| Bioactivity | AFM-30a is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a binds to PAD2 with an EC50 value of 9.5 μM. AFM-30a also inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a can be used for the research of certain cancers and a variety of autoimmune diseases including rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis[1]. | |||||||||
| Invitro | AFM-30a (compound 30a; 25 μM) has good potency to enter HEK293T/PAD2 cells and covalent modify PAD2 with an EC50 of 9.5 μM[1].AFM-30a shows good ability to inhibit H3 citrullination with an EC50 of 0.4 μM[1]. Cell Viability Assay[1] Cell Line: | |||||||||
| In Vivo | AFM-30a suppresses NLRP3 signaling and decreases airway remodeling in PAD2-/-transgenic mice[2]. | |||||||||
| Name | AFM-30a | |||||||||
| CAS | 2095107-57-4 | |||||||||
| Formula | C24H27FN6O3 | |||||||||
| Molar Mass | 466.51 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Aaron Muth, et al. Development of a Selective Inhibitor of Protein Arginine Deiminase 2. J Med Chem. 2017 Apr 13;60(7):3198-3211. [2]. R. Surolia, et al. Role of PAD2 Regulated Inflammasome Signaling in Arsenic Induced Airway Inflammation and Remodeling. American Journal of Respiratory and Critical Care Medicine 2020;201:A2976. |
AFM-30a
CAS: 2095107-57-4 F: C24H27FN6O3 W: 466.51
AFM-30a is a potent protein arginine deiminase 2 (PAD2) inhibitor and has excellent PAD2-selectivity. AFM-30a binds to P
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