PROTAC TEAD/IAP degrader-1 

PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma^[1]. (Pink: TEAD ligand (HY-181595); Blue: IAP ligand (HY-181531); Black: linker).

PROTAC TEAD/IAP degrader-1 (Compound A536) (20 h) degrades HiBiT-TEAD1 in NCI-H2052 cells with a DC₅₀ of 233 nM and a D_max of 67%^[1].
PROTAC TEAD/IAP degrader-1 (20 h) degrades endogenous TEAD1 in NCI-H2052 cells with a DC₅₀ of 110 nM and a Dₘₐₓ of 51%^[1].
PROTAC TEAD/IAP degrader-1 (20 h) weakly degrades endogenous TEAD4 in NCI-H2052 cells with a DC₅₀ of 990 nM and a D_max of 24%, showing selectivity for TEAD1 over TEAD4^[1].
PROTAC TEAD/IAP degrader-1 (18 h) preferentially degrades HiBiT-TEAD1 in NCI-H226 cells following 18 h treatment, with weak activity against HiBiT-TEAD3 (D_max of 16%) and minimal activity against HiBiT-TEAD2 and HiBiT-TEAD4^[1].
PROTAC TEAD/IAP degrader-1 (2 h) engages cellular cIAP1 in HEK293T cells with an IC₅₀ of 327 nM in live cells and has moderate intracellular availability^[1].
PROTAC TEAD/IAP degrader-1 (2 h) engages cellular XIAP in HEK293T cells with an IC₅₀ of 701 nM^[1].
PROTAC TEAD/IAP degrader-1 (4 h) promotes formation of a cIAP1-TEAD1 ternary complex in NCI-H2052 cells with an EC_max of 1920 nM and an E_max of 73 mBU^[1].
PROTAC TEAD/IAP degrader-1 (4 h) promotes formation of a XIAP-TEAD1 ternary complex in NCI-H2052 cells with an EC_max of 6860 nM and an E_max of 22 mBU^[1].
PROTAC TEAD/IAP degrader-1 (144 h) inhibits proliferation of Hippo-dependent mesothelioma cell lines (NCI-H226, NCI-H2052, ZL55) and Hippo-independent NCI-H520 cells with IC₅₀ values ranging from 386 nM to 1250 nM^[1].
PROTAC TEAD/IAP degrader-1 (48 h) downregulates CTGF mRNA (a TEAD target gene) in Hippo-dependent mesothelioma cell lines with IC₅₀ values ranging from 170 nM to 380 nM and E_max values ranging from 87% to 93%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

952.06

C₅₁H₄₈F₃N₁₁O₃S

CN[C@H](C(NC1=CC=C(C(C#CC2=CN=CS2)=N1)C3=C(N(N=C3C)CC(N4CC5(C4)CCN(CC5)C6=CC=CC(CNC(C7=CC8=CC=CC(C9=CC=C(C=C9)C(F)(F)F)=C8N=C7)=O)=N6)=O)C)=O)C

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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]