For research use only. Not for therapeutic Use.
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 (IC<sub>50</sub> = 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 (Item No. <span class=/itemid/>17488</span>), which demonstrates an IC<sub>50</sub> value of 50 nM. GSK199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils.
| Catalog Number | R065526 |
| CAS Number | 1549811-53-1 |
| Synonyms | [(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, monohydrochloride |
| Molecular Formula | C₂₄H₂₉ClN₆O₂ |
| Purity | ≥95% |
| Target | Protein Arginine Deiminase |
| Storage | -20°C |
| InChI | InChI=1S/C24H28N6O2.ClH/c1-4-30-19(12-15-7-5-9-26-22(15)30)23-27-18-11-16(13-20(32-3)21(18)28(23)2)24(31)29-10-6-8-17(25)14-29;/h5,7,9,11-13,17H,4,6,8,10,14,25H2,1-3H3;1H/t17-;/m1./s1 |
| InChIKey | KRGMIOKDGHBYQE-UNTBIKODSA-N |
| SMILES | O=C(N1C[[email protected]](N)CCC1)C2=CC(OC)=C3N(C)C(C4=CC5=CC=CN=C5N4CC)=NC3=C2.[H]Cl |
| Reference | 1.Jones, J.E.,Causey, C.P.,Knuckley, B., et al. Protein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential. Curr. Opin. Drug Discov. Devel. 12(5), 616-627 (2009). |
