Z62954982

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

Z62954982 (ZINC08010136) is a potent, selective and?cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982?disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).

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 IC50 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.

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.

——

Cell Cycle/DNA Damage

Rho

Rho

——

——

1090893-12-1

415.46

C20H21N3O5S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 14.29 mg/mL (34.40 mM; 超声助溶 )

O=C(NC1=CC=C(C(=C1)S(=O)(=O)N)C)C=2C=CC=C(OCC=3C(=NOC3C)C)C2

——

(-20℃)

With Ice Pack

≥ 2 years