MBQ-167, Rac/Cdc42 inhibitor

Product Details

Formal Name: 1-(9-Ethyl-9H-carbazol-3-yl)-5-phenyl-1H-1,2,3-triazole; 9-Ethyl-3-(5-phenylcarbazol-1-yl)carbazole

Molecular Formula: C₂₂H₁₈N₄

Formula Weight: 338.41

CAS Number: 2097938-73-1

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 25 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

Rac/Cdc42 inhibitor

Functions

Dual inhibitor of the Rho GTPases Rac (IC50 = 103 nM) and Cdc42 (IC50 = 78 nM). It inhibits breast cancer cell migration, viability, and mammosphere formation.  MBQ-167 induced polarity loss resulting in 95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells and was active in GFP-HER2-BM, MDA-MB-468, and Hs578t breast cancer cells as well as Mia-PaCa-2 pancreatic cancer cells, SKOV3 ovarian cancer cells, AGS and NCI-N87 gastric cancer cells, and SH-SY5Y neuroblastoma cells. Non-cancerous mammary epithelial MCF10A and epithelial breast cancer MCF-7 cells were resistant to MBQ-167. MBQ-167 inhibited viability and induced apoptosis in gefitinib and lapatinib resistant SKBR3 breast cancer cells. MBQ-167 inhibited triple negative breast cancer tumor growth and lung metastasis in a mouse model. Active in vivo.

Application Procedures

First dissolved in DMSO (up to 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 2 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)