A Smac mimetic and IAP inhibitor; binds to the BIR3 domains of IAP1

AZD 5582 – 5 mg

Brand:
Cayman
CAS:
1258392-53-8
Storage:
-20
UN-No:
Non-Hazardous - /

AZD 5582 is a dimeric Smac mimetic and an inhibitor of the inhibitor of apoptosis (IAP) proteins.{60061} It binds to the BIR3 domains of IAP1, IAP2, and XIAP (IC50s = 15, 21, and 15 nM, respectively). It disrupts the protein-protein interaction between IAP1 and caspase-9 in vitro, as well as induces degradation of IAP1 in (EC50 = 0.1 nM) and reduces the growth of MDA-MB-231 breast cancer cells (GI50 = In vivo, AZD 5582 (0.1, 0.5, and 3 mg/kg) induces intratumoral apoptosis and reduces tumor volume in an MDA-MB-231 mouse xenograft model. AZD 5582 (3 mg/kg) also increases CD4+ T cell, spleen, thymus, bone marrow, liver, lung, and lymph node levels of HIV RNA, indicating HIV latency reversal, in a humanized mouse model of antiretroviral therapy-suppressed HIV infection.{60062}  

 

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SKU: 30932 - 5 mg Category:

Description

A Smac mimetic and IAP inhibitor; binds to the BIR3 domains of IAP1, IAP2, and XIAP (IC50s = 15, 21, and 15 nM, respectively); disrupts the protein-protein interaction between IAP1 and caspase-9 in vitro; induces degradation of IAP1 in (EC50 = 0.1 nM) and reduces the growth of MDA-MB-231 breast cancer cells (GI50 = + T cell, spleen, thymus, bone marrow, liver, lung, and lymph node levels of HIV RNA in a humanized mouse model of antiretroviral therapy-suppressed HIV infection at 3 mg/kg

Formal name: 3,3′-[2,4-hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolinamide

Synonyms: 

Molecular weight: 1,015.30

CAS: 1258392-53-8

Purity: ≥98%

Formulation: A crystalline solid

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