| Description | YM-254890, a macrocyclohexapeptide isolated from Chromobacterium sp, is a selective and potent inhibitor of Gαq/11 protein, inhibits ADP-induced platelet aggregation and inhibits G protein signaling. |
| In vitro | 方法：使用稳定表达人类 P2Y1 或 P2Y12 受体的 C6-15 细胞检查 YM-254890 对 P2Y1 和 P2Y12 信号转导通路的影响。结果：2MeSADP 刺激 P2Y1-C6-15 细胞会导致细胞内钙动员增加。在该测定中，YM-254890 抑制 [Ca2+]i 的增加（IC50：0.031 μM）。然而，40 μM 的 YM-254890 不会影响 2MeSADP 诱导的对 P2Y12-C6-15 细胞中福斯高林刺激的腺苷酸环化酶活性的抑制作用 [1]。 |
| Synonyms | YM254890, YM 254890 |
| molecular weight | 960.08 |
| Molecular formula | C46H69N7O15 |
| CAS | 568580-02-9 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: DMSO: 30 mg/mL (31.25 mM), Sonication is recommended. |
| References | 1. Taniguchi M, et al. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666. J Antibiot (Tokyo). 2003 Apr;56(4):358-63. 2. Zhang H, et al. Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. Eur J Med Chem. 2018 Aug 5;156:847-860. |