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P4HB inhibitor 2a

Chemical Structure : P4HB inhibitor 2a

CAS No.: 1401089-31-3

P4HB inhibitor 2a

Catalog No.: PC-25629Not For Human Use, Lab Use Only.

P4HB inhibitor 2a is a tau-aggregate clearing compound (EC50=0.18 uM) that covalently targets protein disulfide isomerase 1 (P4HB, PDIA1), shows maximal tau clearance of 91% with no observable cytotoxicity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

P4HB inhibitor 2a is a tau-aggregate clearing compound (EC50=0.18 uM) that covalently targets protein disulfide isomerase 1 (P4HB, PDIA1), shows maximal tau clearance of 91% with no observable cytotoxicity.
P4HB inhibitor 2a likely undergoes metabolic activation to form a cysteine-reactive species that covalently modifies C397 of P4HB.
P4HB inhibitor 2a aminoindole potently clears aggregates in multiple tauopathy models, activates mild ER stress.

Physicochemical Properties

M.Wt 251.29
Formula C15H13N3O
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

6-amino-N-phenyl-1H-indole-3-carboxamide

References

1. Conway LP, et al. Cell Chem Biol. 2025 Oct 16;32(10):1235-1248.e34.

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