PROTAC Tubulin degrader-2
PROTAC Tubulin degrader-2 is a cereblon (CRBN)-dependent α/β-tubulin PROTAC degrader with DC50 values of 1.73 μM and 1.38 μM. PROTAC Tubulin degrader-2 can inhibit cancer cells proliferation and migration. PROTAC Tubulin degrader-2 can induce G2/M arrest, apoptosis, ROS accumulation. PROTAC Tubulin degrader-2 can be used for the research of cancer, such as non-small-cell lung cancer.
(Pink: α-Tubulin and β-Tubulin ligand (HY-N2146); Blue: Cereblon ligand (HY-A0003); Black: linker).
For research use only. We do not sell to patients.
- Formula: C40H45N5O10
- Molecular Weight:755.81
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
More
Biological Activity
|
Cereblon |
α-tubulin 1.73 μM (DC50) |
β-tubulin 1.38 μM (DC50) |
PROTAC Tubulin degrader-2 (Compound C02) (0.1-50 μM; 12-48 h) degrades α/β-tubulin in A549 cells with DC50 values of 1.73 μM and 1.38 μM respectively, inhibits proliferation with an IC50 of 0.71 μM[1].
PROTAC Tubulin degrader-2 (0.5-2 μM; 12-48 h) induces G2/M arrest, apoptosis, ROS accumulation, and migration inhibition in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A549 cells
-
Concentration:0.5, 1 and 2 μM
-
Incubation Time:12, 24 and 36 h
-
Result:Increased the proportion of A549 cells in the G2/M phase, reaching 43.1% at 24 h, compared to 9.6% in the untreated control.
Declined the proportion of G2/M cells after 36 h.
-
Cell Line:A549 cells
-
Concentration:0.5, 1 and 2 μM
-
Incubation Time:24 and 48 h
-
Result:Increased the total numbers of late apoptosis cells from 3.9-13.1%.
Chemical Information
-
Molecular Weight 755.81
-
Formula C40H45N5O10
-
SMILES
O=C(NC1=CC=CC2=C1CN(C(CC3)C(NC3=O)=O)C2=O)CCN4CCN(C(COC5=CC(/C=C\C6=CC(OC)=C(OC)C(OC)=C6)=CC=C5OC)=O)CC4
-
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)