2170140-50-6
Chemical Structure
(R)-GSK-3685032
- CAS No.: 2170140-50-6
- Formula:C22H24N6OS
- Molecular Weight:420.53
IUPAC Name: (R)-2-((6-(4-aminopiperidin-1-yl)-3,5-dicyano-4-ethylpyridin-2-yl)thio)-2-phenylacetamide
InChIKey: KNKHRZYILDZLRE-LJQANCHMSA-N
SMILES: N#CC1=C(N2CCC(CC2)N)N=C(C(C#N)=C1CC)S[C@H](C3=CC=CC=C3)C(N)=O
Biological Activity: (R)-GSK-3685032 is the R-enantiomer of GSK-3685032 (HY-139664) and is a potent, non-covalent, reversible DNMT1-selective inhibitor with an IC50 of 0.036 μM against DNMT1. (R)-GSK-3685032 preferentially binds DNMT1 in a hemimethylated DNA context, inhibits DNA methylation maintenance by occupying the DNMT1 active site loop that inserts into DNA and by interacting with the target recognition domain, thereby inducing DNA hypomethylation and transcriptional activation. (R)-GSK-3685032 is useful for research on DNMT1, acute myeloid leukemia, and B cell humoral immunity[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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(R)-GSK-3685032 | 98.97% | (R)-GSK-3685032 is the R-enantiomer of GSK-3685032 (HY-139664) and is a potent, non-covalent, reversible DNMT1-selective inhibitor with an IC50 of 0.036 μM against DNMT1. (R)-GSK-3685032 preferentially binds DNMT1 in a hemimethylated DNA context, inhibits DNA methylation maintenance by occupying the DNMT1 active site loop that inserts into DNA and by interacting with the target recognition domain, thereby inducing DNA hypomethylation and transcriptional activation. (R)-GSK-3685032 is useful for research on DNMT1, acute myeloid leukemia, and B cell humoral immunity. | ||||||||||||||||||||
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References
- [1]. Cousu C, et al. Germinal center output is sustained by HELLS-dependent DNA-methylation-maintenance in B cells. Nature communications. 2023 Sep 14;14(1):5695. [Content Brief]
- [2]. Pappalardi MB, et al. Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia. Nature cancer. 2021 Oct;2(10):1002-1017. [Content Brief]
