Cayman 5-pH-IAA

5-pH-IAA is a phenylic substituted indole and ligand used for bump and hole, a technique used to study single protein isoforms when familial homology would interfere with other isoform-selective approaches.^1,2 It activates a bump-and-hole-modified protein, transport inhibitor response 1 (TIR1), which forms a PROTAC-associated complex that targets and degrades sister chromatid cohesion 1 (RAD21) and induces cell cycle arrest at the g₂ or M phase in Arabidopsis when used at a concentration of 1 µM.² Intraperitoneal administration of 5-pH-IAA (1, 3, or 10 mg/kg per day) reduces tumor growth via the same process by targeting and degrading bromodomain-containing protein 4 (BRD4) in an HCT116 colorectal cancer xenograft mouse model.

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