Lificiguat  别名：YC-1; 利非西呱

Lificiguat (YC-1) induces cell cycle arrest and inhibits tumor growth both in vitro and in vivo via the up-regulation of p21 (CIP1/WAP1) expression in HA22T cells. Lificiguat (YC-1) induces apoptosis and inhibits tumour growth of breast cancer cells via down-regulation of EZH2 by activating c-Cbl and ERK. Lificiguat (YC-1) inhibited the aggregation of and ATP release from washed rabbit platelets induced by arachidonic acid (AA), collagen, U46619, platelet-activating factor (PAF), and thrombin in a concentration-dependent manner. Lificiguat (YC-1) also disaggregated the clumped platelets caused by these inducers. Lificiguat (YC-1) increases the catalytic rate of the enzyme and sensitizes the enzyme toward its gaseous activators nitric oxide or carbon monoxide. Lificiguat (YC-1) activation of sGC can occur independently of heme, but that activation is substantially increased when the heme moiety is present in the enzyme.

Compared with tumors from vehicle-treated mice, tumors from YC-1-treated mice were statistically significantly smaller (P<.01 for all comparisons), expressed lower levels of HIF-1 alpha (P<.01 for all comparisons), were less vascularized (P<.01 for all comparisons), and expressed lower levels of HIF-1-inducible genes, regardless of tumor type.