TYMJ-01
TYMJ-01 is a fluorescent probe and eEF2K degrader. TYMJ-01 induces dose-dependent and specific degradation of eEF2K via the ubiquitin-proteasome pathway, with a DC50 of 82 nM. TYMJ-01 inhibits the proliferation, migration and invasion of triple-negative breast cancer cells. TYMJ-01 enables dynamic fluorescent imaging of eEF2K degradation in triple-negative breast cancer cells; it enhances the anti-tumor activity of Paclitaxel (HY-B0015). TYMJ-01 can be used for the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3109321-90-3
- Formula: C27H28N6O4S
- Molecular Weight:532.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CaMK III/eEF-2K 82 nM (DC50) |
Bcl-2 |
In Vitro
TYMJ-01 (500 nM; 3-48 h) enables real-time visualization of eEF2K degradation in immobilized MDA-MB-231 cells. Its fluorescence intensity decreases with increasing incubation duration from 3 to 48 h, and it colocalizes with nuclear eEF2K[1].
TYMJ-01 (10 μM; 1-48 h) enables real-time visualization of eEF2K degradation in live MDA-MB-231 cells. Its fluorescence intensity peaks at 6 h and then decreases, with no associated cell damage[1].
TYMJ-01 (500 nM; 24 h) exhibits extremely low single-agent cytotoxicity, but it significantly enhances the anti-tumor activity of Paclitaxel in MDA-MB-231 cells[1].
TYMJ-01 (0.2-1.0 μM; 24 h) inhibits the proliferation of MDA-MB-231 cells[1].
TYMJ-01 (0.2-1.0 μM; 48 h) induces G1-phase cell cycle arrest in MDA-MB-231 cells by downregulating key cell cycle regulators[1].
TYMJ-01 (200 nM; 48 h) inhibits the migration of MDA-MB-231 cells by downregulating key migration-related regulatory factors[1].
TYMJ-01 (4.12-1000 nM; 24 h) downregulates the expression of proliferation-, survival- and migration-related proteins c-Myc, Bcl-2 and N-cadherin in a dose-dependent manner in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MDA-MB-231 cells
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Concentration:500 nM
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Incubation Time:3, 6, 12, 24, 48 h
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Result:Showed decreasing green fluorescence intensity (corresponding to eEF2K binding) over incubation time, which correlated with decreasing red fluorescence from anti-eEF2K antibody.
Co-localized fluorescence with DAPI-stained nuclei, confirming nucleoplasmic distribution of eEF2K binding.
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Cell Line:MDA-MB-231 cells
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Concentration:500 nM (alone or in combination with paclitaxel 10 nM)
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Incubation Time:24 h
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Result:Had minimal impact on cell viability when used alone.
Increased the cell inhibitory rate by nearly 25% when combined with paclitaxel (10 nM) compared to paclitaxel alone.
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Cell Line:MDA-MB-231 cells
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Concentration:0.2, 0.5 and 1.0 μM(24 h, EdU assay); not specified (10 days, colony formation assay)
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Incubation Time:24 h (EdU assay); 10 days (colony formation assay)
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Result:Markedly reduced the proportion of EdU-positive cells.
Significantly suppressed colony formation capacity.
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Cell Line:MDA-MB-231 cells
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Concentration:0.2, 0.5 and 1.0 μM
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Incubation Time:48 h
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Result:Increased the proportion of cells in the G1 phase and decreased the proportion of cells in the S phase in a dose-dependent manner.
Downregulated mRNA expression of cell cycle-related genes cyclinD, cyclinE, CDK4, and CDK6.
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Cell Line:MDA-MB-231 cells
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Concentration:200 nM
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Incubation Time:48 h
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Result:Markedly reduced the wound closure rate.
Downregulated mRNA and protein expression of migration-related genes/proteins N-cadherin, E-cadherin, Vimentin, and c-Myc.
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Cell Line:MDA-MB-231 cells
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Concentration:4.12, 12.35, 37, 111, 333 and 1000 nM
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Incubation Time:24 h
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Result:Induced dose-dependent downregulation of c-Myc, Bcl-2, and N-cadherin protein levels.
Chemical Information
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CAS No. 3109321-90-3
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Molecular Weight 532.61
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Formula C27H28N6O4S
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SMILES
CC1=C(C=C(C=C1)N2N=C(C(N(C2=O)CCCNS(=O)(C3=C4C=CC=C(C4=CC=C3)N(C)C)=O)=O)C#N)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Cell invasion
Cell invasion is the ability of cells to migrate from one area to another via the extracellular matrix. Cell invasion is the response of normal and cancer cells to chemical and mechanical stimuli. Before migrating to a new region, the extracellular matrix is degraded by proteases within the cell. Cell invasion often occurs during wound repair, vascularization and inflammation, abnormal tissue invasion, and tumor cell metastasis.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TYMJ-01 Related Classifications
HY-181506 Related Classifications
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