1G244
Product Sizes
5 mg
£193.00
10-4584-5MG
25 mg
£407.00
10-4584-25MG
About this Product
- SKU:
- 10-4584
- Additional Names:
- PTX-1210
- Extra Details:
- Potent and selective inhibitor of the prolyl dipeptidases DPP8 (IC50 = 14 nM) and DPP9 (IC50 = 53 nM).1,2 It does not inhibit DPP2, DPP4 or fibroblast activation protein (FAP) at 100 uM.1,2 1G244 is a slow binding competitive inhibitor of DPP8 but a competitive and reversible inhibitor of DPP9.2 Inhibition of DPP8/9 by 1G244 has been shown to cause pro-caspase-1-dependent pyroptosis in macrophages and monocytes.3 1G244 also induced cell death in DPP8/9 knockout cells at higher concentration indicating there may be some off-target effects.3 1G244 blocks adipogenesis in preadipocyte 3T3-L1 and 3T3-F422A cells.4 DPP8/9 inhibition attenuates PPARg2 induction during preadipocyte differentiation.4 Because of its inhibitory effects on pro-inflammatory macrophages, 1G244 inhibition of DPP8/9 has been examined as a potential therapy for reducing atherosclerosis and/or in the prevention of plaque rupture.5,6 Cell permeable.
- Molecular Weight:
- 504.57
- Physical State:
- Solid
- Purity:
- >98%
- Purification:
- HPLC Purified
- Shipping Conditions:
- Ambient
- Storage Conditions:
- -20[o]C
- Supplier:
- Focus Biomolecules
- Type:
- Proteins, Peptides, Small Molecules & Other Biomolecules: Inhibitors
- Manufacturer's Data Sheet:https://focusbiomolecules.com/new-products/1g244-dpp8-9-inhibitor/