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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Rac1 Inhibitor W56 TFA targets Rac1, a member of the Rho family of small GTPases. The peptide corresponds to the GEF recognition/activation site of Rac1 (residues 45-60). By binding to this region, it selectively inhibits the interaction between Rac1 and its guanine nucleotide exchange factors (GEFs), including TrioN, GEF-H1, and Tiam. This prevents the exchange of GDP for GTP, thereby blocking Rac1 activation and downstream signaling.
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| ln Vitro |
In vitro, Rac1 Inhibitor W56 TFA inhibits the interaction of Rac1 with the guanine nucleotide exchange factors TrioN, GEF-H1, and Tiam. By preventing Rac1 activation, it blocks downstream signaling pathways involved in cell migration, proliferation, and cytoskeletal reorganization. It is a selective inhibitor of Rac1-GEF interactions, leaving other small GTPases (e.g., Cdc42, RhoA) unaffected. The peptide is a valuable tool for dissecting Rac1-specific functions in various cellular processes.
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| ln Vivo |
In vivo, Rac1 Inhibitor W56 TFA can be used to study the role of Rac1 in animal models of cancer, inflammation, and developmental biology. By inhibiting Rac1 activation, it can suppress tumor cell invasion and metastasis, reduce inflammation, and alter cytoskeletal dynamics. However, specific in vivo efficacy data have not been reported. The peptide is typically delivered using cell-penetrating peptide technology or by direct microinjection.
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| Enzyme Assay |
A cell-free Rac1 activation assay can be performed using a G-LISA or pull-down assay. Purified Rac1 protein (0.5-1 microg) is incubated with a constitutively active GEF (e.g., Tiam1 catalytic domain) and GTPgammaS (100 microM) in the presence of varying concentrations (0.1-100 microM) of Rac1 Inhibitor W56 TFA in assay buffer (20 mM Tris-HCl, pH 7.5, 50 mM NaCl, 1 mM DTT, 5 mM MgCl2). The reaction is stopped after 15-30 min. Activated GTP-bound Rac1 is captured on a plate coated with a Rac1-binding domain (e.g., PAK-PBD) and detected with an anti-Rac1 antibody. The IC50 is calculated.
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| Cell Assay |
A cell-based Rac1 activation assay is performed using the G-LISA or pull-down method. Cells (e.g., fibroblasts or cancer cells) are seeded in 10 cm dishes and treated with Rac1 Inhibitor W56 TFA (10-100 microM) for 2-24 h. The peptide can be delivered using a cell-penetrating peptide tag (e.g., TAT) or a transfection reagent. After treatment, cells are lysed. Activated GTP-bound Rac1 in the lysate is captured using the PAK-PBD domain. The amount of active Rac1 is detected by Western blot using an anti-Rac1 antibody. The effect on downstream signaling is assessed by Western blot for p-PAK and p-cofilin.
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| Animal Protocol |
Rac1 Inhibitor W56 TFA can be studied in mouse models of cancer metastasis. Female BALB/c nude mice (6-8 weeks, n=8-10 per group) are injected intravenously (tail vein) with 1×10⁶ highly metastatic cancer cells (e.g., B16-F10 melanoma). Rac1 Inhibitor W56 TFA (5-20 mg/kg) is administered intraperitoneally daily for 14-21 days. Lungs are harvested, and metastatic colonies are counted. The peptide is expected to reduce the number of lung metastases. The peptide can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline.
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| ADME/Pharmacokinetics |
Rac1 Inhibitor W56 TFA is a peptide with a molecular weight of approximately 2000-2500 Da. The TFA salt form enhances solubility. The powder should be stored at -20degC for up to 3 years. In solution, it is stable for 6 months at -80degC. Specific PK parameters have not been reported. As a peptide, its plasma half-life is expected to be short (minutes to hours). The compound is soluble in DMSO and water.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for Rac1 Inhibitor W56 TFA are available. As a peptide derived from a natural protein sequence, it is expected to have low inherent toxicity. Standard safety precautions for peptide handling should be followed. The compound is not intended for human use. Formal toxicology studies (e.g., 28-day repeat-dose) have not been published.
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| References | |
| Additional Infomation |
Rac1 Inhibitor W56 TFA is a research-grade peptide and is not approved for clinical use. It is a selective inhibitor of Rac1-GEF interactions and is used to study Rac1-mediated signaling in cell migration, proliferation, and cytoskeletal reorganization. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C76H118F3N19O25S
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| Molecular Weight |
1785.95
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| Related CAS # |
Rac1 Inhibitor W56;1095179-01-3
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O :~100 mg/mL (~55.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (55.99 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5599 mL | 2.7996 mL | 5.5993 mL | |
| 5 mM | 0.1120 mL | 0.5599 mL | 1.1199 mL | |
| 10 mM | 0.0560 mL | 0.2800 mL | 0.5599 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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