Cat. No.: HY-107777

LLY-283

7 Cited Publications

Customer Review

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 K_d of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.

For research use only. We do not sell to patients.

Purity: 98.93%
CAS No.: 2040291-27-6
Formula: C₁₇H₁₈N₄O₄
Molecular Weight:342.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LLY-283 Chemical Structure

CAS No.: 2040291-27-6

Size

Price

Stock

Quantity

Sample (0.1mg)

In-stock

(In Japan)

Apply Now

Get Quote Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability Get Quote Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability

Bulk Inquiry

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

PRMT5

All Histone Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2058	IC₅₀	0.013 μM Compound: 1; LLY-283	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	[PMID: 30034588]
A-375	IC₅₀	31.5 nM Compound: 45; LLY-283	Antiproliferation activity against human A-375 cells assessed as cell growth inhibition Antiproliferation activity against human A-375 cells assessed as cell growth inhibition	[PMID: 36274274]
A-375	IC₅₀	32 nM Compound: LLY-283; 1	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	[PMID: 30956011]
A-375	IC₅₀	37 nM Compound: 1; LLY-283	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	[PMID: 30034588]
ARH-77	IC₅₀	0.01 μM Compound: 1; LLY-283	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	[PMID: 30034588]
COLO-829	IC₅₀	0.013 μM Compound: 1; LLY-283	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	[PMID: 30034588]
Daudi	IC₅₀	0.017 μM Compound: 1; LLY-283	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	[PMID: 30034588]
GAK	IC₅₀	0.016 μM Compound: 1; LLY-283	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	[PMID: 30034588]
HCC1937	IC₅₀	0.03 μM Compound: 1; LLY-283	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	[PMID: 30034588]
HEL 92.1.7	IC₅₀	0.003 μM Compound: 1; LLY-283	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	[PMID: 30034588]
IM-9	IC₅₀	0.046 μM Compound: 1; LLY-283	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	[PMID: 30034588]
KARPAS-422	IC₅₀	0.085 μM Compound: 1; LLY-283	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	[PMID: 30034588]
KMS-12-BM	IC₅₀	0.006 μM Compound: 1; LLY-283	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	[PMID: 30034588]
MV4-11	IC₅₀	0.016 μM Compound: 1; LLY-283	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	[PMID: 30034588]
MX1	IC₅₀	>2.5 μM Compound: 1; LLY-283	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	[PMID: 30034588]
NCI-H1651	IC₅₀	>2.5 μM Compound: 1; LLY-283	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	[PMID: 30034588]
NCI-H1930	IC₅₀	>2.5 μM Compound: 1; LLY-283	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	[PMID: 30034588]
NCI-H2122	IC₅₀	0.027 μM Compound: 1; LLY-283	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	[PMID: 30034588]
NCI-H2171	IC₅₀	0.01 μM Compound: 1; LLY-283	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	[PMID: 30034588]
NUGC-3	IC₅₀	0.017 μM Compound: 1; LLY-283	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	[PMID: 30034588]
OPM-2	IC₅₀	>2.5 μM Compound: 1; LLY-283	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	[PMID: 30034588]
OVCAR-3	IC₅₀	0.032 μM Compound: 1; LLY-283	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	[PMID: 30034588]
Rec1	IC₅₀	0.022 μM Compound: 1; LLY-283	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	[PMID: 30034588]
RPMI-8226	IC₅₀	0.009 μM Compound: 1; LLY-283	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	[PMID: 30034588]
Sf9	IC₅₀	9.5 nM Compound: LLY-283; 1	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	[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	[PMID: 30034588]

In Vitro

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 K_d 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.

In Vivo

LLY-283 (20 mg/kg; p.o., QD (once a day)) causes a significant inhibition on tumor growth in mice bearing A375 cells after treatment for 28 days^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2040291-27-6
Appearance Solid
Molecular Weight 342.35
Formula C₁₇H₁₈N₄O₄
Color White to off-white
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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All

Sort by:

Journal Impact Factor

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
Adv Sci (Weinh)

Interferon-Driven Biomarkers and Synergistic Therapy for PRMT5 Inhibition in Triple-Negative Breast Cancer. [Abstract]

2025 Nov 19:e05787. PMID: 41255229
Adv Sci (Weinh)

PRMT5 Maintains Homeostasis of the Intestinal Epithelium by Modulating Cell Proliferation and Survival. [Abstract]

2025 Feb 3:e2415559. PMID: 39899687
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
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
bioRxiv

2026 Apr 13.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9210 mL

14.6049 mL

29.2099 mL

5 mM

0.5842 mL

2.9210 mL

5.8420 mL

10 mM

0.2921 mL

1.4605 mL

2.9210 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zahid Q. Bonday, et al. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med. Chem. Lett., 2018, 9 (7), pp 612-617.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

LLY-283

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LLY-283

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LLY-283

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) LLY-283

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LLY-283 Related Classifications

Cat. No.: HY-107777