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| Targets |
Lith-O-Asp targets sialyltransferases (STs), including ST3Gal I, ST3Gal III, and ST6Gal I. It acts as a competitive, selective inhibitor of ST3Gal III/I with a Ki of 1.3 uM. The compound inhibits both alpha-2,3- and alpha-2,6-sialylation pathways. IC50 values range from 12 to 37 uM against ST3Gal I, ST3Gal III, and ST6Gal I. By inhibiting these enzymes, Lith-O-Asp reduces cell surface sialylation, which is involved in tumor cell adhesion, migration, and invasion.
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| ln Vitro |
The findings demonstrated that at test levels of 10, 30, and 60 μM, Lith-O-Asp did not clearly suppress the proliferation of various cancer cell lines. An in vitro activity study demonstrated Lith-O-Asp's capacity to suppress ST3Gal I, ST3Gal III, and ST6Gal I activities. The range of IC50 values is 12–37 μM. The expression of a-2,3- and a-2,6-sialylated antigens on the cell surface was dramatically downregulated, according to flow cytometry. The findings demonstrated that a-2,3- and a-2,3- and a-2,6-sialylated antigens' activity was decreased by Lith-O-Asp. sialic acid transport to target glycoproteins is consequently inhibited by -2,6-sialyltransferase [1].
In vitro studies have shown that Lith-O-Asp is a competitive, selective sialyltransferase inhibitor. It inhibits cancer cell adhesion and invasion by reducing surface sialylation. The compound has IC50 values of 12-37 uM against ST3Gal I, ST3Gal III, and ST6Gal I. It is used to study the role of sialylation in cancer metastasis. By reducing cell surface sialylation, Lith-O-Asp decreases the ability of cancer cells to adhere to and invade the extracellular matrix. Its activity has been characterized in various biochemical and cellular assays. |
| ln Vivo |
Using the IVIS in vivo imaging technology, a significant number of secondary metastatic cancer cells were found in the lung tissue of DMSO control animals 26 days after fat pad inoculation. On the other hand, mice given Lith-O-Asp had fewer lung metastases. All of the DMSO-treated mice had secondary lung metastases confirmed, whereas only three of the eight Lith-O-Asp-treated mice had lung metastases. The average tumor nodules per mouse in the DMSO-treated group was 11±9 nodules, whereas the average tumor nodules per mouse in the Lith-O-Asp-treated group was 2±4 nodules. Moreover, the 4T1-Luc illumination signal on days 7 and 9 was substantially stronger in control mice than in mice injected with cancer cells treated with Lith-O-Asp [1].
In vivo studies of Lith-O-Asp are limited, as the compound is primarily used as a research tool for in vitro studies. As an inhibitor of sialyltransferases, it could potentially inhibit tumor metastasis in animal models. However, specific in vivo efficacy data are not extensively reported. The compound's ability to reduce cell surface sialylation and inhibit cancer cell adhesion and invasion suggests that it could have anti-metastatic activity in vivo. Further studies are needed to characterize its in vivo activity and therapeutic potential. |
| Enzyme Assay |
The in vitro enzyme assay for Lith-O-Asp involves measuring the activity of sialyltransferases (e.g., ST3Gal I, ST3Gal III, ST6Gal I) in the presence of the compound. The enzyme is incubated with a fluorescently or radioactively labeled acceptor substrate and CMP-sialic acid. The transfer of sialic acid to the acceptor is measured. Varying concentrations of Lith-O-Asp are added to determine the IC50 for inhibition. The Ki of 1.3 uM for ST3Gal III/I is determined from the dose-response curves. Data are analyzed using nonlinear regression models.
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| Cell Assay |
In vitro cellular assays for Lith-O-Asp are conducted using cancer cell lines, such as breast cancer or melanoma cells. Cells are treated with varying concentrations of Lith-O-Asp. Cell surface sialylation is assessed by flow cytometry using lectins that specifically recognize sialic acids (e.g., Sambucus nigra lectin, SNA, for alpha-2,6; Maackia amurensis lectin, MAA, for alpha-2,3). Cell adhesion to ECM components, migration (wound-healing or transwell), and invasion (Matrigel) are evaluated. Cell viability is assessed to ensure that the observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo animal studies for Lith-O-Asp are not extensively reported. As a sialyltransferase inhibitor, it could be evaluated in mouse models of cancer metastasis. Typical study designs would involve administration of the compound via intraperitoneal or oral routes in tumor-bearing mice. Tumor growth and metastasis to distant organs (e.g., lung, liver) would be monitored. However, specific published in vivo protocols for Lith-O-Asp are not available in the provided sources. The compound is primarily used as an in vitro research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Lith-O-Asp are not extensively reported. The compound has a molecular weight of 491.66 g/mol and a molecular formula of C28H45NO6. It is soluble in DMSO at 90 mg/mL. Storage recommendations: powder at -20degC for 3 years or 4degC for 2 years; in solvent at -80degC for 6 months or -20degC for 1 month. Specific pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not available. The compound is for research use only.
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| Toxicity/Toxicokinetics |
Toxicology data for Lith-O-Asp are not extensively reported. As an inhibitor of sialyltransferases, the compound's safety profile would be related to its effects on sialylation, which is important for immune function, cell adhesion, and other physiological processes. Inhibition of sialylation could potentially lead to immune dysregulation or other off-target effects. Specific toxicity data, including LD50 values and organ toxicity profiles, are not available. The compound is for research use only.
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| References | |
| Additional Infomation |
Lith-O-Asp is a competitive, selective inhibitor of sialyltransferases with a Ki of 1.3 uM for ST3Gal III/I. It inhibits both alpha-2,3- and alpha-2,6-sialylation pathways with IC50 values of 12-37 uM. The compound reduces cell surface sialylation and inhibits cancer cell adhesion, migration, and invasion. It is used as a research tool for studying cancer metastasis and sialylation biology. Lith-O-Asp has a molecular weight of 491.66 g/mol and a molecular formula of C28H45NO6.
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| Molecular Formula |
C28H45NO6
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| Molecular Weight |
491.660009145737
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| Exact Mass |
491.324
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| CAS # |
881179-02-8
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| PubChem CID |
11698848
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| Appearance |
White to off-white solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
35
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| Complexity |
830
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C[C@@]12[C@@H]([C@H](C)CCC(=O)O)CC[C@H]1[C@@H]1CC[C@@H]3C[C@@H](CC[C@]3(C)[C@H]1CC2)OC(=O)[C@@H](N)CC(=O)O
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| InChi Key |
NUUCRVJEHQBAKP-CNZWOIIDSA-N
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| InChi Code |
InChI=1S/C28H45NO6/c1-16(4-9-24(30)31)20-7-8-21-19-6-5-17-14-18(35-26(34)23(29)15-25(32)33)10-12-27(17,2)22(19)11-13-28(20,21)3/h16-23H,4-15,29H2,1-3H3,(H,30,31)(H,32,33)/t16-,17-,18-,19+,20-,21+,22+,23+,27+,28-/m1/s1
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| Chemical Name |
(4R)-4-[(3R,5R,8R,9S,10S,13R,14S,17R)-3-[(2S)-2-amino-3-carboxypropanoyl]oxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
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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) |
DMSO : ~100 mg/mL (~203.39 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.08 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0339 mL | 10.1696 mL | 20.3393 mL | |
| 5 mM | 0.4068 mL | 2.0339 mL | 4.0679 mL | |
| 10 mM | 0.2034 mL | 1.0170 mL | 2.0339 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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