Drug intelligence / Profile preview

dim-c-pphtbu

Development stage
Preclinical
Lead developer
Texas A&M AgriLife Research
Modality
Small Molecules
Administration
Oral
01

Overview

DIM-C-pPhtBu is a synthetic small molecule belonging to the C-DIM (1,1-bis(3′-indolyl)-1-(p-substituted phenyl)methane) class, originally developed for anticancer research. It functions primarily as a peroxisome proliferator–activated receptor gamma (PPARγ) agonist, inhibiting tumor cell proliferation and inducing apoptosis across various cancer types, particularly ovarian and renal cell carcinoma. Its mechanism of action includes PPARγ-dependent activation of cell cycle inhibitors (notably p21) and robust PPARγ-independent effects, including proteasome-dependent down-regulation of cyclin D1 and activation of endoplasmic reticulum (ER) stress. DIM-C-pPhtBu also induces the CCAAT/enhancer-binding protein homologous protein (CHOP) via ER stress and c-Jun N-terminal kinase (JNK) pathways, culminating in upregulation of death receptor 5 (DR5) and extrinsic apoptosis signaling[1][3]. Reported actions include mitochondrial and lysosomal dysfunction, induction of excessive mitosis, and broad cytotoxic activities against multiple tumor cell types[2][5]. The agent exhibits both in vitro and in vivo antitumor activities with minimal reported toxicity in animal studies[1].

Other names
1,1-Bis(3-indolyl)-1-(p-t-butylphenyl)methane3,3'-[[4-(tert-butyl)phenyl]methylene]bis(1H-indole)
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)ANT1/2/3 (Mitochondrial ADP/ATP translocase)

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