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HV-118 is a small molecule carbazole derivative and a potent inhibitor of the Rho GTPase Rac (specifically Rac1). Developed as a derivative of the lead compound EHop-016, HV-118 targets the interaction of Rac with its upstream guanine nucleotide exchange factors (GEFs), such as Vav2, thereby preventing Rac activation. In preclinical studies, HV-118 has demonstrated significant efficacy in inhibiting the migration, invasion, and viability of metastatic breast cancer cells (including triple-negative breast cancer lines MDA-MB-231 and MDA-MB-468) at nanomolar concentrations, with minimal toxicity to non-cancerous mammary epithelial cells. In vivo, HV-118 has been shown to reduce tumor growth and metastasis to the lung and liver in mouse models of breast cancer.
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