1096144-06-7
Chemical Structure
PST3.1a
- CAS No.: 1096144-06-7
- Formula:C32H33O6P
- Molecular Weight:544.57
InChIKey: BFDNKVJGHOSKET-DHNIRKAVSA-N
SMILES: O[C@@H]([P@@](O[C@@H]1COCC2=CC=CC=C2)(C3=CC=CC=C3)=O)[C@@H](OCC4=CC=CC=C4)[C@@H]1OCC5=CC=CC=C5
Biological Activity: PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease[1][2].
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PST3.1a | PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease. | |||||||||||||||||||||
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- [1]. Hassani Z, et al. Phostine PST3. 1a targets MGAT5 and inhibits glioblastoma-initiating cell invasiveness and proliferation[J]. Molecular Cancer Research, 2017, 15(10): 1376-1387. [Content Brief]
- [2]. Muyor K, et al. MO072: PST3. 1A, An Inhibitor of MGAT5 Decreases Renal Fibrosis in a Rat Model of Chronic Kidney Disease[J]. Nephrology Dialysis Transplantation, 2022, 37(Supplement_3): gfac063. 024.
Keywords
