For research use only. Not for therapeutic Use.
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)[1][2].
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[1].Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs[1].Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers[2].
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[3].
| Catalog Number | I012103 |
| CAS Number | 1090893-12-1 |
| Synonyms | 3-[(3,5-dimethyl-1,2-oxazol-4-yl)methoxy]-N-(4-methyl-3-sulfamoylphenyl)benzamide |
| Molecular Formula | C20H21N3O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C20H21N3O5S/c1-12-7-8-16(10-19(12)29(21,25)26)22-20(24)15-5-4-6-17(9-15)27-11-18-13(2)23-28-14(18)3/h4-10H,11H2,1-3H3,(H,22,24)(H2,21,25,26) |
| InChIKey | OZZQJOAJXMUXCO-UHFFFAOYSA-N |
| SMILES | CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)OCC3=C(ON=C3C)C)S(=O)(=O)N |
| Reference | [1]. Nicola Ferri,et al. Virtual Screening Approach for the Identification of New Rac1 Inhibitors. J Med Chem. 2009 Jul 23;52(14):4087-90. [2]. Xun E Zhang, et al. Activation of RhoA, but Not Rac1, Mediates Early Stages of S1P-Induced Endothelial Barrier Enhancement. PLoS One. 2016 May 17;11(5):e0155490. [3]. Min Yu, et al. Lack of BCR and Abr Promotes Hypoxia-Induced Pulmonary Hypertension in Mice. PLoS One |
