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  3. 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.

PROTAC Tubulin degrader-2

PROTAC Tubulin degrader-2 Chemical Structure

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Description

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[1]. (Pink: α-Tubulin and β-Tubulin ligand (HY-N2146); Blue: Cereblon ligand (HY-A0003); Black: linker).

IC50 & Target[1]

Cereblon

 

α-tubulin

1.73 μM (DC50)

β-tubulin

1.38 μM (DC50)

In Vitro

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 Cycle Analysis[1]

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.

Apoptosis Analysis[1]

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%.

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
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  • 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.

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Product Name:
PROTAC Tubulin degrader-2
Cat. No.:
HY-181143
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