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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Based on 1 publication(s) in Google Scholar

LLK203 Related Antibodies

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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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LLK203 Related Classifications

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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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