Synonyms: 4SC-301; N-(5-Benzoyl-1H-benzimidazol-2-yl)-2-(1-thieno[3,2-d]pyrimidin-4-yl-4-piperidinyl)-4-thiazolecarboxamide; N-(6-Benzoyl-1H-benzimidazol-2-yl)-2-(1-thieno[3,2-d]pyrimidin-4-yl-4-piperidinyl)-4-thiazolecarboxamide; SC 75741; V1810
Molecular Formula: C29H23N7O2S2
Molecular Weight: 565.67
Linear Structural Formula: C29H23N7O2S2
Purity: >=97% (HPLC)
Storage: 2-8C
Biochem Physiol Actions: SC75741 (4SC-301; V1810) is a potent NF-kappaB (NF-kappaB) inhibitor (IC50 = 200 nM against 10 ng/mL TNF-alpha-induced NF-kappaB reporter gene expression in A549 cells) that impairs p65 subunit (RelA) DNA-binding activity without affecting p65 phosphorylation or nuclear translocation, nor proteasome-mediatted IkappaBalpha degradation. SC75741 induces apoptosis in multiple myeloma cultures (IC50 from 5 to 12 muM in 48 hrs; OPM2, U266, NCI-H929, RPMI-8226), but not PBMCs (89% viability post 4-hr 100 muM SC75741 treatment). NF-kappaB inhibition by SC75741 treatment is reported to effectively block influenza virus propagation both in cultures in vitro (1-5 muM) and in mice in vivo (5 mg/kg daily i.v. or 7.5-15 mg/kg twice a day i.p.).