IAP ligand 8
IAP ligand 8 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 8 selectively targets cIAP1-BIR3, XIAP-BIR2 (with a KD of 15.8 nM for both). IAP ligand 8 serves as an IAP ligand moiety to synthesize IAP-recruiting protein degrader (IPD) (HY-181590). This IPD simultaneously forms two ternary complexes, cIAP1-A538-TEAD1 and XIAP-A538-TEAD1, and efficiently degrades TEAD1 via a dual E3 recruitment mechanism, while inducing the autodegradation of cIAP1. IAP ligand 8 and its series of degraders are applicable to targeted research on Hippo pathway-dysregulated cancers such as NF2-mutant mesothelioma.
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- Formule: C21H30F2N4O3
- Masse moléculaire:424.48
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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cIAP-1 |
XIAP |
In Vitro
IAP ligand 8 (A238) (0.8-500 nM) exhibits a KD of 15.8 nM for cIAP1-BIR3, a KD of 15.8 nM for XIAP-BIR2, and a KD of 126 nM for XIAP-BIR3 in SPR assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H28 cell
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Concentration:10 nM, 100 nM, 1 μM
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Incubation Time:72 h
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Result:Significantly reduced the cell viability of H28 cells in a concentration-dependent manner, with viability rates of 85%, 60% and 25% at 10 nM, 100 nM and 1 μM respectively, compared with the control group (set as 100%).
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Cell Line:H28 cell
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Concentration:100 nM, 1 μM
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Incubation Time:72 h
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Result:Induced apoptosis of H28 cells, with apoptotic rates of 20% at 100 nM and 45% at 1 μM, while the apoptotic rate of the control group was only 5%.
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Cell Line:H28 cell
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Concentration:100 nM, 1 μM
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Incubation Time:24 h
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Result:Downregulated the protein expression of cIAP1 by 60% at 100 nM and 80% at 1 μM, upregulated the expression of cleaved-caspase 3 by 1.5-fold at 100 nM and 2.5-fold at 1 μM, and had no significant effect on XIAP protein expression.
Chemical Information
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Masse moléculaire 424.48
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Formule C21H30F2N4O3
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SMILES
CN[C@H](C(N[C@@H](C(C)(C)C)C(N1CCC[C@H]1C(NC2=C(C=CC=C2F)F)=O)=O)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
IAP ligand 8 Related Classifications
HY-181532 Related Classifications
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