| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
EC50: 54 nM (furin) Ki: 12 nM (furin)[1]
Furin (a proprotein convertase, PCSK3). SSM3 tetraTFA hydrate is a synthetic inhibitor of furin, with comparable potency against PC6B (Ki=0.004 uM) and PACE4 (Ki=0.041 uM). It shows preferential inhibition of furin over PC7 (Ki=0.595 uM) and over other proteases such as trypsin and MT1-MMP, which are not measurably inhibited. |
|---|---|
| ln Vitro |
In 90 minutes, SR 142948 (1 µM) CHO-hNT1-R cells express c-fos and krox24 less frequently when dihydrochloride is present [1]. Inhibiting the binding of [125I-Tyr3]NT to h-NTR1-CHO and HT 29 cell membranes, SR 142948 (0-1 µM; 1 hour) dihydrochloride demonstrates good antagonistic activity, with IC50s of 1.19 and 0.32 nM, respectively [2]. h-NTR1-CHO and HT 29 cells' NT-stimulated IP1 synthesis is inhibited in a concentration-dependent manner by SR 142948 (0-1 µM; 30 min) dihydrochloride [2]. For h-NTR1-CHO cells, SR 142948 (1, 10 nM; 60-80 sec) dihydrochloride inhibits the intracellular calcium mobilization triggered by NT [2].
SSM3 tetraTFA hydrate inhibits furin cleavage of the Pyr-RTKR-AMC substrate with an EC50 of 54 nM in vitro. It blocks furin-dependent conversion of protective antigen-83 (PA83) to PA63 in a dose-dependent manner (0.1-25 uM), protecting cells from anthrax toxin. The compound inhibits furin more potently than trypsin and MT1-MMP, indicating selectivity. |
| ln Vivo |
In vivo efficacy data for SSM3 tetraTFA hydrate are limited, but it has been shown to protect cells from anthrax toxin by blocking furin activity. Furin inhibitors are being explored for therapeutic applications in cancer and infectious diseases, as furin activates numerous growth factors and bacterial toxins. SSM3 tetraTFA hydrate serves as a research tool for these studies.
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| Enzyme Assay |
Furin enzymatic activity assay: Recombinant human furin (5-10 nM) is incubated with increasing concentrations of SSM3 tetraTFA hydrate (0-1000 nM) in assay buffer (100 mM HEPES, pH 7.0, 1 mM CaCl2, 0.5% Triton X-100, 1 mM 2-mercaptoethanol) for 10 min at 37degC. A fluorogenic furin substrate (e.g., Pyr-RTKR-AMC, 50 uM) is added, and fluorescence is measured (ex=380 nm, em=460 nm) for 30 min. The EC50 is calculated from initial rates. Ki values are determined by varying substrate concentrations.
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| Cell Assay |
Cell-based furin inhibition assay: Cells are seeded in 96-well plates and treated with SSM3 tetraTFA hydrate (0.1-25 uM) for 1-2 h. To assess furin-dependent processing of anthrax toxin, protective antigen-83 (PA83, 1 ug/mL) is added, and cells are incubated for 2-4 h. Conversion of PA83 to PA63 is detected by Western blotting of cell lysates or conditioned media. Alternatively, cell viability is measured by MTT assay following anthrax toxin challenge.
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| Animal Protocol |
Not directly applicable. SSM3 tetraTFA hydrate is a research tool used in cell-based experiments to study furin function. It may be administered to animal models (mice) to evaluate the role of furin in tumor progression or bacterial toxin pathogenesis. Doses of 1-10 mg/kg administered intraperitoneally have been explored in research settings.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for SSM3 tetraTFA hydrate are limited. As a synthetic furin inhibitor (MW 979.7), the TFA salt is used to enhance solubility and stability. It is soluble in DMSO (30 mg/mL). The compound is typically used in vitro, and its in vivo pharmacokinetics have not been extensively characterized. The tetraTFA hydrate form indicates the presence of four TFA salt groups.
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| Toxicity/Toxicokinetics |
Toxicity data for SSM3 tetraTFA hydrate are limited. It has been reported to protect cells from anthrax toxin without significant toxicity. In vitro, the compound shows no measurable inhibition against trypsin and MT1-MMP, suggesting a good selectivity profile and potentially low toxicity. It is intended for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
SSM3 tetraTFA hydrate is a research-grade furin inhibitor derived from 2,5-dideoxystreptamine. It is a valuable tool for studying the role of furin in bacterial toxin activation, cancer progression, and viral infectivity. The compound has not entered clinical trials. For research use only. Store at -20degC, sealed, away from moisture.
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| Molecular Formula |
C30H36F12N12O10.1.5H2O
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|---|---|
| Molecular Weight |
979.70
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| Related CAS # |
SSM3 tetraTFA;2320930-10-5
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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) |
DMSO :~30 mg/mL (~30.62 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0207 mL | 5.1036 mL | 10.2072 mL | |
| 5 mM | 0.2041 mL | 1.0207 mL | 2.0414 mL | |
| 10 mM | 0.1021 mL | 0.5104 mL | 1.0207 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.
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