A bivalent Smac mimetic and IAP antagonist; binds to IAP1 and XIAP (Kds = 0.46 and 1.3 nM

BV6 – 5 mg

Brand:
Cayman
CAS:
1001600-56-1
Storage:
-20
UN-No:
Non-Hazardous - /

BV6 is a bivalent Smac mimetic and an antagonist of the inhibitor of apoptosis (IAP) proteins that binds to IAP1 and XIAP (Kds = 0.46 and 1.3 nM, respectively).{53069} It induces autoubiquitination and proteasomal degradation of IAP1 and XIAP in MDA-MB-231 cells when used at a concentration of 5 μM. BV6 (4 μM) induces NF-κB activation and TNF-dependent apoptosis in A2058 and MDA-MB-231 cells. It enhances radiosensitization and increases apoptosis in HCC193 and H460 non-small cell lung cancer (NSCLC) cell lines.{53068} BV6 (1 μM) induces cell death in a panel of 40 primary, patient-derived B cell precursor acute lymphoblastic leukemia (BCP-ALL) samples in a TNF-dependent manner.{53070} In vivo, BV6 (10 mg/kg) increases survival and the time to relapse in a high-risk BCP-ALL patient-derived xenograft (PDX) mouse model.  

 

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Description

A bivalent Smac mimetic and IAP antagonist; binds to IAP1 and XIAP (Kds = 0.46 and 1.3 nM, respectively); induces autoubiquitination and proteasomal degradation of IAP1 and XIAP in MDA-MB-231 cells at 5 μM; induces NF-κB activation and TNF-dependent apoptosis in A2058 and MDA-MB-231 cells at 4 μM; enhances radiosensitization and increases apoptosis in HCC193 and H460 NSCLC cell lines; induces cell death in a panel of 40 primary, patient-derived BCP-ALL samples at 1 μM; increases survival and time to relapse in a high-risk BCP-ALL PDX mouse model

Formal name: 4,4′-(1,6-hexanediyl)bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolyl-β-phenyl-L-phenylalaninamide

Synonyms: 

Molecular weight: 1,205.60

CAS: 1001600-56-1

Purity: ≥98%

Formulation: A crystalline solid

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