3126204-69-8
Chemical Structure
PF-3166
- CAS No.: 3126204-69-8
- Formula:C43H42BrClN6O5S
- Molecular Weight:870.25
InChIKey: SZZJHKUNVBZYMT-RGULYWFUSA-N
SMILES: O=C([C@@H]1N(CC2=CC=C3C(N([C@H](C4=CC=CC=C4Br)CC(NC5=CC(NS(=O)(C)=O)=CC=C5C)=O)C(C6=CC=CC(OC7=CC=C(Cl)C=C7)=C6)=N3)=C2)CCC1)NC
Biological Activity: PF-3166 is a non-covalent allosteric PAD2 inhibitor (human PAD2 IC50 = 150-610 nM and 5.47 μM; Kd = 221 nM). PF-3166 induces a conformational change by binding to the PAD2 dimer interface, causing calcium release from the high-affinity site and masking the other calcium-binding site, thereby preventing catalytic activation. PF-3166 exhibits selectivity for PAD2 over PAD3 and PAD4, and inhibits total cellular citrullination and reduces non-histone H3 citrullination. PF-3166 can be used for research on PAD2-related citrullination[1].
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PF-3166 | PF-3166 is a non-covalent allosteric PAD2 inhibitor (human PAD2 IC50 = 150-610 nM and 5.47 μM; Kd = 221 nM). PF-3166 induces a conformational change by binding to the PAD2 dimer interface, causing calcium release from the high-affinity site and masking the other calcium-binding site, thereby preventing catalytic activation. PF-3166 exhibits selectivity for PAD2 over PAD3 and PAD4, and inhibits total cellular citrullination and reduces non-histone H3 citrullination. PF-3166 can be used for research on PAD2-related citrullination. | |||||||||||||||||||||
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