Argonaute-2 Inhibitor, BCI-137 – Calbiochem

Descrição detalhada : A cell-permeable dioxotetrahydroquinoxaline compound that mimics uridine monophosphate for affinity interaction at the Argonaute-2 (Ago2) Mid domain (KD = 126 microM) and effectively inhibits Ago2 cellular miRNA loading in acute promyelocytic leukemia (APL) NB4 cultures (% inhibition by RIP = 79%/miR-107, 73%/let-7a, 73%/miR-223, 68%/miR-26a, 53%/miR-60a; 100 nM for 48 h) without affecting cellular Ago2 stability. Consistent with the involvement of Ago2 in heterochromatic miR-155HG silencing, BCI-137 is reported to decrease miR-155HG promoter region-associated Ago2 with a concomitant acetylation induction of the promoter region-associated histone H4 (70% reduced Ago2 association and 300% enhanced H4 acetylation, respectively, by ChIP; 10 microM). Likewise, Ago2 inhibition by BCI-137 is shown to boost Retinoic Acid-(RA, Cat. no. 554720) induced NB4 granulocyte differentiation as a result of greatly upregulated expression of the differentiation-related miRNAs (140% and 255% increased miR-26a and miR-223 level, respectively, compared to 100 nM RA stimulation alone for 96 h) without affecting NB4 proliferation or viability (up to 10 microM and 96 h with or without 100 nM RA stimulation)., A cell-permeable, non-toxic dioxotetrahydroquinoxaline compound that mimics uridine and directly and reversibly interacts with the microRNA (miRNA) binding domain of Argonaute-2 (Ago2; KD = 126 microM) and significantly inhibits binding of miR-20a, miR-26a, miR-107, miR-223, and let-7a to Ago2. However, it does not affect Ago2 stability in cells. Displaces Ago2 from the miR-155 host gene promoter region (70% reduction in Ago2 association) and increases histone H4 acetylation (~300%) in NB4 leukemia cell line. Promotes retinoic acid-induced differentiation of NB4 cells to granulocytes.Please note that the molecular weight for this compound is batch-specific due to variable water content.
Sinónimos : Argonaute-2 Inhibitor, BCI-137 - Calbiochem; 2-(2,3-Dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamido) propanoic acid, N-((2,3-Dihydroxy-6-quinoxalinyl)sulfonyl)alanine, Ago2 Inhibitor, BCI137
Fórmula molecula r: C11H11N3O6S
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA