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1G244 | DPP8/9 inhibitor

CAS:
847928-32-9
Catalog Number:
10-4584
Activity:
DPP8/9 inhibitor
Chemical Names:
(S)-2-Amino-4-{4-[bis-(4-fluorophenyl)-methyl]piperazin-1-yl}-1-(1,3-dihydro-isoindol-2-yl)-butane-1,4-dione
Alternate Name:
PTX-1210
Molecular Weight:
504.57
Molecular Formula:
C29H30F2N4O2
Solubility:
Soluble in DMSO (>20 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

1G244 (847928-32-9) is a 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 µM.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.

References/Citations:

  1. Jiaang et al. (2005), Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8; Bioorg.Med.Chem.Lett.15 687
  2. Wu et al. (2009), Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor; Biochem.Pharmacol. 78 203
  3. Okondo et al. (2017), DPP8/9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis; Nat.Chem.Biol. 13 46
  4. Han et al. (2015), Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation; Sci.Rep. 5 12348
  5. Matheeussen et al. (2013), Dipeptidyl peptidases in atherosclerosis: expression and role in macrophage differentiation, activation and apoptosis; Basic Res.Cardiol. 108 350
  6. Waumans et al. (2016), The Dipeptidyl Peptidases 4,8, and 9 in Mouse Monocytes and Macrophages: DPP8/9 Inhibition Attenuates M1 Macrophage Activation in Mice; Inflammation 39 413
1G244 | DPP8/9 inhibitor is also available in the Cellular Metabolism Library.
CAS:
847928-32-9
Catalog Number:
10-4584
Activity:
DPP8/9 inhibitor
Chemical Names:
(S)-2-Amino-4-{4-[bis-(4-fluorophenyl)-methyl]piperazin-1-yl}-1-(1,3-dihydro-isoindol-2-yl)-butane-1,4-dione
Alternate Name:
PTX-1210
Molecular Weight:
504.57
Molecular Formula:
C29H30F2N4O2
Solubility:
Soluble in DMSO (>20 mg/ml)
Physical Properties:
Off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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