PJ-68
CAS No. : 352544-59-3
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| Cat. No. : | HY-124784 |
| M.Wt: | 354.49 |
| Formula: | C25H26N2 |
| Purity: | >98 % |
| Solubility: |
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].
In Vitro:PJ-68 (1-5 μM; 48 h) shows moderate antiproliferative activity against HCC1806 cells[1].
PJ-68 (10-50 μM) specifically inhibits PRMT5 methyltransferase activity and reduces BCR-ABL protein levels in K562 cells[2].
PJ-68 inhibits BCR-ABL gene transcription in K562 cells[2].
PJ-68 inhibits the transcription of the DVL3 gene in K562 cells[2].
PJ-68 reduces the enrichment of PRMT5 at the p15INK4B promoter in K562 cells[2].
PJ-68 (25.0 μM; 1 week) inhibits LTC-IC capacity in CML BM cells, and its combination with IM enhances this effect[2].
PJ-68 reduces H3R2SDM levels in K562 and CML CD34+ cells[2].
PJ-68 increases p15INK4B mRNA levels in K562 and CML CD34+ cells[2].
PJ-68 (0-6.0 μM; 24 h) does not significantly inhibit PRMT5-mediated sDMA modification in HCC1806 cells at concentrations up to 6 μM[1].
PJ-68 is a potent and selective inhibitor of PRMT5 methyltransferase activity with an IC50 of 517 nM[2].
PJ-68 inhibits PRMT5-mediated KLF5 methylation in cell-free in vitro methylation assays[3].
PJ-68 (5 μM; 6 h) decreases KLF5-WT protein levels in HEK293T cells, but does not decrease KLF5-R57K protein levels[3].
PJ-68 reduces the recruitment of PRMT5 and its epigenetic marks to the Mir203 promoter in K562 cells[2].
PJ-68 (25.0 μM; 96 h) selectively induces apoptosis in quiescent CML LSCs compared with NBM CD34+ cells[2].
PJ-68 increases the expression of cell cycle inhibitors p15INK4B and p27KIP1 in CML CD34+ cells[2].
In Vivo:PJ-68 (25-50 mg/kg/d; i.p.; for 2 weeks) significantly prolongs survival and reduces leukemia stem cell populations in a murine CML model[2].
PJ-68 (20-40 mg/kg; i.p.; daily; 3 weeks) significantly inhibits breast tumor growth in vivo in a dose-dependent manner by decreasing KLF5 and its downstream target proteins[3].
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