IAP
Mammalian IAP proteins comprise eight family members, including X chromosome-linked IAP (XIAP), cellular IAP1 (cIAP1), and cIAP2. Among other functions, XIAP can antagonize apoptosis by inhibiting caspases. cIAP proteins act as E3 ubiquitin ligases that mediate ubiquitination of target proteins via their really interesting new gene (RING) domain. Human cancers typically express high levels of IAP proteins which favor their evasion of programmed cell death. Endogenous Smac protein promotes cell death upon its release from the mitochondrial intermembrane space into the cytosol by antagonizing IAP proteins.IAP proteins are their integral components that activate NF-kB and mitogen-activated protein kinase (MAPK) pathways upon ubiquitin chain scaffolds. In TNF family, stimulated signaling E3 ligases c-IAP1 and c-IAP2 are recruited through the adaptor protein TRAF2 to receptor-associated complexes where they promote K63- and K11-linked polyubiquitylation of RIP1, NEMO, TRAF2, and themselves. While cellular IAP proteins are required for the activation of TNF family-induced canonical NF-kB signaling, they are negative regulators of the noncanonical NF-kB pathway. IAP proteins may also play a role in DNA damage, Wnt signaling, cell motility and migration, and autophagy pathways.
References
1.Fulda S. Int Rev Cell Mol Biol. 2017;330:157-169.
2.Silke J,et al. Methods Enzymol. 2014;545:35-65.
References
1.Fulda S. Int Rev Cell Mol Biol. 2017;330:157-169.
2.Silke J,et al. Methods Enzymol. 2014;545:35-65.
Apoptosis
IAP
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HM90822
catalog no : M36356
cas no: 1363145-46-3
HM90822 is a novel synthetic apoptotic protein (IAP) antagonist that induces apoptosis in human pancreatic cancer cells through proteasome-dependent degradation of IAPs containing the BIR2/3 structural domain. -
CUDC-427
catalog no : M33326
cas no: 1446182-94-0
CUDC-427 (GDC-0917) is an orally bioactive and pan antagonist of inhibitor of apoptosis proteins(IAPs). CUDC-427 can be used in research on cancers. -
SM-164
catalog no : M22507
cas no: 957135-43-2
SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains (IC50: 1.39 nM). It acts as an extremely potent antagonist of XIAP. SM-164 binds to XIAP being 300 and 7000-times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. -
APG-1387
catalog no : M21856
cas no: 1570231-89-8
APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). -
GDC-0152
catalog no : M16352
cas no: 873652-48-3
GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM, respectively.