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| Targets |
(R,S)-STT3A/B-IN-1 targets the STT3A and STT3B subunits of the oligosaccharyltransferase (OST) complex. The OST complex catalyzes the transfer of pre-assembled oligosaccharides to asparagine residues of nascent polypeptides in the endoplasmic reticulum, a process known as N-glycosylation. N-glycosylation is essential for proper protein folding, stability, trafficking, and function of many proteins including viral envelope proteins, growth factor receptors, and immune receptors. Inhibition of STT3A/B disrupts this process, leading to misfolding and degradation of glycoproteins.
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| ln Vitro |
In vitro, (R,S)-STT3A/B-IN-1 inhibits N-glycosylation as demonstrated in cell-based assays. The racemic compound shows similar STT3A/B inhibitory activity to the enantiomerically pure STT3A/B-IN-1. In cellular assays, treatment with (R,S)-STT3A/B-IN-1 reduces the glycosylation of model glycoproteins such as vesicular stomatitis virus G protein (VSV-G) or cellular glycosylated proteins. Inhibition of N-glycosylation leads to accumulation of unfolded/misfolded proteins in the endoplasmic reticulum, potentially triggering the unfolded protein response (UPR) and ER stress. The compound has potential applications in research on viral diseases, cancer, and neurodegenerative disorders where protein glycosylation plays a pathogenic role.
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| ln Vivo |
No direct in vivo activity studies have been published for (R,S)-STT3A/B-IN-1. Based on the activity of STT3A/B inhibitors in general, in vivo efficacy would be expected in mouse models of viral infection, cancer, or neurodegenerative diseases. STT3A/B inhibition has been shown to suppress replication of various viruses that rely on host glycosylation machinery for production of viral envelope proteins. However, specific in vivo efficacy data, dosing regimens, and pharmacodynamic markers for (R,S)-STT3A/B-IN-1 are not reported in the available literature. The racemate is used as a reference standard for the active enantiomer.
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| Enzyme Assay |
No specific enzyme/receptor binding protocols have been established for (R,S)-STT3A/B-IN-1 as it targets a protein complex rather than a soluble enzyme. Standard in vitro assays for STT3A/B inhibition use cell-based systems rather than cell-free enzyme assays because OST is a multi-subunit membrane protein complex. Endoglycosidase H (Endo H) sensitivity assays are used to assess N-glycosylation status. Cells are treated with (R,S)-STT3A/B-IN-1 for 6-24 hours, lysed, and proteins are separated by SDS-PAGE. Duplicate samples are treated with Endo H, which digests high-mannose N-glycans only on unprocessed glycoproteins. Shift in migration on western blot indicates loss of glycosylation. Quantification of deglycosylated protein bands is performed. Alternatively, lectin-based assays using concanavalin A or other glycan-binding proteins can measure overall cellular glycosylation levels.
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| Cell Assay |
In vitro cellular protocols for (R,S)-STT3A/B-IN-1 involve culturing mammalian cell lines such as HEK293T, HeLa, or viral-infected cells in DMEM or RPMI-1640 with 10% FBS at 37degC in 5% CO2. Cells are seeded in 6-well or 12-well plates and allowed to reach 70-80% confluence. Cells are treated with varying concentrations of (R,S)-STT3A/B-IN-1 (0.1-10 microM) for 6-24 hours. For glycosylation assessment, cells are lysed in RIPA buffer with protease inhibitors. Protein samples are divided into two: one treated with Endo H (500-1000 U) overnight at 37degC, the other untreated. Samples are analyzed by SDS-PAGE and western blotting using antibodies against glycosylated proteins of interest (e.g., VSV-G, gp120, or transferrin receptor). GAPDH or beta-actin serve as loading controls. All experiments are performed in triplicate. Cell viability is assessed by MTT assay.
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| Animal Protocol |
For in vivo studies of (R,S)-STT3A/B-IN-1, standard animal protocols could involve xenograft models in immunodeficient mice or viral infection models, though specific protocols are not published for this racemate. For anticancer studies, approximately 5×10⁶ cancer cells are injected subcutaneously into nude mice. When tumors reach ~150-200 mm3, mice are treated with (R,S)-STT3A/B-IN-1 administered intraperitoneally at doses of 10-50 mg/kg. For viral infection studies, mice are infected with influenza virus or other enveloped viruses and treated with the inhibitor. Tumor volumes are measured every 2-3 days. N-glycosylation of target proteins in tumor tissues is assessed by Endo H sensitivity assay. All procedures require approval by institutional animal care committees.
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| ADME/Pharmacokinetics |
No direct pharmacokinetic studies have been published for (R,S)-STT3A/B-IN-1. Computed properties include molecular formula C19H21N3O2S, molecular weight 355.45 g/mol, and a predicted logP of approximately 2.0-3.0, suggesting moderate lipophilicity. The compound is likely to be cell-permeable, as STT3A/B inhibitors need to enter cells to reach the endoplasmic reticulum. Solubility data is not reported. For PROTAC applications, the compound is used as a building block. No PK parameters such as half-life, clearance, bioavailability, or volume of distribution are reported for this racemate.
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| Toxicity/Toxicokinetics |
Safety data for (R,S)-STT3A/B-IN-1 is limited. The compound is for research use only and not for human therapeutic applications. As an inhibitor of N-glycosylation, it could have off-target effects on normal protein glycosylation in healthy tissues, potentially leading to cytotoxicity at high concentrations or prolonged exposure. Standard laboratory safety precautions should be followed: wear protective gloves, safety goggles, and a lab coat. Work in a well-ventilated fume hood. Avoid inhalation, ingestion, and contact with skin and eyes. The compound should be stored at -20degC, protected from light and moisture. While specific toxicity data is limited, the compound should be treated as potentially hazardous.
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| References | |
| Additional Infomation |
(R,S)-STT3A/B-IN-1 is the racemic mixture of STT3A/B-IN-1, an inhibitor of the STT3A and STT3B subunits of the oligosaccharyltransferase (OST) complex. N-glycosylation is a critical post-translational modification essential for proper folding and function of many proteins, including viral envelope proteins, growth factor receptors, and immune receptors. STT3A/B inhibitors have potential applications in antiviral therapy, cancer treatment, and neurodegenerative disease research. The racemate is used as a reference standard or control in studies investigating the stereospecificity of STT3A/B inhibition. No clinical trial data is available, and the compound is not approved for human therapy.
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| Molecular Formula |
C19H21N3O2S
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| Molecular Weight |
355.45
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| CAS # |
3067185-00-3
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| Related CAS # |
STT3A/B-IN-1
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| Appearance |
Off-white to light yellow 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.8133 mL | 14.0667 mL | 28.1334 mL | |
| 5 mM | 0.5627 mL | 2.8133 mL | 5.6267 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8133 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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