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^[1]. (Pink: TEAD1 and cIAP-1 ligand (HY-181536); Blue: IAP ligand (HY-181530); Black: linker (HY-141371)).

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.

910.96

C₄₆H₄₅F₃N₈O₇S

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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• [1]. Gupta N, et al. Expanding the toolbox to develop IAP-based degraders of TEAD transcription factors. Commun Chem. 2026;9(1):69. Published 2026 Jan 19.  [Content Brief]