A cell-permeable Smac mimetic and an inhibitor of XIAP; binds to BIR2 and BIR3 domain-containing XIAP (IC50 = 1.39 nM); inhibits growth (IC50 = 1 nM)

SM-164 – 1 mg

Brand:
Cayman
CAS:
957135-43-2
Storage:
-20
UN-No:
Non-Hazardous - /

SM-164 is a cell-permeable bivalent mimetic of Smac and an inhibitor of X-linked inhibitor of apoptosis (XIAP).{45621} It binds to BIR2 and BIR3 domain-containing XIAP with an IC50 value of 1.39 nM and interacts with both domains. SM-164 inhibits growth (IC50 = 1 nM), as well as activates caspase-3 and caspase-9, and induces cleavage of the caspase-3 substrate poly(ADP-ribose)-polymerase (PARP), a marker of apoptosis, in HL-60 leukemia cells when used at a concentration of 10 nM. It also reduces tumor volume by 80% in a 2LMP breast cancer mouse xenograft model when administered at a dose of 5 mg/kg in combination with TNF-related apoptosis-inducing ligand (TRAIL).{45622}  

 

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SKU: 28632 - 1 mg Category:

Description

A cell-permeable Smac mimetic and an inhibitor of XIAP; binds to BIR2 and BIR3 domain-containing XIAP (IC50 = 1.39 nM); inhibits growth (IC50 = 1 nM), as well as activates caspase-3 and caspase-9, and induces cleavage of PARP in HL-60 leukemia cells at 10 nM; reduces tumor volume by 80% in a 2LMP breast cancer mouse xenograft model at 5 mg/kg in combination with TRAIL

Formal name: (3S,3′S,6S,6′S,10aS,10′aS)-N,N′-[1,4-phenylenebis[4,1-butanediyl-1H-1,2,3-triazole-1,4-diyl[(S)-phenylmethylene]]]bis[decahydro-6-[[(2S)-2-(methylamino)-1-oxopropyl]amino]-5-oxo-pyrrolo[1,2-a]azocine-3-carboxamide

Synonyms: 

Molecular weight: 1,121.40

CAS: 957135-43-2

Purity: ≥95%

Formulation: A solid

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