| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
Purity: =98.73%
| Targets |
LLL12 targets signal transducer and activator of transcription 3 (STAT3), a transcription factor that plays a critical role in cell proliferation, survival, angiogenesis, and immune evasion. STAT3 is constitutively activated in many cancers and is associated with poor prognosis. LLL12 inhibits STAT3 dimerization, preventing its translocation to the nucleus and subsequent transcriptional activity. By inhibiting STAT3 phosphorylation and downstream target gene expression (e.g., Bcl-xL, Mcl-1, Cyclin D1, VEGF), LLL12 induces apoptosis and inhibits cancer cell growth.
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| ln Vitro |
Cardiovascular cell viability can be inhibited by LLL12 (0.01-1 μM; 72 h) in response to cisplatin (0.5 μM, 2.5 μM) and paclitaxel (0.25 μM, 0.5 μM) [1].
In vitro, LLL12 inhibits STAT3 phosphorylation and downstream target gene expression in various cancer cell lines. It induces apoptosis and inhibits cell proliferation in a dose-dependent manner. The compound has shown activity against a wide range of cancer cell lines, including those from breast, lung, prostate, and pancreatic cancers. Detailed IC50 values for cell growth inhibition are not extensively reported in the available literature, but the compound demonstrates potent anticancer activity. |
| ln Vivo |
In mouse osteosarcoma cell and tumor growth, LLL12 (5 mg/kg; intraperitoneal injection; once daily for 13 days) demonstrates potent growth inhibitory action [2].
In vivo, LLL12 has shown antitumor activity in preclinical models, including xenograft studies in immunodeficient mice. It inhibits tumor growth and induces apoptosis in tumor tissues. The compound has been studied in models of various cancers, including breast, lung, and pancreatic cancer. Detailed in vivo efficacy data are not extensively reported in the available literature, but the compound has demonstrated potential as an anticancer agent. |
| Enzyme Assay |
Non-cell-based assays for LLL12 include STAT3 dimerization assays using purified STAT3 protein. The compound is incubated with STAT3, and dimerization is assessed using gel electrophoresis, fluorescence polarization, or surface plasmon resonance. STAT3 DNA binding activity can be assessed using electrophoretic mobility shift assays (EMSA) with STAT3 consensus DNA sequences. Inhibition of STAT3 phosphorylation can be assessed using in vitro kinase assays with purified JAK kinases or using cell lysates.
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| Cell Assay |
Western blot analysis [1]
Cell Types: A2780, SKOV3, CAOV-3 and OVCAR5 ovarian cancer cell lines Tested Concentrations: 0.25, 0.5 and 1 μM μM) Phosphorylation of STAT3 (Tyr705) in fluorescently labeled dye lines [1]. A2780 and OVCAR5; SKOV3 and CAOV-3 at 1, 2.5 and 5 μM respectively. Incubation Duration: 72 hrs (hours). Experimental Results: Inhibition of STAT3 phosphorylation at Tyr705. Cellular assays for LLL12 utilize cancer cell lines with constitutively active STAT3 signaling. Cells are treated with the compound at various concentrations for specified durations. STAT3 phosphorylation (p-STAT3) and total STAT3 levels are measured by Western blotting. STAT3 target gene expression (e.g., Bcl-xL, Mcl-1, Cyclin D1, VEGF) is measured by qPCR or Western blotting. Cell proliferation is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated using Annexin V/PI staining or caspase activity assays. |
| Animal Protocol |
Animal/Disease Models: Mouse xenograft SJSA or OS-33 osteosarcoma cells [2]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 13 days Experimental Results: Result in OS-33 and SJSA xenograft mice Tumor volume and tumor mass were Dramatically diminished. In vivo animal models for LLL12 include xenograft studies in immunodeficient mice bearing human cancer cell lines. The compound is administered orally or intraperitoneally at various doses. Tumor growth is monitored by caliper measurements. Tumor tissues are collected for analysis of STAT3 phosphorylation and target gene expression. Apoptosis in tumor tissues is assessed by TUNEL staining or immunohistochemistry for cleaved caspase-3. Toxicity is monitored by body weight and organ histology. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of LLL12 include CAS number 1260247-42-4. The compound is a small molecule STAT3 inhibitor. Detailed PK parameters such as molecular weight, half-life, bioavailability, and solubility are not extensively reported in the available literature. The compound is supplied as a research reagent for laboratory use only.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for LLL12 are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is supplied for research use only. Given its mechanism of STAT3 inhibition, potential effects on normal tissues that depend on STAT3 signaling (e.g., immune system, skin) would be key safety considerations.
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| References |
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| Additional Infomation |
LLL12 is a small molecule STAT3 inhibitor used for cancer research. It has CAS number 1260247-42-4. The compound inhibits STAT3 dimerization and prevents its nuclear translocation, inhibiting STAT3 phosphorylation and downstream target gene expression. It has shown anticancer activity in various cancer cell lines and preclinical models. It is a research tool for studying STAT3 biology and a lead compound for anticancer drug development. It is for research use only.
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| Molecular Formula |
C14H9NO5S
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|---|---|
| Molecular Weight |
303.29
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| Exact Mass |
303.02
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| CAS # |
1260247-42-4
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| PubChem CID |
46911017
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.596
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
566
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CQBHSRLUQDYPBU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H9NO5S/c15-21(19,20)10-6-2-4-8-12(10)14(18)7-3-1-5-9(16)11(7)13(8)17/h1-6,16H,(H2,15,19,20)
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| Chemical Name |
5-hydroxy-9,10-dioxoanthracene-1-sulfonamide
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| Synonyms |
LLL 12; LLL-12; LLL12
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~329.72 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.5 mg/mL (1.65 mM) in 2% DMSO + 40% PEG300 +5% Tween-80 + 53% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2972 mL | 16.4859 mL | 32.9717 mL | |
| 5 mM | 0.6594 mL | 3.2972 mL | 6.5943 mL | |
| 10 mM | 0.3297 mL | 1.6486 mL | 3.2972 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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