Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
2.7113 mL
13.5567 mL
27.1135 mL
5 mM
0.5423 mL
2.7113 mL
5.4227 mL
10 mM
0.2711 mL
1.3557 mL
2.7113 mL
50 mM
0.0542 mL
0.2711 mL
0.5423 mL
Description
FX1 is a selective inhibitor with an IC50 value of 35 μM in reporter assays. FX1 shows great selectivity against a panel of 50 different kinases. 10 μM FX1 fails to significantly inhibit of any of these kinases. FX1 induces .
Features
Recommend for freshly prepared each time for in vitro experiment
FX1 disrupted formation of the BCL6 repression complex, reactivated BCL6 target genes, and mimicked the phenotype of mice engineered to express BCL6 with corepressor binding site mutations. FX1 suppressed ABC-DLBCL cells in vitro and in vivo, as well as primary human ABC-DLBCL specimens ex vivo. FX1 is specific to BCL6 and binds with a greater affinity than the natural BCL6 ligand SMRT. FX1 almost invariantly induced significant derepression of these genes(BCL6 target genes CASP8, CD69, CXCR4, CDKN1A, and DUSP5) as compared with vehicle in 2 independent DLBCL cell lines. FX1 was more than 100-fold more powerful than the previous generation of BCL6 inhibitors represented by 79-6, and 300-fold more potent than the recently reported binding of the antibiotics rifamycin and rifabutin (KD ~1 mM).