IAP ligand 9
IAP ligand 9 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 9 selectively targets cIAP1-BIR3, XIAP-BIR3, exhibits extremely weak binding affinity for XIAP-BIR2, with a KD of 100 nM for cIAP1-BIR3 and 10 nM for XIAP-BIR2. IAP ligand 9 can be used to synthesize IAP-recruiting protein degraders (IPD), and can calibrate the cell permeability and cellular-level target binding assays of the IPD molecule SNIPER (TEAD)-1 (HY-181607). IAP ligand 9 and its series of degraders can be used in the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C22H33FN4O4
- Molecular Weight:436.52
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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cIAP-1 |
XIAP |
IAP ligand 9 (A255), which exhibits favorable cell permeability, serves as a cell-permeable reference compound for determining the intracellular availability index of other IPDs[1].
In NanoBRET cellular target binding assays, IAP ligand 9 (0.0001-10 μM; 3 h) exhibits an IC50 of 39 nM in live cells and 149 nM in permeabilized cells against cIAP1F616A, and serves as the reference standard for the intracellular availability index (AI) of IAP-recruiting degraders[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 436.52
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Formel C22H33FN4O4
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SMILES
CN[C@H](C(N[C@@H](C(C)(C)C)C(N1CCC[C@H]1C(NC2=CC(OC)=CC=C2F)=O)=O)=O)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)