- Cat. No.
- A11928
LCL-161
LCL161 is an orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity.
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Inhibitor of apoptosis (IAP) antagonists target proteins that restrain caspases and cell death signaling. X-linked inhibitor of apoptosis protein (XIAP) was shown in 1997 to inhibit caspases directly through its baculovirus IAP repeat (BIR) domains. The mitochondrial protein second mitochondria-derived activator of caspases (Smac) relieves this block by binding to IAPs. Most listed compounds are Smac mimetics, which cause autoubiquitination and loss of cellular IAP 1 and 2 (cIAP1, cIAP2). This activates nuclear factor kappa B (NF-κB) and cell death driven by tumor necrosis factor alpha (TNF-α). Birinapant, LCL-161, xevinapant and GDC-0152 are examples, and BV-6 acts on cIAP1, cIAP2 and XIAP. Embelin, a natural benzoquinone, is listed as an XIAP inhibitor.
LCL161 is an orally bioavailable second mitochondrial-derived activator of caspases (SMAC) mimetic and inhibitor of IAP (Inhibitor of Apoptosis Protein) family of proteins, with potential antineoplastic activity.
Synonyms: TL-32711
Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
GDC-0152 is a second mitochondrial activator of caspases (Smac) mimetic inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity.
CST626 (Compound 9) is a pan-IAP degrader PROTAC that targets and degrades inhibitor of apoptosis proteins XIAP, cIAP1, and cIAP2 in MM.1S cells, with DC₅₀ values of 0.7 nM, 2.4 nM, and 6.2 nM, respectively.