GSK3685032

Product Name: GSK3685032
Chemical Name: GSK3685032
Synonyms: GSK3685032
CBNumber: CB89735154
Formula Weight: 0
MOL File: Mol file

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Hazard and Precautionary Statements (GHS)

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GSK3685032 Chemical Properties,Usage,Production

Definition

GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition.

Mechanism of action

GSK3685032 is a potent first-in-class DNMT1-selective inhibitor shown via crystallographic studies to compete with the active-site loop of DNMT1 for penetration into hemimethylated DNA between two CpG base pairs. GSK3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition in vitro[1].

References

[1] M. Pappalardi. “Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.” Nature cancer 2 1 (2021): 1002–1017.

GSK3685032 Preparation Products And Raw materials

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