2170136-65-7
Chemical Structure
GSK-3484862
Synonym(s): (R)-GSK3482364
- CAS No.: 2170136-65-7
- Formula:C19H19N5OS
- Molecular Weight:365.45
IUPAC Name: (R)-2-((3,5-dicyano-6-(dimethylamino)-4-ethylpyridin-2-yl)thio)-2-phenylacetamide
InChIKey: KIEQQZZDWUNUQK-MRXNPFEDSA-N
SMILES: O=C(N)[C@H](SC1=NC(N(C)C)=C(C#N)C(CC)=C1C#N)C2=CC=CC=C2
Biological Activity: GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma[1][2][3][4].
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GSK-3484862 | 99.95% | GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma. | ||||||||||||||||||||
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GSK-3484862 (GMP) | GSK-3484862 GMP is GSK-3484862 (HY-135146) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma. | |||||||||||||||||||||
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GSK-3484862 (Standard) | ≥98% | GSK-3484862 (Standard) is the analytical standard of GSK-3484862 (HY-135146). This product is intended for research and analytical applications. GSK-3484862 is a highly potent non-covalent inhibitor and demethylating agent of DNMT1. GSK-3484862 induces genome-wide DNA demethylation, including the regulatory elements of DNMT3B and the promoter region of TERT, and significantly inhibits cell viability, growth, proliferation and self-renewal. GSK-3484862 blocks the transformation of young AT2 cells, induces apoptosis, and generates transcriptomic features similar to those of senescent cells. GSK-3484862 is widely used in studies related to lung cancer, oral squamous cell carcinoma and lung adenocarcinoma. | ||||||||||||||||||||
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References
- [1]. Azevedo Portilho N, et al. The DNMT1 inhibitor GSK-3484862 mediates global demethylation in murine embryonic stem cells. Epigenetics Chromatin. 2021;14(1):56. Published 2021 Dec 15. [Content Brief]
- [2]. Liu Y, et al. DNMT1-targeting remodeling global DNA hypomethylation for enhanced tumor suppression and circumvented toxicity in oral squamous cell carcinoma. Mol Cancer. 2024;23(1):104. Published 2024 May 16. [Content Brief]
- [3]. Zhuang X, et al. Aging limits stemness and tumorigenesis in the lung by reprogramming iron homeostasis[J]. BioRxiv, 2024: 2024.06. 23.600305.
- [4]. Chen Q, et al. GSK-3484862, a DNMT1 degrader, promotes DNMT3B expression in lung cancer cells. NAR Cancer. 2025;7(2):zcaf018. Published 2025 May 27. [Content Brief]
