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Drug intelligence / Profile preview
1H-indole-2-hydroxy-3-carboxylic acid
- Development stage
- Preclinical
- Modality
- Small Molecules
01
Overview
1H-indole-2-hydroxy-3-carboxylic acid (IHCA) is a natural indole derivative and alkaloid isolated from the caper plant (*Capparis ovata*). It functions as a small molecule MDM2 inhibitor, which stabilizes the tumor suppressor protein p53 and induces p53-mediated apoptosis in cancer cells. Research indicates that IHCA increases the expression of tumor suppressor genes such as P53, PTEN, and RB, while downregulating oncogenic factors like KRAS and cell cycle regulators like CDK4. In vitro studies have demonstrated its efficacy against prostate cancer (LNCaP) and colorectal cancer (Caco-2) cell lines, showing superior binding stability to MDM2 compared to the reference inhibitor Nutlin-3a. It is currently being explored as a lead compound for anticancer drug development.
- Other names
- Indole-2-hydroxy-3-carboxylic acidIndole2-hydroxy-3-carboxylic acidIndole 2-hydroxy-3-carboxylic acid
02
Targets
CDK4 (Cyclin-dependent kinase 4)KRAS (Kirsten rat sarcoma viral oncogene homolog)MDM2 (Mouse double minute 2 homolog)PTEN (Phosphatase and tensin homolog deleted on chromosome ten)RB1 (Retinoblastoma-associated Protein)TP53 (Cellular Tumor Antigen p53 R175H)
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