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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.
| Molecular Weight | 304.34 |
| Formula | C19H16N2O2 |
| CAS Number | 170632-47-0 |
| Solubility (25°C) | DMSO ≥ 36 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Ko FN, et al. Blood. YC-1, a novel activator of platelet guanylate cyclase.
| Related HIF Products |
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| FG-4592 (Roxadustat)
FG-4592 (Roxadustat; ASP1517) is a novel Hypoxia Inducible Factor Prolyl Hydroxylase inhibitor. |
| 2-Methoxyestradiol
2-methoxyestradiol (2-ME2), an endogenous metabolite of 17β -estradiol (E2) with oral activity, is an apoptosis inducer and angiogenesis inhibitor with effective antitumor activity. Methoxyestradiol can also destabilize microtubules. Methoxyestradiol is a potent inhibitor of superoxide dismutase (SOD) and reactive oxygen species (ROS) that can induce autophagy in transformed cell line HEK293, cancer cell line U87 and HeLa. |
| DMOG
DMOG (Dimethyloxaloyl glycine) is an antagonist of α-ketoglutarate cofactor and a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy. |
| IOX2
IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM, >100-fold selectivity over JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH. |
| Hydralazine hydrochloride
Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM. |
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