| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
LY5 targets STAT3 (signal transducer and activator of transcription 3), a transcription factor that plays a critical role in cell proliferation, survival, angiogenesis, and immune response. STAT3 is frequently constitutively activated in many human cancers, including medulloblastoma, and contributes to tumor progression and drug resistance. LY5 inhibits STAT3 phosphorylation, which is a key step in its activation. By inhibiting STAT3 phosphorylation, LY5 prevents the dimerization and nuclear translocation of STAT3, thereby blocking the transcription of STAT3 target genes involved in cell survival and proliferation. The IC50 of LY5 for STAT3 inhibition is 0.5 μM.
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| ln Vitro |
LY5 has inhibitory effects with IC50 values of 0.52, 0.55, and 1.39 μM on RH30, RD2, and U2OS cancer cells, respectively [1]. In human sarcoma cancer cells, LY5 (0.25-1 μM; 16 h) suppresses STAT3 phosphorylation and causes apoptosis [1]. The phosphorylation of STAT3 elicited by IL-6 is inhibited by LY5 (0.25-1 μM; 5 hours) [1].
In vitro studies have demonstrated that LY5 is a potent inhibitor of STAT3. It inhibits STAT3 phosphorylation in medulloblastoma cells, leading to the downregulation of STAT3 target genes. LY5 inhibits cell viability, cell migration, and angiogenesis in medulloblastoma cells. The compound induces apoptosis, as evidenced by the activation of caspases and the cleavage of PARP. The IC50 for STAT3 inhibition is 0.5 μM. These in vitro findings establish LY5 as a valuable tool for studying the role of STAT3 in cancer biology and for validating STAT3 as a therapeutic target. |
| ln Vivo |
In vivo development of breast tumors is inhibited by LY5 (5 mg/kg; intraperitoneally given once daily for 21 days) [1].
In vivo studies have shown that LY5 exhibits antitumor activity. In animal models of cancer, LY5 has been demonstrated to inhibit tumor growth, likely through its effects on STAT3 phosphorylation and downstream signaling pathways. However, specific details regarding the in vivo efficacy of LY5, such as the tumor models used, dosing regimens, and routes of administration, are not extensively detailed in the available literature. The compound's ability to induce apoptosis and inhibit angiogenesis in vitro suggests that it would have similar effects in vivo. LY5 is used in cancer research to study the role of STAT3 in tumor progression and to explore the potential of STAT3 inhibition as a therapeutic strategy. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assays for LY5 are designed to measure its inhibition of STAT3. STAT3 is a transcription factor that is activated by phosphorylation. LY5 inhibits STAT3 phosphorylation, which can be measured using various biochemical assays. A common approach is to use a cell-free kinase assay, where purified STAT3 protein is incubated with its upstream kinase (e.g., JAK2) and ATP in the presence of varying concentrations of LY5. The level of phosphorylated STAT3 is then measured using an ELISA or Western blot with a phospho-specific antibody. The IC50 for STAT3 inhibition is determined from the dose-response curve. Alternatively, a fluorescence polarization or TR-FRET assay can be used to measure the binding of LY5 to STAT3 or to measure the inhibition of STAT3-DNA binding. These assays provide a quantitative measure of LY5's potency at its molecular target.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: RH30 and EW8 cell lines Tested Concentrations: 0.25-1 μM Incubation Duration: 16 hrs (hours) Experimental Results: 0.5 μM completely inhibits Tyr705 phosphorylation and dose-dependently reduces the formation of P-STAT3. In vitro cell-based assays for LY5 are used to study its effects on STAT3 signaling and cancer cell biology. A typical assay involves treating medulloblastoma cells or other cancer cell lines with varying concentrations of LY5. STAT3 phosphorylation is measured by Western blotting using a phospho-specific antibody (p-STAT3). Cell viability is assessed using assays such as MTT, CellTiter-Glo, or trypan blue exclusion. Cell migration is measured using wound-healing or transwell migration assays. Angiogenesis is assessed using tube formation assays with endothelial cells. Apoptosis is measured using Annexin V staining, caspase-3/7 activation assays, or TUNEL staining. These cell-based assays confirm that LY5 inhibits STAT3 signaling and exerts anti-cancer effects in vitro. |
| Animal Protocol |
Animal/Disease Models: MDA-MB-231 cancer cells were injected into nude mice [1].
Doses: 5 mg/kg. Route of Administration: intraperitoneal (ip) injection; 5 mg/kg; one time/day; for 21 days. Experimental Results: Inhibited tumor growth and Dramatically diminished tumor size. size. In vivo animal experiments for LY5 would typically be conducted using xenograft models. In a standard protocol, immunodeficient mice are injected subcutaneously with medulloblastoma or other cancer cells. Once tumors have reached a measurable size, the mice are randomized into treatment groups. LY5 is administered by intraperitoneal or oral injection at various doses. Tumor growth is monitored by measuring tumor dimensions with calipers. At the end of the study, tumors are harvested for analysis of STAT3 phosphorylation and apoptosis markers. These studies are used to evaluate the antitumor activity of LY5 and to confirm its mechanism of action in vivo. However, specific in vivo protocols for LY5 are not detailed in the available literature. |
| ADME/Pharmacokinetics |
LY5 has a molecular weight of 329.33 g/mol and a molecular formula of C15H11N3O4S. It is a solid powder with a purity of >98%. LY5 is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C for long-term storage (months to years) or at 0-4°C for short-term storage (days to weeks). The compound has a shelf life of more than 2 years if stored properly. Pharmacokinetic properties such as half-life, bioavailability, and tissue distribution have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for LY5 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. In vitro studies have shown that LY5 inhibits cell viability in cancer cell lines, but its effects on normal cells are not well-documented. The compound's selectivity for cancer cells over normal cells would be an important factor in its safety profile. As with all research chemicals, standard laboratory safety precautions should be followed when handling LY5. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
Structure in the first source
LY5 is a research compound and is not approved for any clinical or therapeutic use. It is a small-molecule inhibitor of STAT3 that acts by inhibiting cell viability, cell migration, and angiogenesis in medulloblastoma cells. LY5 induces apoptosis and inhibits STAT3 phosphorylation. It has an IC50 value of 0.5 μM for STAT3 inhibition. LY5 shows antitumor activity in vivo and can be used for cancer research. The compound is also known as 6-(3-pyridylamino)-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide. LY5 is a valuable tool for studying the role of STAT3 in cancer biology and for validating STAT3 as a therapeutic target. |
| Molecular Formula |
C15H11N3O4S
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|---|---|
| Molecular Weight |
329.33
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| Exact Mass |
329.047
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| CAS # |
1436382-03-4
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| PubChem CID |
71680713
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
635.6±65.0 °C at 760 mmHg
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| Flash Point |
338.2±34.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.717
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| LogP |
0.03
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
638
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C(=O)C=C(C2=O)NC3=CN=CC=C3)C(=C1)S(=O)(=O)N
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| InChi Key |
GSGMKINCHGAOPK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11N3O4S/c16-23(21,22)13-5-1-4-10-14(13)12(19)7-11(15(10)20)18-9-3-2-6-17-8-9/h1-8,18H,(H2,16,21,22)
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| Chemical Name |
5,8-dioxo-6-(pyridin-3-ylamino)naphthalene-1-sulfonamide
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| Synonyms |
LY5; LY 5; LY-5;
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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 | 3.0365 mL | 15.1823 mL | 30.3647 mL | |
| 5 mM | 0.6073 mL | 3.0365 mL | 6.0729 mL | |
| 10 mM | 0.3036 mL | 1.5182 mL | 3.0365 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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| NCT05957146 | NOT YET RECRUITING | Device: Routine hemodialysis | End-stage Kidney Disease | Amsterdam UMC, location VUmc | 2023-08 | |
| NCT03096665 | UNKNOWN STATUS | Diagnostic Test: blood test | Acute Abdomen Cardiovascular Diseases Cerebrovascular Disorders Renal Disease Respiratory Disease |
Hanyang University | 2017-04-01 |
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