2. PROTAC Apoptosis
  3. Ligands for E3 Ligase IAP
  4. 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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IAP ligand 8

IAP ligand 8 Chemical Structure

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IAP ligand 8 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B

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cIAP cIAP-1 cIAP-2 XIAP

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Description

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[1].

IC50 & Target

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.

IAP ligand 8 Related Antibodies

Cell Viability Assay[1]

Cell Line: H28 cell
Concentration: 10 nM, 100 nM, 1 μM
Incubation Time: 72 h
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%).

Apoptosis Analysis[1]

Cell Line: H28 cell
Concentration: 100 nM, 1 μM
Incubation Time: 72 h
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%.

Western Blot Analysis[1]

Cell Line: H28 cell
Concentration: 100 nM, 1 μM
Incubation Time: 24 h
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.
Molecular Weight

424.48

Formula

C21H30F2N4O3
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IAP ligand 8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IAP ligand 8IAP ligand8IAP ligand-8Ligands for E3 LigaseIAPE3 ligase-recruiting MoietyPROTACs/IPDsSMAC mimeticIAP-recruiting proteolysis-targeting chimerasIAP familyTEAD1Inhibitorinhibitorinhibit

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