2278356-90-2
Chemical Structure
PRT543
- CAS No.: 2278356-90-2
- Formula:C18H18Cl2N4O4
- Molecular Weight:425.27
IUPAC Name: (2R,3S,4R,5R)-5-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-((R)-(3,4-dichlorophenyl)(hydroxy)methyl)-3-methyltetrahydrofuran-3,4-diol
InChIKey: NVZVVFMXEHOMQR-FOOXYVKASA-N
SMILES: O[C@@]1(C)[C@@H](O)[C@H](N2C3=NC=NC(N)=C3C=C2)O[C@@H]1[C@H](O)C4=CC=C(Cl)C(Cl)=C4
Biological Activity: PRT543 is an orally active selective PRMT5 inhibitor. PRT543 reduces intracellular symmetric dimethylarginine (sDMA) levels, downregulates the expression of genes related to DNA damage repair and DNA replication pathways, and induces abnormal alternative splicing. PRT543 inhibits the MYB, NOTCH1 and PI3K/AKT signaling pathways, promotes nuclear translocation of FOXO1, upregulates the pro-apoptotic protein BAX, and enhances cellular sensitivity to BCL-2 inhibition. PRT543 disrupts the normal RNA splicing process and exerts a synthetic lethal effect on myeloid tumor cells carrying splicing factor mutations. PRT543 can be used in research related to various cancers including breast cancer, ovarian cancer and acute myeloid leukemia[1][2][3][4][5].
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PRT543 | PRT543 is an orally active selective PRMT5 inhibitor. PRT543 reduces intracellular symmetric dimethylarginine (sDMA) levels, downregulates the expression of genes related to DNA damage repair and DNA replication pathways, and induces abnormal alternative splicing. PRT543 inhibits the MYB, NOTCH1 and PI3K/AKT signaling pathways, promotes nuclear translocation of FOXO1, upregulates the pro-apoptotic protein BAX, and enhances cellular sensitivity to BCL-2 inhibition. PRT543 disrupts the normal RNA splicing process and exerts a synthetic lethal effect on myeloid tumor cells carrying splicing factor mutations. PRT543 can be used in research related to various cancers including breast cancer, ovarian cancer and acute myeloid leukemia. | |||||||||||||||||||||
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- [1]. Brown F, et al. PRMT5 Inhibition Drives Therapeutic Vulnerability to BCL-2 Inhibition with Venetoclax and Provides Rationale for Combination Therapy in Mantle Cell Lymphoma. Blood. 2019;134(Suppl 1):302.
- [2]. Carter J, et al. Abstract 1138: PRMT5 inhibition downregulates MYB and NOTCH1 signaling, key molecular drivers of adenoid cystic carcinoma. Cancer Res. 2021;81(13_Supplement):1138.
- [3]. Bewersdorf JP, et al. Phase Ib study of PRT543, an oral protein arginine methyltransferase 5 (PRMT5) inhibitor, in patients with advanced splicing factor-mutant myeloid malignancies. Leukemia. 2025;39:765-769.
- [4]. Carter J, et al. PRMT5 Inhibitors Regulate DNA Damage Repair Pathways in Cancer Cells and Improve Response to PARP Inhibition and Chemotherapies. Cancer Res Commun. 2023;3(11):2233-2243. [Content Brief]
- [5]. Bewersdorf JP, et al. Phase Ib study of PRT543, an oral protein arginine methyltransferase 5 (PRMT5) inhibitor, in patients with advanced splicing factor-mutant myeloid malignancies. Leukemia. 2025;39(3):765-769. [Content Brief]
Keywords
