Tubulin degrader 2
Tubulin degrader 2 is a tubulin HyT degrader and tubulin polymerization inhibitor, with a DC50 of 4.9 μM against α-tubulin in MCF-7 cells and an IC50 of 7.5 μM for the polymerization of purified recombinant tubulin. Tubulin degrader 2 binds to the colchicine-binding site of tubulin, induces proteasome-dependent degradation of α-tubulin and β-tubulin, inhibits the polymerization of purified recombinant tubulin, and triggers microtubule disruption and cell cycle arrest in cancer cells. Tubulin degrader 2 exhibits antitumor activity in a breast cancer allograft mouse model. Tubulin degrader 2 can be applied in the research of breast cancer, lung cancer, and colorectal cancer.
(Pink: α-Tubulin and β-Tubulin ligand (HY-10340); Blue: HyT ligand (HY-W037850); Black: linker (HY-W008820)).
For research use only. We do not sell to patients.
- Formula: C37H44N4O4
- Molecular Weight:608.77
-
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
α-Tubulin |
β-Tubulin |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.032 μM
|
Antiproliferative activity against human breast adenocarcinoma MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human breast adenocarcinoma MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
38703557 |
| A549 | IC50 |
0.060 μM
|
Antiproliferative activity against human pulmonary carcinoma A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human pulmonary carcinoma A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
38703557 |
| HCT-116 | IC50 |
0.029 μM
|
Antiproliferative activity against human colorectal carcinoma HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human colorectal carcinoma HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
38703557 |
| MCF7 | DC50 |
4.9 μM
|
Degradation of α-tubulin in human breast adenocarcinoma MCF-7 cells incubated for 24 hrs, measured via Western blot analysis.
Degradation of α-tubulin in human breast adenocarcinoma MCF-7 cells incubated for 24 hrs, measured via Western blot analysis.
|
38703557 |
In Vitro
Tubulin degrader 2 (Compound 14b) (72 h) potently inhibits the proliferation of MCF-7, A549, and HCT-116 cells, with IC50 values of 0.032, 0.060, and 0.029 μM, respectively[1].
Tubulin degrader 2 (0.1-5 μM; 24 h) induces a dose-dependent, proteasome-mediated degradation of α-tubulin and β-tubulin in MCF-7 cells, with a DC50 of 4.9 μM for α-tubulin, and this compound binds to the binding site of microtubule-destabilizing agents on tubulin[1].
Tubulin degrader 2 (2 μM; 24 h) induces microtubule fragmentation in MCF-7 cells[1].
Tubulin degrader 2 (0.5-2 μM; 24 h) inhibits the migration of MCF-7 cells in a dose-dependent manner[1].
Tubulin degrader 2 (20-150 nM; 24 h) induces concentration-dependent G2/M phase cell cycle arrest in MCF-7 cells, and the proportion of arrested cells reaches 69.69% at a concentration of 150 nM after 24 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7 cells
-
Concentration:0.1, 0.2, 0.5, 1, 2, 5 μM (24 h treatment); 5 μM (pre-treatment with proteasome inhibitor Bortezomib (HY-10227), proteasome inhibitor MG132 (HY-13259), or microtubule-disrupting agent Colchicine (HY-16569)) prior to 5 μM (24 h treatment)
-
Incubation Time:24 h (treatment); 2 h (pre-treatment) prior to 24 h treatment
-
Result:Induced dose-dependent degradation of α- and β-tubulin.
At 5 μM, reduced α-tubulin levels by approximately 50% (DC50 = 4.9 μM) and β-tubulin levels by approximately 44%.
Pre-treatment with proteasome inhibitors blocked α-tubulin degradation, confirming proteasome-dependent activity.
Pre-treatment with microtubule-disrupting agent reduced α-tubulin degradation, indicating binding to the microtubule-disrupting agent-binding site.
-
Cell Line:MCF-7 cells
-
Concentration:2 μM (24 h treatment); 2 μM (pre-treatment with MG132) prior to 2 μM (24 h treatment)
-
Incubation Time:24 h (treatment); 2 h (pre-treatment) prior to 24 h treatment
-
Result:Caused microtubule fragmentation, characterized by disruption of the microtubule network, formation of short fragments, and uniform tubulin diffusion around the nucleus.
Pre-treatment with MG132 suppressed this fragmentation, resulting in tubulin depolymerization similar to colchicine.
-
Cell Line:human breast adenocarcinoma MCF-7 cells
-
Concentration:20, 50, 100, 150 nM
-
Incubation Time:24 h
-
Result:Induced concentration-dependent G2/M phase cell cycle arrest.
Treatment with 100 nM resulted in 39.41% of cells in G2/M phase, while 150 nM resulted in 69.69% of cells in G2/M phase.
-
Cell Line:human breast adenocarcinoma MCF-7 cells
-
Concentration:0.5, 1, 2 μM
-
Incubation Time:24 h
-
Result:Inhibited MCF-7 cell migration in a dose-dependent manner, with increasing concentrations resulting in significantly reduced wound closure compared to controls.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c (female)[1]
-
Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
-
Administration:i.v.; once every 3 days; 18 days
-
Result:Achieved a tumor growth inhibition (TGI) value of 56.21% at 5 mg/kg.
Achieved a tumor growth inhibition (TGI) value of 66.89% at 10 mg/kg.
Achieved a tumor growth inhibition (TGI) value of 74.27% at 20 mg/kg.
Caused a slight decrease in mouse body weight at 20 mg/kg; no noticeable body weight changes occurred at lower doses.
Showed no visible histopathological changes in lung, liver, heart, kidney, and spleen across all doses compared to the control group.
Chemical Information
-
Molecular Weight 608.77
-
Formula C37H44N4O4
-
SMILES
O=C(CC1=NC=C(C2=CC=C(OCCNC(CCCC(NC3[C@@H]4C[C@@H]5C[C@H]3C[C@@H](C5)C4)=O)=O)C=C2)C=C1)NCC6=CC=CC=C6
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin degrader 2 Related Classifications
HY-161641 Related Classifications
Powered by Bioz