All AbMole products are for research use only, cannot be used for human consumption.
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. GSK121 is the initial compound identified in a screen for PAD4 inhibitors and was optimized to produce the more potent PAD4 inhibitors, GSK484 and GSK199 . GSK121 was shown to inhibit the citrullination of PAD4 target proteins in a functional assay with an IC50 value of 3.2 µM.
| Molecular Weight | 501.51 |
| Formula | C25H26F3N5O3 |
| CAS Number | 1652591-80-4 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Yuta Sawanaka, et al. Nat Commun. A self-complementary macrocycle by a dual interaction system
[5] V H Rodrigues, et al. Acta Crystallogr C. Betainium trifluoroacetate
| Related PAD Products |
|---|
| GSK484 hydrochloride
GSK484 hydrochloride is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. |
| Cl-amidine hydrochloride
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. |
| GSK199 hydrochloride
GSK199 hydrochloride is a selective PAD4 inhibitor with half-maximum inhibitory concentration (IC50) values, in the absence of calcium, of 200 nM. |
| BB-Cl-Amidine
BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor. |
| BMS-P5
BMS-P5 is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
