产品
编 号:F348122
分子式:C5H3N5O2S3
分子量:261.3
产品类型
结构图
CAS No: 40045-50-9
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产品详情
生物活性:
Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase.
体内研究:
Halicin (Compound 9;25 mg/kg;腹腔注射;雄性BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db小鼠) 处理具有能力恢复糖尿病小鼠模型的胰岛素敏感性。 Halicin 具有良好的微粒体和血浆稳定性 (T1/2=27 分钟)。Animal Model:Male BKS.Cg-+Leprdb/+Leprdb/OlaHsd db/db mice (11-week-old ) injected with insulin
Dosage:25 mg/kg
Administration:Intraperitoneal injection
Result:Resulted in a statistically significant reduction in blood glucose levels.
体外研究:
Halicin (Compound 9) 能够抑制 HeLa 细胞中 TNF-α 刺激的 c-Jun 磷酸化 (EC50=6.23 μM)。 Halicin (25 nM) 预处理人脑微血管内皮细胞 (hCMEC/D3) 可有效减少 LPS 诱导的多形核白细胞 (PMN) 滚动/粘附到 hCMEC/D3,防止 AP-1 的激活,并显著降低 VCAM-1 的表达。