Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T16577 |
PRMT5-IN-2
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-2 is an inhibitor of protein arginine methyltransferase 5. | |||
T79274 |
PRMT5-IN-31
|
Histone Methyltransferase | Chromatin/Epigenetic |
PRMT5-IN-31(Compound 3m)作为一种高选择性PRMT5抑制剂,其IC50为0.31 μM。它能够通过占据PRMT5的底物位点以及与氨基酸残基形成必要相互作用来上调hnRNP E1蛋白水平。此外,PRMT5-IN-31能有效抑制A549细胞增殖,其机制涉及诱导apoptosis和阻碍细胞迁移。该化合物在人肝微粒体中表现出较高的代谢稳定性,半衰期为132.4分钟。 | |||
T36630 | MRTX9768 hydrochloride | ||
MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-de... | |||
T79275 |
Antiproliferative agent-25
|
Histone Methyltransferase | Chromatin/Epigenetic |
Antiproliferative agent-25 (Compound 3s4)作为一种选择性PRMT5抑制剂(IC50: 0.11 μM),能够上调hnRNP E1蛋白水平,并通过与SAM及PRMT5的E444残基形成氢键相互作用。该化合物通过促进apoptosis和抑制细胞迁移,有效抑制A549细胞的增殖。此外,Antiproliferative agent-25在人和大鼠肝微粒体中的高清除率表明,其T1/2分别为21.8和4.7分钟。 |