352544-59-3
Chemical Structure
PJ-68
- CAS No.: 352544-59-3
- Formula:C25H26N2
- Molecular Weight:354.49
IUPAC Name: N-((9-ethyl-9H-carbazol-3-yl)methyl)-1,2,3,4-tetrahydronaphthalen-1-amine
InChIKey: PUQGENRBXGZWDZ-UHFFFAOYSA-N
SMILES: CCN1C2=C(C3=C1C=CC=C3)C=C(CNC4CCCC5=C4C=CC=C5)C=C2
Biological Activity: PJ-68 is a selective PRMT5 inhibitor (IC50 = 517 nM). PJ-68 reduces KLF5 methylation, stability, and downstream target gene expression. PJ-68 induces Apoptosis, inhibits self-renewal capacity, blocks the Wnt/β-catenin signaling pathway by reducing DVL3 expression, and decreases BCR-ABL mRNA and protein levels. PJ-68 serves as a Ligand for Target Protein for PROTAC for the synthesis of PRMT5 PROTAC degraders, such as YZ-17 (HY-189213). PJ-68 inhibits the growth of basal-like breast cancer. PJ-68 prolongs the survival of CML mice. PJ-68 is used for research on basal-like breast cancer and chronic myeloid leukemia[1][2][3].
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PJ-68 | PJ-68 is a selective PRMT5 inhibitor (IC50 = 517 nM). PJ-68 reduces KLF5 methylation, stability, and downstream target gene expression. PJ-68 induces Apoptosis, inhibits self-renewal capacity, blocks the Wnt/β-catenin signaling pathway by reducing DVL3 expression, and decreases BCR-ABL mRNA and protein levels. PJ-68 serves as a Ligand for Target Protein for PROTAC for the synthesis of PRMT5 PROTAC degraders, such as YZ-17 (HY-189213). PJ-68 inhibits the growth of basal-like breast cancer. PJ-68 prolongs the survival of CML mice. PJ-68 is used for research on basal-like breast cancer and chronic myeloid leukemia. | |||||||||||||||||||||
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References
- [1]. Li Y, et al. Discovery of novel cereblon-recruiting PRMT5 degraders with in vivo efficacy against triple-negative breast cancer. European journal of medicinal chemistry. 2026 Nov 15;318:119199. [Content Brief]
- [2]. Jin Y, et al. Targeting methyltransferase PRMT5 eliminates leukemia stem cells in chronic myelogenous leukemia. The Journal of clinical investigation. 2016 Oct 03;126(10):3961-3980.
- [3]. Wang X, et al. Arginine methyltransferase PRMT5 methylates and stabilizes KLF5 via decreasing its phosphorylation and ubiquitination to promote basal-like breast cancer. Cell death and differentiation. 2021 Oct;28(10):2931-2945.
