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Cancer stem cells are pivotal players in tumors initiation, growth, and metastasis. While several markers have been identified, there remain challenges particularly in heterogeneous malignancies like adult soft tissue sarcomas, where conventional markers are inherently overexpressed. Here, we designed BODIPY scaffold fluorescence probes (BD‐IMC‐1, BD‐IMC‐2) that activate via disaggregation targeting for cyclooxygenase (COX), a potential marker for CSCs in sarcoma in clinical pathology. Based on their structures, BD‐IMC‐1 showcased higher susceptibility to disaggregation compared to BD‐IMC‐2, consistent with their selective interaction with COX. Notably, the BD‐IMC‐1 revealed positive cooperativity binding to COX‐2 at sub‐micromolar ranges. Both probes showed significant fluorescence turn‐on upon LPS or PMA triggered COX‐2 upregulation in live RAW264.7, HeLa, and human sarcoma cell line (Saos‐LM2) up to 2‐fold increase with negligible toxicity. More importantly, the BD‐IMC‐1 demonstrated their practical imaging for COX‐2 positive cells in paraffin‐fixed human sarcoma tissue. Considering the fixed tissues are most practiced pathological sample, our finding suggests a potential of disaggregation activated chemosensor for clinical applications. [ABSTRACT FROM AUTHOR]

Disaggregation‐activated turn‐on imaging probes were designed using BODIPY fluorophore and the pan‐COX inhibitor indomethacin, as reported by Woo Young Jang, Jun‐Seok Lee et al. in their Communication (e202405525). The aggregation‐state‐dependent imaging probe demonstrated its practical usages for pan‐COX imaging of fixed clinical tissue from human sarcoma. The cover image was created with BioRender.com...By Kyung Tae Hong; Seung Bin Park; Dhiraj P. Murale; Jung Hoon Lee; Jangsun Hwang; Woo Young Jang and Jun‐Seok LeeReported by Author; Author; Author; Author; Author; Author; Author [Extracted from the article]

Disaggregation‐activated turn‐on imaging probes were designed using BODIPY fluorophore and the pan‐COX inhibitor indomethacin, as reported by Woo Young Jang, Jun‐Seok Lee et al. in their Communication (e202405525). The aggregation‐state‐dependent imaging probe demonstrated its practical usages for pan‐COX imaging of fixed clinical tissue from human sarcoma. The cover image was created with BioRender.com...By Kyung Tae Hong; Seung Bin Park; Dhiraj P. Murale; Jung Hoon Lee; Jangsun Hwang; Woo Young Jang and Jun‐Seok LeeReported by Author; Author; Author; Author; Author; Author; Author [Extracted from the article]