GSK3326595

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性、可逆且具有口服活性的 PRMT5 抑制剂，IC50 为 22 nM。

A potent, selective, reversible and orally active PRMT5 inhibitor with IC50 of 22 nM; potently inhibits tumor growth in cellular and animal models.Blood Cancer Phase 1 Clinical.

Western Blot AnalysisCell Line:HEK-293T cells, A549 cells Concentration:10 nM, 25 nM, 50 nM, 100 nM Incubation Time:48 h Result:Strongly inhibited ACE2-RBD interaction at low concentration.Inhibited SARS-CoV-2 Omicron and other variants Spike1 binding with ACE2.Inhibits SARS-CoV-2 spike pseudovirus infection host cells.Cell Cytotoxicity Assay Cell Line:MCL cells Concentration:0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM Incubation Time:72 h Result:Resulted in modest growth inhibition in MCL cells.

Animal Model:LDL receptor knockout miceDosage:5 mg/kg Administration:Intraperitoneal injection (i.p.)Result:Did not alter atherosclerosis susceptibility.Increased hepatic triglyceride levels without changing the hyperlipidemia extent.Activated genes involved in fatty acid acquisition.Animal Model:myelocytomatosis transgene turned on mice Dosage:25 mg/kg, 50 mg/kg Administration:Oral Result:Significantly suppressed tumor growth at 50 mg/kg.Showed better therapeutic efficacy at 25 mg/kg.

GSK-3326595 | EPZ015938 | EPZ-015938

Chromatin/Epigenetic

HMTase

HMTase

Cancer

Blood cancer

1616392-22-3

452.54928

C24H32N6O3

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(C)N1CCC(NC2=NC=NC(C(NC[C@H](O)CN3CCC(C=CC=C4)=C4C3)=O)=C2)CC1

4-Pyrimidinecarboxamide, 6-[(1-acetyl-4-piperidinyl)amino]-N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-

(-20℃)

With Ice Pack

≥ 2 years