LLY-283
Based on 7 publication(s) in Google Scholar
LLY-283, a chemical probe, is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.93%
- No. CAS: 2040291-27-6
- Fòrmula: C17H18N4O4
- Peso molecular:342.35
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LLY-283
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2023 Jan 6;14(1):97. [Abstract]
- Nucleic Acids Res. 2025 Oct 14;53(19):gkaf993. [Abstract]
- Adv Sci (Weinh). 2025 Nov 19:e05787. [Abstract]
- Adv Sci (Weinh). 2025 Mar;12(12):e2415559. [Abstract]
- Neurosci Lett. 2022 Apr 17:776:136576. [Abstract]
- bioRxiv. 2026 Apr 13.
Customer Validation & Images
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WB
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Cell Imaging/Staining
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In Vivo Efficacy Study
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Cell Imaging/Staining
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RT-PCR
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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PRMT5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2058 | IC50 |
0.013 μM
Compound: 1; LLY-283
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Antiproliferative activity against human A2058 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human A2058 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| A-375 | IC50 |
31.5 nM
Compound: 45; LLY-283
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Antiproliferation activity against human A-375 cells assessed as cell growth inhibition
Antiproliferation activity against human A-375 cells assessed as cell growth inhibition
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[PMID: 36274274] |
| A-375 | IC50 |
32 nM
Compound: LLY-283; 1
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Antiproliferative activity against human A375 cells measured after 7 days by cell titer glo-based luminescence assay
Antiproliferative activity against human A375 cells measured after 7 days by cell titer glo-based luminescence assay
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[PMID: 30956011] |
| A-375 | IC50 |
37 nM
Compound: 1; LLY-283
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Antiproliferative activity against human A375 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human A375 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| ARH-77 | IC50 |
0.01 μM
Compound: 1; LLY-283
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Antiproliferative activity against human ARH77 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human ARH77 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| COLO-829 | IC50 |
0.013 μM
Compound: 1; LLY-283
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Antiproliferative activity against human COLO829 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human COLO829 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| Daudi | IC50 |
0.017 μM
Compound: 1; LLY-283
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Antiproliferative activity against human Daudi cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human Daudi cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| GAK | IC50 |
0.016 μM
Compound: 1; LLY-283
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Antiproliferative activity against human GAK cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human GAK cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| HCC1937 | IC50 |
0.03 μM
Compound: 1; LLY-283
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Antiproliferative activity against human HCC1937 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human HCC1937 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| HEL 92.1.7 | IC50 |
0.003 μM
Compound: 1; LLY-283
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Antiproliferative activity against human HEL 92.1.7 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human HEL 92.1.7 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| IM-9 | IC50 |
0.046 μM
Compound: 1; LLY-283
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Antiproliferative activity against human IM9 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human IM9 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| KARPAS-422 | IC50 |
0.085 μM
Compound: 1; LLY-283
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Antiproliferative activity against human KARPAS422 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human KARPAS422 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| KMS-12-BM | IC50 |
0.006 μM
Compound: 1; LLY-283
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Antiproliferative activity against human KMS-12-BM cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human KMS-12-BM cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| MV4-11 | IC50 |
0.016 μM
Compound: 1; LLY-283
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Antiproliferative activity against human MV4-11 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human MV4-11 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| MX1 | IC50 |
>2.5 μM
Compound: 1; LLY-283
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Antiproliferative activity against human MX1 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human MX1 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| NCI-H1651 | IC50 |
>2.5 μM
Compound: 1; LLY-283
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Antiproliferative activity against human NCI-H1651 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human NCI-H1651 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| NCI-H1930 | IC50 |
>2.5 μM
Compound: 1; LLY-283
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Antiproliferative activity against human NCI-H1930 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human NCI-H1930 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| NCI-H2122 | IC50 |
0.027 μM
Compound: 1; LLY-283
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Antiproliferative activity against human NCI-H2122 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human NCI-H2122 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| NCI-H2171 | IC50 |
0.01 μM
Compound: 1; LLY-283
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Antiproliferative activity against human NCI-H2171 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human NCI-H2171 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| NUGC-3 | IC50 |
0.017 μM
Compound: 1; LLY-283
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Antiproliferative activity against human NUGC3 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human NUGC3 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| OPM-2 | IC50 |
>2.5 μM
Compound: 1; LLY-283
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Antiproliferative activity against human OPM2 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human OPM2 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| OVCAR-3 | IC50 |
0.032 μM
Compound: 1; LLY-283
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Antiproliferative activity against human OVCAR3 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human OVCAR3 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| Rec1 | IC50 |
0.022 μM
Compound: 1; LLY-283
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Antiproliferative activity against human Rec1 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human Rec1 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| RPMI-8226 | IC50 |
0.009 μM
Compound: 1; LLY-283
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Antiproliferative activity against human RPMI8226 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human RPMI8226 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
| Sf9 | IC50 |
9.5 nM
Compound: LLY-283; 1
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Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histon
Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (1 to 637 residue) /full length human N-terminal His tagged MEP50 expressed in baculovirus infected Sf9 insect cells assessed as reduction in methyl transfer from [3H]-SAM to biotinylated histon
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[PMID: 30956011] |
| UACC-812 | IC50 |
>2.5 μM
Compound: 1; LLY-283
|
Antiproliferative activity against human UACC-812 cells after 7 days by cell-titer glo based luminescence assay
Antiproliferative activity against human UACC-812 cells after 7 days by cell-titer glo based luminescence assay
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[PMID: 30034588] |
LLY-283 is a potent, oral and selective arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM in vitro and 25 nM in cells, as well as a Kd of 6 nM for PRMT5:MEP50 complex in vitro; LLY-283 inhibits the proliferation of A375 cell with an IC50 of 46 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2040291-27-6
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Appearance Solid
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Peso molecular 342.35
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Fòrmula C17H18N4O4
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Color White to off-white
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SMILES
O[C@H]1[C@@H](O[C@@]([C@@H](C2=CC=CC=C2)O)([H])[C@H]1O)N3C4=NC=NC(N)=C4C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
Dysregulation of PRMT5 in chronic lymphocytic leukemia promotes progression with high risk of Richter's transformation. [Abstract]2023 Jan 6;14(1):97. PMID: 36609611
LLY-283 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jan 6;14(1):97. [Abstract]
LLY-283 (1, 10, 100, 1000 nM; 3, 6, 9, 12 days) induced time and dose-dependent growth inhibition beginning at 100 nM in the HG3 and Mec-1 cell line.
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Nucleic Acids Res
Molecular insights into the Drosophila piRNA pathway via systematic ReLo protein interaction screening and structure prediction. [Abstract]2025 Oct 14;53(19):gkaf993. PMID: 41099705 -
Adv Sci (Weinh)
Interferon-Driven Biomarkers and Synergistic Therapy for PRMT5 Inhibition in Triple-Negative Breast Cancer. [Abstract]2025 Nov 19:e05787. PMID: 41255229
LLY-283 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 19:e05787. [Abstract]
LLY-283 (1 μM; 5 days) decreased the protein expression of SDMA in HCC1806 and Hs-578T cells.
LLY-283 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 19:e05787. [Abstract]
LLY-283 (0, 5, 10, 20, 40, 80, 160 nM; 5 days) inhibited the viability of patient‐derived xenograft organoids (PDXDOs).
LLY-283 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Nov 19:e05787. [Abstract]
LLY-283 (50 mg/kg; ig; 3 days on, 4 days off) inhibited tumor growth of 4T1 tumors in immunocompetent BALB/c mice.
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Adv Sci (Weinh)
PRMT5 Maintains Homeostasis of the Intestinal Epithelium by Modulating Cell Proliferation and Survival. [Abstract]2025 Mar;12(12):e2415559. PMID: 39899687
LLY-283 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(12):e2415559. [Abstract]
LLY-283 (25 nM; 4-5 days) suppressed organoid budding.
LLY-283 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Mar;12(12):e2415559. [Abstract]
LLY-283 (25 nM; 4-5 days) decreased the mRNA expression of Ki67, Pcna, Lgr5, Olfm4, and Ascl2 in mouse small intestinal crypts organoids.
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Neurosci Lett
Inhibition of PRMT5 attenuates cerebral ischemia/reperfusion-Induced inflammation and pyroptosis through suppression of NF-κB/NLRP3 axis. [Abstract]2022 Apr 17:776:136576. PMID: 35278646 -
Solvente y solubilidad
DMSO : 100 mg/mL (292.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 3.57 mg/mL (10.43 mM; ultrasonic and warming and heat to 60°C)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.9210 mL | 14.6049 mL | 29.2099 mL | 73.0247 mL |
| 5 mM | 0.5842 mL | 2.9210 mL | 5.8420 mL | 14.6049 mL | |
| 10 mM | 0.2921 mL | 1.4605 mL | 2.9210 mL | 7.3025 mL | |
| DMSO | 15 mM | 0.1947 mL | 0.9737 mL | 1.9473 mL | 4.8683 mL |
| 20 mM | 0.1460 mL | 0.7302 mL | 1.4605 mL | 3.6512 mL | |
| 25 mM | 0.1168 mL | 0.5842 mL | 1.1684 mL | 2.9210 mL | |
| 30 mM | 0.0974 mL | 0.4868 mL | 0.9737 mL | 2.4342 mL | |
| 40 mM | 0.0730 mL | 0.3651 mL | 0.7302 mL | 1.8256 mL | |
| 50 mM | 0.0584 mL | 0.2921 mL | 0.5842 mL | 1.4605 mL | |
| 60 mM | 0.0487 mL | 0.2434 mL | 0.4868 mL | 1.2171 mL | |
| 80 mM | 0.0365 mL | 0.1826 mL | 0.3651 mL | 0.9128 mL | |
| 100 mM | 0.0292 mL | 0.1460 mL | 0.2921 mL | 0.7302 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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