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P4HB inhibitor 2b

Chemical Structure : P4HB inhibitor 2b

CAS No.:

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P4HB inhibitor 2b

Catalog No.: PC-25630Not For Human Use, Lab Use Only.

P4HB inhibitor 2b is a tau-aggregate clearing compound (EC50=0.11 uM) that covalently targets protein disulfide isomerase 1 (P4HB, PDIA1), shows maximal tau clearance of >90% with no observable cytotoxicity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

P4HB inhibitor 2b is a tau-aggregate clearing compound (EC50=0.11 uM) that covalently targets protein disulfide isomerase 1 (P4HB, PDIA1), shows maximal tau clearance of >90% with no observable cytotoxicity.
P4HB inhibitor 2b covalently engages P4HB at the C397/C400 active site upon metabolic activation, eliciting an effect that feeds into tau aggregation clearance in multiple model systems.

Physicochemical Properties

M.Wt 414.47
Formula C23H22N6O2
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
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Solubility

10 mM in DMSO
Chemical Name/SMILES

6-amino-N-(4-((2-(3-(but-3-yn-1-yl)-3H-diazirin-3-yl)ethyl) carbamoyl)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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