2798856-04-7
Chemical Structure
SCR-7952
- CAS No.: 2798856-04-7
- Formula:C19H15ClN4O
- Molecular Weight:350.80
InChIKey: FELOKFNJXFDCKP-UHFFFAOYSA-N
SMILES: O=C1N(C2=CC=CN=C2C3CC3)C4=C(C=CC(Cl)=C4)C5=C1N=CN5C
Biological Activity: SCR-7952 is an orally active MAT2A allosteric inhibitor (IC50 = 18.7 nM; Ki = 14.49 nM; Kd = 0.56 nM). SCR-7952 reduces SAM production, PRMT5 activity, and SDMA marks by binding to the MAT2A allosteric pocket, and dysregulates RNA splicing through FANCA intron retention, thereby selectively inhibiting the proliferation of MTAP-deleted cancer cells and producing synergistic effects with PRMT5 inhibitors. SCR-7952 can be used for research on MTAP-deleted cancers[1][2][3][4][5][6][7][8][9].
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SCR-7952 | 99.34% | SCR-7952 is an orally active MAT2A allosteric inhibitor (IC50 = 18.7 nM; Ki = 14.49 nM; Kd = 0.56 nM). SCR-7952 reduces SAM production, PRMT5 activity, and SDMA marks by binding to the MAT2A allosteric pocket, and dysregulates RNA splicing through FANCA intron retention, thereby selectively inhibiting the proliferation of MTAP-deleted cancer cells and producing synergistic effects with PRMT5 inhibitors. SCR-7952 can be used for research on MTAP-deleted cancers. | ||||||||||||||||||||
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References
- [1]. Yu Z, et al. SCR-7952, a highly selective MAT2A inhibitor, demonstrates synergistic antitumor activities in combination with the -adenosylmethionine-competitive or the methylthioadenosine-cooperative protein arginine methyltransferase 5 inhibitors in methylthioadenosine phosphorylase-deleted tumors. MedComm. 2024 Oct;5(10):e705. [Content Brief]
- [2]. Yang S, et al. Discovery of Novel Spirocyclic MAT2A Inhibitors Demonstrating High In Vivo Efficacy in MTAP-Null Xenograft Models. Journal of medicinal chemistry. 2025 Feb 13;68(3):3480-3494. [Content Brief]
- [3]. Zhou F, et al. Discovery of SCR-7952, a novel, potent and high selective MAT2A inhibitor shows robust anti-tumor activities and better safety profile. Cancer Research. 2022 Jun 15;82(12_Supplement):5434-.
- [4]. Chen Y, et al. Integrating proteomics and metabolomics to reveal MAT2A for metabolic reprogramming in non-small cell lung cancer cells. iScience. 2026 Sep 18;29(9):117336.
- [5]. Pulous FE, et al. MAT2A inhibition combats metabolic and transcriptional reprogramming in cancer. Drug discovery today. 2024 Nov;29(11):104189.
- [6]. Zhou Y, et al. Structure-Based Discovery of a Series of Novel MAT2a Inhibitors. ACS medicinal chemistry letters. 2025 Apr 10;16(4):646-650. [Content Brief]
- [7]. Shakil MS, et al. The Methionine-Mitochondria Axis in Cancer: Metabolic Cross-Talk and Therapeutic Vulnerabilities. Current pharmacology reports. 2026;12(1):38.
