Potent antagonist for cIAP1 (Kd <1 nM) and XIAP (Kd\xa0= 45 nM). Not only binds to the isolated BIR3 domains of cIAP1, cIAP2, XIAP but the single BIR domain of ML-IAP with high affinity and degrades TRAF2-bound cIAP1 and cIAP2 rapidly accordingly inhibiti
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST, INHIBITOR
Mechanism of action
cIAP1/cIAP2 inhibitor
Note
Refer to SDS for further information Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Properties
ALogP
3.3
Associated Targets(Human)
BIRC2TchemBaculoviral IAP repeat-containing protein 2 (3 Activities)
1.Allensworth JL, Sauer SJ, Lyerly HK, Morse MA, Devi GR. (2013) Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism.. Breast Cancer Res Treat, 137 (2):(359-71). [PMID:23225169][10.1021/op500134e]
2.Krepler C, Chunduru SK, Halloran MB, He X, Xiao M, Vultur A, Villanueva J, Mitsuuchi Y, Neiman EM, Benetatos C et al.. (2013) The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells.. Clin Cancer Res, 19 (7):(1784-94). [PMID:23403634][10.1021/op500134e]
3.Fulda S. (2014) Molecular pathways: targeting inhibitor of apoptosis proteins in cancer--from molecular mechanism to therapeutic application.. Clin Cancer Res, 20 (2):(289-95). [PMID:24270683][10.1021/op500134e]
4.Benetatos CA, Mitsuuchi Y, Burns JM, Neiman EM, Condon SM, Yu G, Seipel ME, Kapoor GS, Laporte MG, Rippin SR et al.. (2014) Birinapant (TL32711), a bivalent SMAC mimetic, targets TRAF2-associated cIAPs, abrogates TNF-induced NF-κB activation, and is active in patient-derived xenograft models.. Mol Cancer Ther, 13 (4):(867-79). [PMID:24563541][10.1021/op500134e]
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L2207375