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.
(Pink: TEAD ligand (HY-181595); Blue: IAP ligand (HY-181531); Black: linker).
For research use only. We do not sell to patients.
- Formula: C51H48F3N11O3S
- Molecular Weight:952.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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cIAP |
XIAP |
TEAD1 |
TEAD4 |
PROTAC TEAD/IAP degrader-1 (Compound A536) (20 h) degrades HiBiT-TEAD1 in NCI-H2052 cells with a DC50 of 233 nM and a Dmax 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 Dmax 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 (Dmax 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 ECmax of 1920 nM and an Emax 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 ECmax of 6860 nM and an Emax 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 Emax values ranging from 87% to 93%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 952.06
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Formula C51H48F3N11O3S
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SMILES
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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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)
PROTAC TEAD/IAP degrader-1 Related Classifications
HY-181594 Related Classifications
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