| Identification | Back Directory | [Name]
Rac1 Inhibitor II | [CAS]
1090893-12-1 | [Synonyms]
Rac1 Inhibitor II
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]- | [Molecular Formula]
C20H21N3O5S | [MDL Number]
MFCD11736677 | [MOL File]
1090893-12-1.mol | [Molecular Weight]
415.46 |
| Chemical Properties | Back Directory | [storage temp. ]
-20C | [solubility ]
Soluble in DMSO | [form ]
Off-white solid | [color ]
White to off-white | [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=CC=C(NC(C2=CC(OCC3=C(C)ON=C3C)=CC=C2)=O)C=C1S(N)(=O)=O |
| Hazard Information | Back Directory | [Uses]
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]. | [General Description]
A cell-permeable isoxazolyl-benzamide compound that is more effective than NSC23766 (Cat. Nos. 553502 & 553508) in inhibiting PDGF-BB- (Cat. No. 521225) induced cellular Rac1 activation (45.8% vs 11.1% inhibition by 4 h pretreatment of the respective compound at 50 μM) in serum-starved SMCs (human aortic smooth muscle cells) by interfering Rac1-Tiam1 interaction, while exhibiting no effect toward cellular Cdc42 and RhoA activation or Rac1 interaction to its effector Pak1. Shown to effectively prevent PDGF-BB-induced membrane ruffling and lamellipodia formation in serum-starved 3T3 cells (4 h pretreatment at 25 μM). Also available in InSolution format (Cat. No. 553512). | [in vivo]
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]. | 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[3] | | 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. |
| [References]
[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. DOI:10.1021/jm8015987
[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. DOI:10.1371/journal.pone.0155490
[3] Min Yu, et al. Lack of BCR and Abr Promotes Hypoxia-Induced Pulmonary Hypertension in Mice. PLoS One DOI:10.1371/journal.pone.0049756 |
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Merck KGaA
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MedChemExpress
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