An inhibitor of the TRADD-TRAF2 protein-protein interaction
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Apostatin-1

Item No. 45992

Technical Information
Formal Name
N-cycloheptyl-α-[(4,5-dihydro-1-methyl-1Himidazol-2-yl)thio]-benzeneacetamide
CAS Number
2559703-06-7
Synonyms
  • Apt-1
Molecular Formula
C19H27N3OS
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CN1CCN=C1SC(C(NC2CCCCCC2)=O)C3=CC=CC=C3
InChi Code
InChI=1S/C19H27N3OS/c1-22-14-13-20-19(22)24-17(15-9-5-4-6-10-15)18(23)21-16-11-7-2-3-8-12-16/h4-6,9-10,16-17H,2-3,7-8,11-14H2,1H3,(H,21,23)
InChi Key
OXBMBNASDMMXSA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Apostatin-1 is an inhibitor of the protein-protein interaction between TNFR1-associated DEATH domain protein (TRADD) and TNF receptor-associated factor 2 (TRAF2).1 It selectively binds to the N-terminal of TRADD (Kd = 2.17 µM) over a panel of 97 kinases at 10 µM. Apostatin-1 inhibits bortezomib-induced apoptosis in Jurkat cells and RIPK1-mediated apoptosis in TNF-stimulated mouse embryonic fibroblasts (MEFs; IC50s = 0.97 and 1.28 µM, respectively) and induces autophagy in H4 cells. It inhibits RIPK1-mediated apoptosis, induces autophagy, and reduces tau levels and neurofibrillary tangle-like pathology in a mouse model of Alzheimer’s disease and tauopathy.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xu, D., Zhao, H., Jin, M., et al. Modulating TRADD to restore cellular homeostasis and inhibit apoptosis. Nature 587(7832), 133-138 (2020).