CAY10526 is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES1), exerting its effects by specifically modulating mPGES1 expression without influencing cyclooxygenase-2 (COX-2). This compound effectively reduces PGE2 production, leading to significant suppression of tumor growth and enhanced apoptosis in melanoma xenografts. CAY10526 downregulates anti-apoptotic proteins BCL-2 and BCL-XL while elevating levels of pro-apoptotic proteins BAX and BAK, along with cleaved caspase-3, promoting cell death. It demonstrates potent cytotoxicity with an IC50 of less than 5 μM in melanoma cell lines expressing mPGES1, making it valuable for cancer research and therapeutic studies.
CAY10526 is a selective inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES1), exerting its effects by specifically modulating mPGES1 expression without influencing cyclooxygenase-2 (COX-2). This compound effectively reduces PGE2 production, leading to significant suppression of tumor growth and enhanced apoptosis in melanoma xenografts. CAY10526 downregulates anti-apoptotic proteins BCL-2 and BCL-XL while elevating levels of pro-apoptotic proteins BAX and BAK, along with cleaved caspase-3, promoting cell death. It demonstrates potent cytotoxicity with an IC50 of less than 5 μM in melanoma cell lines expressing mPGES1, making it valuable for cancer research and therapeutic studies.
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