| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Galectin-8
Galectin-8 N-terminal domain (Gal-8N), a carbohydrate-binding protein (lectin) with tandem CRDs (N-terminal and C-terminal) that bind beta-galactoside-containing glycoconjugates, regulating cell adhesion, migration, proliferation, and immune responses. |
|---|---|
| ln Vitro |
In vitro, Galectin-8N-IN-1 (compound 19a) is a potent and selective galectin-8N inhibitor with a Kd value of 1.8 uM. It is a galectin-8N ligand that selectively targets the N-terminal CRD, disrupting galectin-8-mediated cell adhesion and signaling processes. It can be used to study galectin-8's role in immune cell activation and cancer cell migration.
|
| ln Vivo |
No published in vivo data. As a selective Gal-8N inhibitor, it would be expected to modulate galectin-8 functions in vivo, such as reducing tumor growth, inhibiting metastasis, or modulating immune responses, though this remains to be validated for this specific compound.
|
| Enzyme Assay |
A direct binding fluorescence polarization (FP) assay is used: recombinant human Gal-8N protein is incubated with a fluorescently labeled lactose probe in the presence of serially diluted Gal-8N-IN-1 (0.1-1000 uM). The Kd is calculated from the competition curve. Selectivity over Gal-8C (C-terminal domain) is assessed using the same assay.
|
| Cell Assay |
For in vitro cellular assays, immune cells (e.g., T cells or NK cells) or cancer cell lines are treated with serial dilutions of Gal-8N-IN-1 (1-100 uM). Gal-8N-mediated functions such as cell adhesion to extracellular matrix proteins (fibronectin, laminin) or cell migration (transwell assay) are assessed. Binding of Gal-8N to cell surface glycans can be detected by flow cytometry using a labeled recombinant Gal-8N probe in the presence of the inhibitor.
|
| Animal Protocol |
No published in vivo data. For research use, a syngeneic mouse tumor model (e.g., melanoma or breast cancer) can be used to assess anti-metastatic activity. Gal-8N-IN-1 is administered at 5-30 mg/kg i.p. daily for 2-4 weeks. Primary tumor growth and lung metastasis are evaluated. Immune cell infiltration into tumors (by flow cytometry) and serum cytokine profiles (by ELISA) are also analyzed.
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| ADME/Pharmacokinetics |
Gal-8N-IN-1 has a molecular weight of 529.39 g/mol and a formula of C22H22Cl2N2O7S. DMSO solubility is ≥50 mg/mL (94.45 mM). Detailed PK parameters are not publicly available; as a small molecule, PK properties (half-life, oral bioavailability) are unknown but can be assessed for research purposes.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles are not publicly available. As a selective Gal-8N inhibitor, no severe toxicities are expected at efficacious doses based on the absence of major safety concerns with other galectin inhibitors. No in vivo toxicity studies have been reported.
|
| References | |
| Additional Infomation |
Gal-8N-IN-1 is a research chemical not approved for clinical use. It is referenced in a structure-based design and optimisation study (Eur J Med Chem. 2021 Nov 5;223:113664). It is used to study the selective targeting of the galectin-8 N-terminal domain, immune system modulation, and galectin-8 biology in cancer and host-pathogen interactions.
|
| Molecular Formula |
C22H22CL2N2O7S
|
|---|---|
| Molecular Weight |
529.39
|
| Exact Mass |
528.052
|
| CAS # |
2667628-25-1
|
| PubChem CID |
164610940
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.7
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
34
|
| Complexity |
712
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
CN1C(=NC2=CC=C(C=C21)C(=O)O)CO[C@H]1[C@H]([C@H](O[C@@H]([C@@H]1O)SC1C=CC(=C(C=1)Cl)Cl)CO)O
|
| InChi Key |
FKJDXCHMRVVEIN-DIINWTLSSA-N
|
| InChi Code |
InChI=1S/C22H22Cl2N2O7S/c1-26-15-6-10(21(30)31)2-5-14(15)25-17(26)9-32-20-18(28)16(8-27)33-22(19(20)29)34-11-3-4-12(23)13(24)7-11/h2-7,16,18-20,22,27-29H,8-9H2,1H3,(H,30,31)/t16-,18+,19-,20+,22-/m1/s1
|
| Chemical Name |
2-[[(2R,3R,4S,5S,6R)-2-(3,4-dichlorophenyl)sulfanyl-3,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxymethyl]-3-methylbenzimidazole-5-carboxylic acid
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ≥ 50 mg/mL (94.45 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1 mg/mL (1.89 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 | 1.8890 mL | 9.4448 mL | 18.8897 mL | |
| 5 mM | 0.3778 mL | 1.8890 mL | 3.7779 mL | |
| 10 mM | 0.1889 mL | 0.9445 mL | 1.8890 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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