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Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
| Molecular Weight | 598.18 |
| CAS Number | 1071992-57-8 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
| Related IAP Products |
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| AT-406
Xevinapant (Debio1143,AT-406, SM-406) is a potentially first-in-class, highly potent oral antagonist of inhibitor of apoptosis protein (IAP), which not only promotes cancer cell death by inhibiting IAP, but also It can enhance the anti-tumor immune response by inhibiting IAP. |
| GDC-0152
GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins with potential antineoplastic activity. |
| Birinapant
Birinapant (TL32711) is a bivalent Smac analogue, which is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces autoubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: Caspase-8 complex, which activates and induces tumor cell death. |
| BV6
BV6 is a small molecule Smac analog that antagonizes cIAP1 and XIAP. |
| LCL161
LCL161 is an orally bioavailable SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). LCL161 enhanced the proapoptotic effects of nilotinib and PKC412, against leukemic disease in vitro and potentiated the activity of both kinase inhibitors against leukemic disease in vivo. |
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