2. Cell Cycle/DNA Damage Apoptosis
  3. Deubiquitinase Apoptosis
  4. LLK203

LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model.

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LLK203 Chemical Structure

LLK203 Chemical Structure

CAS No. : 2758090-62-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

LLK203 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

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USP1 USP2 USP7 USP8 USP30 UCHL1

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Description

LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model[1].

IC50 & Target[1]

USP2

0.89 μM (IC50)

USP8

0.52 μM (IC50)

In Vitro

LLK203 (0-100 μM; 36 h) demonstrates high inhibitory activity on MCF-7 cells (IC50=3.4 μM) compared with ML364 (IC50=9.3 μM). LLK203 demonstrates a 4-fold increase in USP2 activity and a 9-fold increase in USP8 activity compared to ML364 (HY-100900)[1].
LLK203 (10-50 μM; 24 h) increases the ratio of apoptotic cells and remaines largely in G1 phas on MCF-7 cells[1].
LLK203 (2-50 μM; 24 h) can degrade various proteins (MDM2, Cyclin D1, Her2, ERα) in a dosedependent manner[1].
LLK203 (2-50 μM; for 7 days) shows a robust ability of inhibiting clone formation at the concentration of 10 μM[1].

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

LLK203 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 and MCF10A cells
Concentration: 0-100 μM
Incubation Time: 36 h
Result: Exhibited lower cytotoxicity towards normal cells (MCF10A; IC50=20.4 μM), while demonstrating higher inhibitory activity on BC cells (MCF-7; IC50=3.4 μM).

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10, 30, 50 μM
Incubation Time: 24 h
Result: Increased the ratio of apoptotic cells.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10, 30, 50 μM
Incubation Time: 24 h
Result: Remained largely in G1 phase.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 2, 5, 10, 30, 50 μM
Incubation Time: 24 h
Result: Could degrade various proteins (MDM2, Cyclin D1, Her2, ERα) in a dosedependent manner.
In Vivo

LLK203 (20 mg/kg; Intraperitoneal; every day; for 23 days) significantly reduces tumor growth in a 4T1 tumor-bearing mice model[1].
Pharmacokinetic Parameters of LLK203 in male Sprague-Dawley rats[1].

Intravenously (5 mg/kg) Orally (50 mg/kg)
Tmax (h) 6
Cmax (ng/mL) 36630 1572
AUC0-t (h∗ng/mL) 60824 19144
T1/2 (h) 20 6.14
CL (mL/h/kg) 58
F (%) 2.2%

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

Animal Model: BALB/c mice subcutaneously inoculated with 4T1 cells[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal; every day; for 23 days
Result: Significantly reduced tumor growth in a 4T1 tumor-bearing mice model.
Molecular Weight

561.69

Formula

C28H23N3O4S3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(OC)C=C1NS(=O)(C2=CC=C(C3=CC=C(C)S3)C=C2)=O)NC4=NC(C5=CC=CC=C5)=CS4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (178.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7803 mL 8.9017 mL 17.8034 mL
5 mM 0.3561 mL 1.7803 mL 3.5607 mL
View the 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.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.

  • Protocol 1

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

    Solubility: ≥ 5 mg/mL (8.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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
DMSO 1 mM 1.7803 mL 8.9017 mL 17.8034 mL 44.5085 mL
5 mM 0.3561 mL 1.7803 mL 3.5607 mL 8.9017 mL
10 mM 0.1780 mL 0.8902 mL 1.7803 mL 4.4509 mL
15 mM 0.1187 mL 0.5934 mL 1.1869 mL 2.9672 mL
20 mM 0.0890 mL 0.4451 mL 0.8902 mL 2.2254 mL
25 mM 0.0712 mL 0.3561 mL 0.7121 mL 1.7803 mL
30 mM 0.0593 mL 0.2967 mL 0.5934 mL 1.4836 mL
40 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1127 mL
50 mM 0.0356 mL 0.1780 mL 0.3561 mL 0.8902 mL
60 mM 0.0297 mL 0.1484 mL 0.2967 mL 0.7418 mL
80 mM 0.0223 mL 0.1113 mL 0.2225 mL 0.5564 mL
100 mM 0.0178 mL 0.0890 mL 0.1780 mL 0.4451 mL
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LLK203 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LLK2032758090-62-7LLK 203LLK-203DeubiquitinaseApoptosisDUBsUSP2USP8ERαbreast cancerMCF-74T1 tumorInhibitorinhibitorinhibit

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