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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[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 |
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| PAD4-IN-2
PAD4-IN-2 is a PAD4 inhibitor (IC50=1.94 μM). |
| Cl-amidine
Cl-amidine 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. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model. |
| GSK106
GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 and GSK199. |
| BMS-P5 free base
BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 free base blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model. |
| 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. |
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