3062376-84-2
Chemical Structure
SGC8158
- CAS No.: 3062376-84-2
- Formula:C27H31ClN6O3S
- Molecular Weight:555.09
IUPAC Name: (2R,3R,4S,5S)-2-(6-amino-9H-purin-9-yl)-5-(((4-(((4'-chloro-[1,1'-biphenyl]-3-yl)methyl)amino)butyl)thio)methyl)tetrahydrofuran-3,4-diol
InChIKey: UDFJXRJYAZANFF-VBHAUSMQSA-N
SMILES: O[C@H]1[C@@H](O)[C@H](N2C(N=CN=C3N)=C3N=C2)O[C@@H]1CSCCCCNCC4=CC=CC(C5=CC=C(Cl)C=C5)=C4
Biological Activity: SGC8158 is a selective PRMT7 inhibitor. SGC8158 occupies the adenosine/hydrophobic pocket, blocks PRMT7 methylation, and is noncompetitive with peptide. SGC8158 has an IC50 of <2.5 nM and a Kd of 6.4 nM against PRMT7. SGC8158 is not cell membrane permeable and requires the prodrug SGC3027 (HY-112445) to exert cellular activity, being released by reductases to reduce Socs3 transcription, STAT3 occupancy, HSP70, survival/proliferation, and increase ER stress, DNA damage, endothelial death, and impair angiogenesis. SGC8158 can be used for research on SARS-CoV-2 infection and C. difficile infection[1][2][3][4][5][6][7][8].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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SGC8158 | 97.6% | SGC8158 is a selective PRMT7 inhibitor. SGC8158 occupies the adenosine/hydrophobic pocket, blocks PRMT7 methylation, and is noncompetitive with peptide. SGC8158 has an IC50 of <2.5 nM and a Kd of 6.4 nM against PRMT7. SGC8158 is not cell membrane permeable and requires the prodrug SGC3027 (HY-112445) to exert cellular activity, being released by reductases to reduce Socs3 transcription, STAT3 occupancy, HSP70, survival/proliferation, and increase ER stress, DNA damage, endothelial death, and impair angiogenesis. SGC8158 can be used for research on SARS-CoV-2 infection and C. difficile infection. | ||||||||||||||||||||
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Similarity Score 0.70
HY-112445SGC3027 -
Similarity Score 0.69
HY-183653AK442 -
Similarity Score 0.68
HY-162082METTL1-WDR4-IN-2 -
Similarity Score 0.64
HY-137241S-Adenosyl-3-thiopropylamine -
Similarity Score 0.64
HY-156291XSJ2-46 -
Similarity Score 0.62
HY-162177SARS-CoV-2-IN-78 -
Similarity Score 0.62
HY-W750643m-APTA -
Similarity Score 0.62
HY-124131DS-437 -
Similarity Score 0.62
HY-138993NNMT-IN-6 -
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References
- [1]. Szewczyk MM, et al. Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response. Nature communications. 2020 May 14;11(1):2396.
- [2]. Srour N, et al. PRMT7 restricts CD8+ T cells expansion via the NF-ΚB pathway. Nature communications. 2026 Sep 06;17(1):10564.
- [3]. Ahn BY, et al. Prmt7 regulates the JAK/STAT/Socs3 signaling pathway in postmenopausal cardiomyopathy. Experimental & molecular medicine. 2024 Mar;56(3):711-720.
- [4]. Tran TTV, et al. Endothelial PRMT7 prevents dysfunction, promotes revascularization and enhances cardiac recovery post-myocardial infarction. Experimental & molecular medicine. 2025 Aug;57(8):1759-1774.
- [5]. Kottur J, et al. Structures of SARS-CoV-2 N7-methyltransferase with DOT1L and PRMT7 inhibitors provide a platform for new antivirals. PLoS pathogens. 2023 Jul;19(7):e1011546.
- [6]. Kulkarni AS, et al. Tailoring PRMT Inhibition: Shifting PRMT7 Selectivity to PRMT4 through “T-Shape” Strategy and “Linker-Specific” Preferences. Journal of Medicinal Chemistry. 2026 May 1;69(9):9977-90. [Content Brief]
- [7]. Talukdar A, et al. Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues. Journal of medicinal chemistry. 2022 Feb 10;65(3):1662-1684. [Content Brief]
- [8]. Zhou J, et al. Repurposing epigenetic inhibitors to target the Clostridioides difficile-specific DNA adenine methyltransferase and sporulation regulator CamA. Epigenetics. 2022 Sep 2;17(9):970-81.
