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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Arginine Deiminase (PAD)-GSK199
GSK199

Chemical Structure : GSK199

CAS No.: 1549810-81-2

GSK199 (GSK-199)

货号: PC-62216Not For Human Use, Lab Use Only.

GSK199 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay.

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

生物&药学活性

GSK199 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 250 nM in FP binding assay (0.2 mM Ca), 200 nM in PAD4 NH3 release inhibition assay.
GSK199 shows high specificity for PAD4 over PAD1/2/3/6.
GSK199 affects cellular citrullination and mimic the deficiency in NET production in mice.
GSK199 significantly decreases in complement C3 deposition in both synovium and cartilage in mice.

物理化学性质&存储条件

分子量 432.528
分子式 C24H28N6O2
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

[(3R)-3-amino-1-piperidinyl][2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-methanone

参考文献

1. Lewis HD, et al. Nat Chem Biol. 2015 Mar;11(3):189-91.

2. Willis VC, et al. Clin Exp Immunol. 2017 May;188(2):263-274.

3. Slade DJ, et al. ACS Chem Biol. 2015 Apr 17;10(4):1043-53.

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