GSK3326595

SKU: orb1226050

Description

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.

Key Properties

• CAS Number: 1616392-22-3
• MW: 452.54928
• Purity: >98% (HPLC)
• Formula: C₂₄H₃₂N₆O₃
• SMILES: O=C(C)N1CCC(NC2=NC=NC(C(NC[C@H](O)CN3CCC(C=CC=C4)=C4C3)=O)=C2)CC1
• Target: HMTase
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vivo:
  Animal model: LDL receptor knockout mice. Dosage: 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.
• In Vitro:
  Western blot analysis. Cell 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK-3326595 | EPZ015938 | EPZ-015938

Quick Database Links

Gene Symbol

HMTase