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Chemical Structure : 1G244
CAS No.: 847928-32-9
Catalog No.: PC-49843Not For Human Use, Lab Use Only.
1G244 is a potent and selective DPP8/9 inhibitor with IC50 of 14/53 nM and Ki of 0.9/4.2 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 25 mg | $148 | In stock | |
| 50 mg | $238 | In stock | |
| 100 mg | Get quote |
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1G244 is a potent and selective DPP8/9 inhibitor with IC50 of 14/53 nM and Ki of 0.9/4.2 nM, respectively.
1G244 did not inhibit DPP-IV, FAP, or DPP2 with IC50 value of >100 uM.
1G244 was a slow-tight binding competitive inhibitor of DPP8, but it was a competitive and reversible inhibitor of DPP9.
1G244 blocks adipogenesis in preadipocyte 3T3-L1 and 3T3-F422A, while DPP4 and FAP inhibitors have no effect.
1G244 demonstrated anti-myeloma effects on several cell lines and CD138+ cells from patients as well as in murine xenograft model.
| M.Wt | 504.58 | |
| Formula | C29H30F2N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
|
| Chemical Name/SMILES |
(S)-2-amino-4-(4-(bis(4-fluorophenyl)methyl)piperazin-1-yl)-1-(isoindolin-2-yl)butane-1,4-dione |
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1. Sato T, et al. Sci Rep. 2019 Dec 2;9(1):18094.
2. Wu JJ, et al. Biochem Pharmacol. 2009 Jul 15;78(2):203-10.
3. Han R, et al. Sci Rep. 2015 Aug 5;5:12348.
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