This study explores the microtubule inhibitor kzl054 targeting β-tubulin polymerization, down-regulating the expression and secretion of TGF-β1 in WPMY-1 cells, and inhibiting EMT transformation in BPH-1 cells, thereby regulating the proliferation and progression of BPH cells in vivo and providing new insights for BPH treatment. Here, TGFB1 is linked to benign prostatic hyperplasia.