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PAD1 inhibitor 1

Chemical Structure : PAD1 inhibitor 1

CAS No.: 2369045-71-4

PAD1 inhibitor 1

Catalog No.: PC-20329Not For Human Use, Lab Use Only.

PAD1 inhibitor 1 is a potent selective Protein Arginine Deiminase 1 (PAD1) inhibitor with IC50 of 18 uM for RFA labelling of PAD1 inhibition, kinact/KI value of 10,400 ± 2,380 M-1min-1.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PAD1 inhibitor 1 is a potent selective Protein Arginine Deiminase 1 (PAD1) inhibitor with IC50 of 18 uM for RFA labelling of PAD1 inhibition, kinact/KI value of 10,400 ± 2,380 M-1min-1.
PAD1 inhibitor 1 exhibits 74-fold selectivity for PAD1 over the other PADs.
PAD1 inhibitor 1 inhibit histone H3 citrullination in a dose-dependent manner with EC50 of 14.5 uM in HEK293TPAD1 cells in the presence of calcium.

Physicochemical Properties

M.Wt 635.22
Formula C20H20FI2N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(1-(1H-benzo[d]imidazol-2-yl)-4-(2-fluoroacetimidamido)butyl)-2-hydroxy-3,5-diiodobenzamide

References

1. Mondal S, et al. Angew Chem Int Ed Engl. 2019 Sep 2;58(36):12476-12480.

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