PROTAC TEAD1/IAP degrader-3
PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma.
(Pink: TEAD1 ligand (HY-181592); Blue: IAP ligand (HY-181591); Black: linker).
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- Fòrmula: C47H50F4N6O6
- Peso molecular:870.93
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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cIAP1 |
TEAD1 |
PROTAC TEAD1/IAP degrader-3 (A538) (0.0001-10 μM; 20 h) induces proteasome-dependent degradation of TEAD1 in NCI-H2052 cells, with a DC50 of 44 nM and a maximum degradation rate of 42%. The degradation depends on cIAP1 and XIAP, where XIAP contributes to achieving the maximum degradation efficacy, while cIAP1 helps enhance the activity of the degrader[1].
PROTAC TEAD1/IAP degrader-3 (0.001-10 μM; 20 h) induces partial degradation of TEAD1 in NCI-H226 cells, with a DC50 of 76 nM and a maximum degradation rate of 38%[1].
PROTAC TEAD1/IAP degrader-3 (0.0001-30 μM; 4 h) forms a stable ternary complex with cIAP1, XIAP and TEAD1 in NCI-H2052 cells[1].
PROTAC TEAD1/IAP degrader-3 (0.5 μM; 16 h) specifically downregulates TEAD1 at the proteome level in NCI-H2052 cells, with no significant effects on other TEAD paralogs[1].
PROTAC TEAD1/IAP degrader-3 (1 nM-10 μM; 144 h) inhibits the proliferation of ZL55, NCI-H2052 and NCI-H226 cell lines[1].
PROTAC TEAD1/IAP degrader-3 (0.001-10 μM; 48 h) modulates Hippo pathway activity in ZL55, NCI-H2052 and NCI-H226 cells via TEAD-dependent downregulation of CTGF gene expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H2052 cells (stably expressing HiBiT-TEAD1; wildtype)
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Concentration:0, 0.0001,0.001, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 M
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Incubation Time:20 h
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Result:Achieved 48% degradation of endogenous TEAD1 at 3 μM treatment.
Induced HiBiT-TEAD1 degradation with a Dmax of 49% and a DC50 of 293 nM.
Degraded endogenous TEAD1 with a Dmax of 42% and a DC50 of 44 nM.
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Cell Line:NCI-H226 cells
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Concentration:0.001-10 μM
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Incubation Time:20 h
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Result:Degraded endogenous TEAD1 with a Dmax of 38% and a DC50 of 76 nM.
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Cell Line:NCI-H2052 cells
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Concentration:3 μM; 5 μM (MG132)
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Incubation Time:16 h
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Result:Completely abolished TEAD1 degradation induced by 3 μM PROTAC TEAD1/IAP degrader-3 (A538), with near 100% recovery of TEAD1 levels, in the presence of MG132.
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Cell Line:NCI-H2052 wildtype, cIAP1 KO, XIAP KO, and cIAP1/XIAP DKO cell lines
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:20 h
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Result:Induced TEAD1 degradation in wildtype cells with a Dmax of 48% and a DC50 of 64 nM.
Reduced Dmax to 27% with a DC50 of 61 nM in XIAP KO cells.
Right-shifted DC50 to 340 nM with a Dmax of 44% in cIAP1 KO cells.
Achieved a Dmax of 28% with a DC50 of 220 nM in cIAP1/XIAP DKO cells.
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Cell Line:NCI-H2052 cells; NCI-H226 transgenic cell lines (stably expressing HiBiT-TEAD1-4)
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM (endogenous assay); 0.3 nM-10 μM (HiBiT assay)
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Incubation Time:20 h (endogenous assay); 18 h (HiBiT assay)
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Result:Degraded TEAD4 with a Dmax of 9% and a DC50 of 510 nM in NCI-H2052 cells, compared to TEAD1 Dmax of 42% and DC50 of 44 nM.
Induced degradation of TEAD1 with a Dmax of ~40%, TEAD2 with a Dmax of <5%, TEAD3 with a Dmax of 13%, and TEAD4 with a Dmax of <5% in NCI-H226 HiBiT assays.
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Cell Line:ZL55, NCI-H226, NCI-H2052 (mesothelioma cell lines); NCI-H520 (Hippo pathway-independent cell line)
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Concentration:1 nM-10 μM
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Incubation Time:144 h
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Result:Inhibited proliferation in ZL55 cells with an IC50 of 925 nM and an Emax of 100%.
Inhibited proliferation in NCI-H226 cells with an IC50 of 733 nM and an Emax of 100%.
Inhibited proliferation in NCI-H2052 cells with an IC50 of 1267 nM and an Emax of 99%.
Inhibited proliferation in NCI-H520 cells with an IC50 of 443 nM and an Emax of 96%.
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Cell Line:ZL55, NCI-H226, NCI-H2052 (mesothelioma cell lines)
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Concentration:0.001-10 μM
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Incubation Time:48 h
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Result:Inhibited CTGF expression in ZL55 cells with an IC50 >1000 nM.
Inhibited CTGF expression in NCI-H226 cells with an IC50 of 826 nM and an Emax of 99%.
Inhibited CTGF expression in NCI-H2052 cells with an IC50 of 875 nM and an Emax of 89%.
Chemical Information
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Peso molecular 870.93
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Fòrmula C47H50F4N6O6
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SMILES
O=C(C1=CC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2N=C1)NCC4=CC=CC(OCCOC5=CC=C(F)C(NC([C@H]6N(C([C@@H](NC([C@@H](NC)C)=O)C(C)(C)C)=O)CCC6)=O)=C5)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC TEAD1/IAP degrader-3 Related Classifications
HY-181590 Related Classifications
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