Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist H3B-5942 For research use only.

H3B-5942

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.

H3B-5942 Chemical Structure

H3B-5942 Chemical Structure

CAS No. 2052128-15-9

Purity & Quality Control

Batch: S874601 DMSO]99 mg/mL]false]Ethanol]13 mg/mL]false]Water]Insoluble]false Purity: 98.06%
98.06

H3B-5942 Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

Description H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both ERα WT and ERα mutation. The Ki values are 1 nM and 0.41 nM, respectively.
Targets
ERα (Y537S) [1] ERα WT [1]
0.41 nM(Ki) 1 nM(Ki)
In vitro
In vitro

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 ERαWT and ERαMUT lines with GI50 values of 0.5, 2, and 30 nmol/L in the MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C 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-ERαWT line. In the presence of E2, H3B-5942 shows a significant dose-dependent decrease in ER-mediated transactivation in all cell lines tested[1].
In Vivo
In vivo

In vivo, H3B-5942 demonstrates significant single-agent antitumor activity in xenograft models representing ERαWT and ERαY537S breast cancer[1].
Animal Research Animal Models Mice bearing PDX tumors representing Erα(Y537S/WT) breast cancer
Dosages 3, 10, 30, 100, and 200 mg/kg
Administration PO

Chemical Information & Solubility

Molecular Weight 494.63 Formula

C31H34N4O2
CAS No. 2052128-15-9 SDF --
Smiles CCC(=C(C1=CC=C(C=C1)OCCNCC=CC(=O)N(C)C)C2=CC3=C(C=C2)NN=C3)C4=CC=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 99 mg/mL ( (200.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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