PROTAC TEAD1/IAP degrader-1
PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma.
(Pink: TEAD1 and cIAP-1 ligand (HY-181536); Blue: IAP ligand (HY-181530); Black: linker (HY-141371)).
For research use only. We do not sell to patients.
- Formula: C46H45F3N8O7S
- Molecular Weight:910.96
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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cIAP1 270 nM (DC50) |
TEAD1 14 nM (DC50) |
Treatment of NCI-H2052 cells with PROTAC TEAD1/IAP degrader-1 for 20 h induces up to 55% degradation of HiBiT-TEAD1, with a DC50 of 196 nM[1].
Treatment with PROTAC TEAD1/IAP degrader-1 (0.01-10 μM; 20 h) induces up to 32% degradation of endogenous TEAD1 in NCI-H2052 cells with a DC50 of 14 nM, and simultaneously induces up to 88% degradation of endogenous cIAP1 with a DC50 of 270 nM[1].
PROTAC TEAD1/IAP degrader-1 (0.001-10 μM; 144 h) inhibits the proliferation of ZL55, NCI-H226, NCI-H2052 and NCI-H520 cells, with IC50 values of 2194 nM, 798 nM, 1375 nM and 2491 nM, respectively, and achieves nearly complete maximal inhibitory effect after 144 h of treatment[1].
PROTAC TEAD1/IAP degrader-1 (0.001-10 μM; 48 h) reduces the transcriptional level of CTGF in ZL55, NCI-H226 and NCI-H2052 cells, with IC50 values of 866 nM, 497 nM and 125 nM, respectively, after 48 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ZL55, NCI-H226, NCI-H2052, NCI-H520
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Concentration:0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:144 h
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Result:Inhibited cell proliferation with an IC50 of 2194 nM (ZL55), 798 nM (NCI-H226), 1375 nM (NCI-H2052), and 2491 nM (NCI-H520), with a maximum inhibition (Emax) of 99% (ZL55), 100% (NCI-H226), 99% (NCI-H2052), and 98% (NCI-H520).
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Cell Line:ZL55, NCI-H226, NCI-H2052
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:48 h
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Result:Reduced CTGF transcript levels with an IC50 of 866 nM (ZL55), 497 nM (NCI-H226), and 125 nM (NCI-H2052), with an Emax of 72% (ZL55), 100% (NCI-H226), and 73% (NCI-H2052).
Chemical Information
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Molecular Weight 910.96
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Formula C46H45F3N8O7S
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SMILES
O=C(C1=CC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2N=C1)NCC4=NC(OCCN(C)C(COCCOCCOC5=CC=C(NC([C@@H](NC)C)=O)N=C5C#CC6=CN=CS6)=O)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)