1. Others PROTAC Neuronal Signaling Apoptosis Cytoskeleton
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  3. 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.

TYMJ-01

TYMJ-01 Chemical Structure

CAS No. : 3109321-90-3

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Description

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[1].

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.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 500 nM
Incubation Time: 3, 6, 12, 24, 48 h
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.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 500 nM (alone or in combination with paclitaxel 10 nM)
Incubation Time: 24 h
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.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.2, 0.5 and 1.0 μM(24 h, EdU assay); not specified (10 days, colony formation assay)
Incubation Time: 24 h (EdU assay); 10 days (colony formation assay)
Result: Markedly reduced the proportion of EdU-positive cells.
Significantly suppressed colony formation capacity.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.2, 0.5 and 1.0 μM
Incubation Time: 48 h
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.

Cell Migration Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 200 nM
Incubation Time: 48 h
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.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 4.12, 12.35, 37, 111, 333 and 1000 nM
Incubation Time: 24 h
Result: Induced dose-dependent downregulation of c-Myc, Bcl-2, and N-cadherin protein levels.
Molecular Weight

532.61

Formula

C27H28N6O4S

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Product Name:
TYMJ-01
Cat. No.:
HY-181506
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