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1090893-12-1

中文名称 Z62954982
英文名称 Rac1 Inhibitor II
CAS 1090893-12-1
分子式 C20H21N3O5S
分子量 415.46
MOL 文件 1090893-12-1.mol
1090893-12-1 结构式 1090893-12-1 结构式

基本信息

英文别名
Rac1 Inhibitor II
Z-62954982,Z62954982
Z62954982 (Synonyms: ZINC08010136)
Rac1 Inhibitor II - CAS 1090893-12-1 - Calbiochem
InSolution Rac1 Inhibitor II, Z62954982 - CAS 1090893-12-1 - Calbiochem
Benzamide, N-[3-(aminosulfonyl)-4-methylphenyl]-3-[(3,5-dimethyl-4-isoxazolyl)methoxy]-

物理化学性质

储存条件-20C
溶解度Soluble in DMSO
形态类白色固体
颜色White to off-white

常见问题列表

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。
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.

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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