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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Dipeptidyl Peptidase (DPP)-1G244
1G244

Chemical Structure : 1G244

CAS No.: 847928-32-9

1G244 (DPP8/9 inhibitor 1G244)

货号: 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.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 504.58
分子式 C29H30F2N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
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

参考文献

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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