2. Others Neuronal Signaling Apoptosis Cytoskeleton
  3. Fluorescent Dye CaMK c-Myc Bcl-2 Family Cadherin
  4. TYMJ-01

TYMJ-01 是一种荧光探针和 eEF2K 降解剂。TYMJ-01 可通过泛素-蛋白酶体通路诱导 eEF2K 呈剂量依赖性的特异性降解，其 DC50 为 82 nM。TYMJ-01 可抑制三阴性乳腺癌细胞的增殖、迁移和侵袭。TYMJ-01 可实现三阴性乳腺癌细胞内 eEF2K 降解的动态荧光成像；可增强 Paclitaxel (HY-B0015) 的抗肿瘤活性。TYMJ-01 可用于三阴性乳腺癌的研究。

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TYMJ-01

TYMJ-01 Chemical Structure

CAS No. : 3109321-90-3

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TYMJ-01 相关抗体

Top Publications Citing Use of Products

查看 CaMK 亚型特异性产品:

查看所有亚型
CaMK II CaMK III/eEF-2K CAMK IV PHK Trio DCAMKL

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

TYMJ-01 (500 nM; 3-48 h) 可对固定化 MDA-MB-231 细胞中 eEF2K 的降解过程进行实时可视化观察，其荧光强度随 3-48 h 孵育时长增加而降低，且与细胞核内的 eEF2K 共定位[1]。
TYMJ-01 (10 μM; 1-48 h) 可对活的 MDA-MB-231 细胞中 eEF2K 的降解过程进行实时可视化观察，其荧光强度在 6 h 时达到峰值后下降，且不会造成细胞损伤[1]。
TYMJ-01 (500 nM; 24 h) 单药细胞毒性极低，但可显著增强 Paclitaxel 在 MDA-MB-231 细胞中的抗肿瘤活性[1]。
TYMJ-01 (0.2-1.0 μM; 24 h) 可抑制 MDA-MB-231 细胞增殖[1]。
TYMJ-01 (0.2-1.0 μM; 48 h) 可通过下调关键细胞周期调控因子，在 MDA-MB-231 细胞中诱导 G1 期细胞周期阻滞[1]。
TYMJ-01 (200 nM; 48 h) 可通过下调关键迁移相关调控因子抑制 MDA-MB-231 细胞的迁移[1]。
TYMJ-01 (4.12-1000 nM; 24 h) 可在 MDA-MB-231 细胞中以剂量依赖方式下调增殖、存活及迁移相关蛋白 c-Myc、Bcl-2 和 N-cadherin 的表达[1]。

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

TYMJ-01 相关抗体:

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.
分子量

532.61

Formula

C27H28N6O4S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

TYMJ-01 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

TYMJ-013109321-90-3TYMJ01TYMJ 01Fluorescent DyeCaMKc-MycBcl-2 FamilyCadherinCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesMyctriple-negative breast cancer cellsubiquitin-proteasome pathwaypaclitaxeleEF2Keukaryotic elongation factor 2 kinaseN-cadherinBcl-2MDA-MB-231 cellsInhibitorinhibitorinhibit

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