 and αSMA double-positive cells in α-SMA+ mesenchymal lesions in the indicated kidneys. Immunofluorescence staining and counting were performed on three sagittal sections from different kidney regions for each mouse.
|
|
| S8951 |
TED-347TED-347 is a potent, irreversible, covalent and allosteric inhibitor of the TEAD⋅Yap protein-protein interaction. TED-347 inhibits TEAD4⋅Yap1 protein-protein interaction with an apparent EC50 of 5.9 μM. |
||
| S9735 |
MGH-CP1MGH-CP1 is a potent and selective inhibitor of transcriptional enhanced associate domain (TEAD) palmitoylation. MGH-CP1 exhibits dose-dependent and potent inhibition of TEAD2/4 auto-palmitoylation in vitro with IC50 of 710 nM and 672 nM, respectively. |
||
| S8554 |
Super-TDUSuper-TDU is an inhibitory peptide targeting YAP-TEADs interaction. |
||
| S8950 |
MYF-01-37MYF-01-37 is a novel covalent inhibitor of TEAD targeting Cys380 when incubated with the TEAD2 protein. |
||
| S8164 |
YAP-TEAD Inhibitor 1 (Peptide 17)YAP-TEAD Inhibitor 1 (Peptide 17) is a YAP-TEAD protein-protein interaction inhibitor which has potential usage in treatment of YAP-involved cancers with IC50 of 25 nM. |
Hippo pathway inhibitors abrogate recombinant LMO3 protein induced HCC cell invasion and anoikis inhibiton. a and b Huh-7 and SNU-423 cells were treated with 50 nM rLMO3 protein, 50 nM rLMO3 protein plus 50 nM Verteporfin (the inhibitor of YAP-TEAD), 50 nM rLMO3 protein plus 50 nM Peptide 17 (the inhibitor of YAP-TEAD) respectively. The invaded Huh-7 (a) and SNU-423 (b) cells were analyzed after 48 h. Scale bars: 10 μm.
|
|
| S8661 |
CA3 (CIL56)CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS). |
