Z62954982
- CAS号:1090893-12-1
- 英文名:Rac1 Inhibitor II
- 中文名:Z62954982
- CBNumber:CB92684115
- 分子式:C20H21N3O5S
- 分子量:415.46
- MOL File:1090893-12-1.mol
- 储存条件 :-20C
- 溶解度 :Soluble in DMSO
- 形态 :Off-white solid
- 颜色 :White to off-white
Z62954982性质、用途与生产工艺
- 生物活性 Z62954982 (ZINC08010136) 是一种强效的、选择性的、细胞渗透性强的 Rac1 (IC50=12 μM) 抑制剂,比 NSC23766 (HY-15723A) (IC50=50 μM) 有效性强 4 倍。Z62954982 干扰 Rac1/Tiam1 复合物,降低活性 Rac1 (GTP 结合的 Rac1) 的细胞质水平,而不影响其他 Rho GTPases (如,Cdc42 或 RhoA) 的活性。
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体外研究
Z62954982 (5-100 μM; 4 hours) reduces the intracellular levels of Rac1- GTP in a concentration-dependent manner,and shows the most potent inhibitory action with an IC 50 of 12.2 μM in Human SMCs.Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs.Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers.
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体内研究
Z62954982 (intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks) has no obvious signs of toxicity and decreases both phosphorylation of p38 as well as secreted IL-6 in PASMCs in response to hypoxia in both abr -/- and bcr -/- mice.
Animal Model: Male bcr -/- , abr -/- and wt mice (8 to 10-week-old littermates) are exposed to hypoxia (10% O2) or normoxia (21% O2) for 3 weeks Dosage: 10 mg/kg or 20 mg/kg Administration: Intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks Result: Promoted phosphorylation of p38 MAPK and increased IL-6 in Hypoxia in mice.
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