GSK199 (hydrochloride) 是一种可逆的选择性 PAD4 抑制剂，在不含钙的情况下，IC50 为 200 nM。
| Cas No. | 1549811-53-1 |
| Canonical SMILES | N[C@H]1CN(C(C2=CC(N=C(C3=CC(C=CC=N4)=C4N3CC)N5C)=C5C(OC)=C2)=O)CCC1.Cl |
| 分子式 | C24H28N6O2•HCl |
| 分子量 | 469 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases. GSK199 is a reversible inhibitor of PAD4 (IC50 = 200 nM) that binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3.It is less potent than the related PAD4 inhibitor GSK484 , which demonstrates an IC50 value of 50 nM. GSK199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils. |
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