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 (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。
| Cas No. | 1090893-12-1 |
| 别名 | ZINC08010136 |
| Canonical SMILES | O=C(NC1=CC=C(C)C(S(=O)(N)=O)=C1)C2=CC=CC(OCC3=C(C)ON=C3C)=C2 |
| 分子式 | C20H21N3O5S |
| 分子量 | 415.46 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (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]. [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 |
