LEM-14 is a selective inhibitor of NSD2, demonstrating an IC50 of 132 µM. It shows minimal activity against NSD1 and lacks activity towards NSD3. This compound effectively inhibits fibrotic gene expression in non-diabetic bone marrow-derived macrophages (BMDMs) and, when used in combination with ionizing radiation, enhances apoptosis rates and reduces colony formation in colorectal cancer cells. Additionally, LEM-14 has been shown to improve anti-tumor efficacy in Balb/c nude mice with LoVo cell xenografts, making it a promising candidate for research into multiple myeloma and colorectal cancer.
LEM-14 is a selective inhibitor of NSD2, demonstrating an IC50 of 132 µM. It shows minimal activity against NSD1 and lacks activity towards NSD3. This compound effectively inhibits fibrotic gene expression in non-diabetic bone marrow-derived macrophages (BMDMs) and, when used in combination with ionizing radiation, enhances apoptosis rates and reduces colony formation in colorectal cancer cells. Additionally, LEM-14 has been shown to improve anti-tumor efficacy in Balb/c nude mice with LoVo cell xenografts, making it a promising candidate for research into multiple myeloma and colorectal cancer.
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