LLL3
Based on 1 publication(s) in Google Scholar
LLL3 (CLT-005) is an orally effective STAT3 inhibitor. LLL3 blocks STAT3 dimerization, nuclear translocation, and transcription by binding to the SH2 domain. LLL3 induces apoptosis and PARP/caspase-3 cleavage, thereby inhibiting the proliferation and invasion of cancer cells. LLL3 reduces retinal vascular permeability, pro-angiogenic and pro-inflammatory factor levels, ameliorates diabetes-related vision loss and cataracts, and exhibits good biosafety. LLL3 inhibits tumor growth in vivo. LLL3 can be used in research related to glioblastoma, breast cancer, chronic myeloid leukemia, and diabetic retinopathy.
For research use only. We do not sell to patients.
- Purity : 97.20%
- CAS No.: 63972-38-3
- Formula: C16H10O4
- Molecular Weight:266.25
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LLL3
MoreAll Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[2]|
Caspase 3 |
Caspase-7 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
37 μM
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Inhibition of human chronic myeloid leukemia K562 cell viability incubated 24 hrs by WST-1 assay.
Inhibition of human chronic myeloid leukemia K562 cell viability incubated 24 hrs by WST-1 assay.
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19701750 |
| K562 | IC50 |
6.3 μM
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Inhibition of human chronic myeloid leukemia K562 cell viability incubated 48 hrs by WST-1 assay.
Inhibition of human chronic myeloid leukemia K562 cell viability incubated 48 hrs by WST-1 assay.
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19701750 |
| DU-145 | IC50 |
11.3 μM
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Inhibition of human prostate cancer DU145 cell viability incubated 24 hrs by WST-1 assay.
Inhibition of human prostate cancer DU145 cell viability incubated 24 hrs by WST-1 assay.
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19701750 |
| MCF7 | IC50 |
150 μM
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Inhibition of human breast cancer MCF-7 cell viability incubated 24 hrs by WST-1 assay.
Inhibition of human breast cancer MCF-7 cell viability incubated 24 hrs by WST-1 assay.
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19701750 |
In Vitro
LLL3 (20-50 μM; 48 h) inhibits STAT3-specific DNA binding in U373 glioblastoma and MDA-MB-231 breast cancer cells[1].
LLL3 (10-40 μM; 72 h) reduces the viability of U87, U251, and U373 glioblastoma cells[1].
LLL3 (8-200 μM; 24-48 h) inhibits K562 cell viability in a dose- and time-dependent manner[2].
LLL3 (5-20 μM; 24 h) inhibits DU145 cell viability with an IC50 of 11.3 μM[2].
LLL3 (5-80 μM; 24 h) inhibits MCF-7 cell viability only at high concentrations, with an IC50 of 150 μM[2].
LLL3 (40 μM; 24-48 h) combined with Imatinib Mesylate (HY-50946) increases the mortality of K562 cells by 21%-22% compared with Imatinib Mesylate alone[2].
LLL3 (40 μM; 24 h) increases sub-G1 DNA content in K562 cells and enhances IM-induced increases in sub-G1 DNA[2].
LLL3 (20 μM; 48 h) induces PARP cleavage in U87, U251, and U373 glioblastoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U373 glioblastoma and MDA-MB-231 breast cancer cells
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Concentration:20, 30, 40 and 50 μM
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Incubation Time:48 h
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Result:Inhibited STAT3-specific DNA binding activity in U373 glioblastoma and MDA-MB-231 breast cancer cells.
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Cell Line:U87, U251, and U373 human glioblastoma cells
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Concentration:10, 20, 30 and 40 μM
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Incubation Time:72 h
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Result:Decreased cell viability to <25% versus untreated and DMSO control cells.
At 30 μM this compound, cell viability decreased to <10% in U87, U251, and U373 glioblastoma cells.
Decreased cell density was visible by phase contrast microscopy.
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Cell Line:U87 and U373 human glioblastoma cells and normal human bladder smooth muscle cells
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Concentration:20 μM
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Incubation Time:48 h
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Result:High levels of cleaved caspase-3 were observed in U373 and U87 glioblastoma cells, whereas DMSO control and untreated cells had little cleaved caspase-3.
Decreased cell density was evident in this compound-exposed cells.
Induction of cleaved caspase-3 was not observed in normal human bladder smooth muscle cells.
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Cell Line:U87, U251, and U373 human glioblastoma cells
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Concentration:20 μM
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Incubation Time:48 h; 72 h
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Result:U87, U251, and U373 glioblastoma cells exposed to this compound showed high levels of cleaved PARP (Asp214), whereas little PARP cleavage was observed in DMSO control and untreated cells.
GAPDH signal was similar across samples.
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Cell Line:human chronic myeloid leukemia K562 cells
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Concentration:8, 40, 200 μM
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Incubation Time:24 h; 48 h
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Result:Inhibited K562 proliferation in a dose- and time-dependent manner.
IC50 was 37 μM at 24 h and 6.3 μM at 48 h.
At 24 h, bar label values were 8% at 8 μM, 54% at 40 μM, and 63% at 200 μM.
At 48 h, bar label values were 56% at 8 μM, 77% at 40 μM, and 92% at 200 μM.
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Cell Line:human prostate cancer DU145 cells
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Concentration:5, 10, 20 μM
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Incubation Time:24 h
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Result:This compound inhibited DU145 survival with IC50 11.3 μM.
Bar label values were 30% at 5 μM, 47% at 10 μM, and 76% at 20 μM.
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Cell Line:human breast cancer MCF-7 cells
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Concentration:5, 20, 80 μM
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Incubation Time:24 h
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Result:This compound inhibited MCF-7 survival with IC50 150 μM.
Bar label values were 6.5% at 5 μM, 10% at 20 μM, and 29% at 80 μM.
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Cell Line:human chronic myeloid leukemia K562 cells and MBA megakaryocytic cells
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Concentration:40 μM
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Incubation Time:24 h, 48 h
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Result:Co-incubation of 40 μM this compound and 1 μM IM increased the percentage of nonviable K562 cells by 21% at 24 h and 22% at 48 h compared with IM alone.
At 24 h, bar label values were 42% for 40 μM this compound and 67% for 1 μM IM + 40 μM this compound.
At 48 h, bar label values were 68% for 40 μM this compound and 97% for 1 μM IM + 40 μMthis compound.
This compound (40 μM) with IM decreased MBA cell proliferation by 18% at 24 h and 23% at 48 h compared with IM alone.
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Cell Line:human chronic myeloid leukemia K562 cells
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Concentration:40 μM
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Incubation Time:24 h
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Result:28.5% of K562 cells incubated with 40 μM this compound for 24 h showed positive Annexin V-FITC staining.
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Cell Line:human chronic myeloid leukemia K562 cells
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Concentration:40 μM
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Incubation Time:24 h
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Result:This compound increased sub-G1 DNA by 26% over 24 h compared with untreated K562 cells.
This compound together with IM increased sub-G1 DNA content by 25% (41%) compared with IM alone.
In Vivo
LLL3 (125-500 mg/kg/animal; p.o.; once daily; administered continuously for 16 weeks starting 3 days after Streptozotocin injection) delays diabetes-induced vision loss and reduces retinal phosphorylated Stat3 and inflammatory cytokine levels in Streptozotocin-induced diabetic Brown Norway rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude (female, nu/nu)[1]
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Dosage:50 mg/kg
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Administration:intratumoural; single
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Result:Average tumour volume in LLL-3-administered animals was 17.0 mm3.
LLL-3-administered animals had significantly smaller and less hyperintense intracranial tumours and no evidence of contralateral invasion or midline shift.
Median survival time in LLL-3-administered animals was 28.5 days.
Prolonged survival time in the LLL-3 group was 190% compared with the control group.
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Animal Model:Brown Norway (BN) (female, 6-8 weeks old, 126-137 g)[3]
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Dosage:1 µg/eye and 5 µg/eye for vascular permeability; 50 ng/eye and 5 µg/eye for qRT-PCR
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Administration:Intravitreal injection; single administration at 2 weeks post-Streptozotocin
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Result:Retinal vascular permeability was decreased in eyes treated with LLL3 (CLT-005) at doses as low as 1 µg.
At 24 hours after intravitreal injection, 50 ng or 5 µg LLL3 (CLT-005) reduced retinal mRNA expression of LRP-5 and LRP-6; both doses also returned expression of IL-6, TNF-α, TGFβ1, MCP-1, and ICAM-1 to nondiabetic levels.
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Animal Model:Brown Norway (BN) (female, 6-8 weeks old, 126-137 g)[3]
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Dosage:125 mg/kg/animal, 250 mg/kg/animal, and 500 mg/kg/animal
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Administration:p.o. (oral gavage); once daily for 16 consecutive weeks beginning 3 days post-Streptozotocin
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Result:Dose-dependently delayed visual acuity and contrast sensitivity decline in streptozotocin-induced diabetic rats.
Attenuated cataract severity and reduced retinal phosphorylated Stat3 levels.
Lowered blood glucose levels and decreased retinal levels of multiple inflammatory cytokines, including IL-1β, IL-2, IL-6, IFNγ, IL-12, MCP-1, RANTES, and IL-7.
The 500 mg/kg group showed the most prominent effects, maintaining visual acuity through 16 weeks similar to insulin-treated diabetic animals.
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Research Protocol for Inflammation-related Diseases
- Research Protocol for Metabolic Diseases
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
- Cytoplasmic-Nuclear Fractionated Protein Extraction
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Transepithelial/transendothelial electrical resistance assay
- Cell invasion
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 63972-38-3
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Appearance Solid
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Molecular Weight 266.25
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Formula C16H10O4
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Color Light yellow to yellow
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SMILES
O=C1C2=C(C(O)=CC=C2)C(C3=CC=CC(C(C)=O)=C13)=O
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Synonyms
CLT-005
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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NPJ Digit Med
2026 Mar 7;9(1):327. PMID: 41792471
Solvent & Solubility
In Vitro:
DMSO : 20 mg/mL (75.12 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (315 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.7559 mL | 18.7793 mL | 37.5587 mL | 93.8967 mL |
| 5 mM | 0.7512 mL | 3.7559 mL | 7.5117 mL | 18.7793 mL | |
| 10 mM | 0.3756 mL | 1.8779 mL | 3.7559 mL | 9.3897 mL | |
| 15 mM | 0.2504 mL | 1.2520 mL | 2.5039 mL | 6.2598 mL | |
| 20 mM | 0.1878 mL | 0.9390 mL | 1.8779 mL | 4.6948 mL | |
| 25 mM | 0.1502 mL | 0.7512 mL | 1.5023 mL | 3.7559 mL | |
| 30 mM | 0.1252 mL | 0.6260 mL | 1.2520 mL | 3.1299 mL | |
| 40 mM | 0.0939 mL | 0.4695 mL | 0.9390 mL | 2.3474 mL | |
| 50 mM | 0.0751 mL | 0.3756 mL | 0.7512 mL | 1.8779 mL | |
| 60 mM | 0.0626 mL | 0.3130 mL | 0.6260 mL | 1.5649 mL |
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