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
2.0217 mL
10.1086 mL
20.2171 mL
5 mM
0.4043 mL
2.0217 mL
4.0434 mL
10 mM
0.2022 mL
1.0109 mL
2.0217 mL
50 mM
0.0404 mL
0.2022 mL
0.4043 mL
Description
H3B-5942 is a selective and irreversible covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.
H3B-5942 covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation. Upon binding to ERα, H3B-5942 triggers global DNA binding of ERα to ERE-containing promoter and enhancer regions and induces a transcriptionally repressive conformation of ERα by evicting coactivators. H3B-5942 demonstrates potent antiproliferative activity in a panel of ERα and ERα lines with GI50 values of 0.5, 2, and 30 nmol/L in the MCF7-Parental, MCF7-LTED-ERα, and MCF7-LTED-ERα lines, respectively. In the absence of E2, H3B-5942 shows no significant impact on ER-mediated transcription in the MCF7-Parental (endocrine therapy-sensitive) and MCF7-LTED-ERαY537C lines but does result in a 1.5-fold (P = 0.03) increase in the MCF7-LTED-ERα line. In the presence of E2, H3B-5942 shows a significant dose-dependent decrease in ER-mediated transactivation in all cell lines tested.
