PROTAC Sirt2 Degrader-2
PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer.
(Pink: SIRT3 ligand (HY-19339); Blue: Cereblon ligand (HY-A0003); Black: linker).
For research use only. We do not sell to patients.
- Formula: C37H42N6O5S
- Molecular Weight:682.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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SIRT2 |
Cereblon |
PROTAC Sirt2 Degrader-2 (Compound W10) (72 h) exhibits potent antiproliferative activity and high selectivity against various ovarian cancer cell lines, including SKOV3 (IC50 = 0.33 μM), OVCAR3 (IC50 = 0.25 μM), and A2780 (IC50 = 0.08 μM) ovarian cancer cells, while showing lower toxicity against normal cells IOSE80 (CC50 = 2.64 μM)[1].
PROTAC Sirt2 Degrader-2 (0.01-20 μM, 6-48 h) efficiently and selectively degrades SIRT2 protein in A2780 ovarian cancer cells. The mechanism is concentration- and time-dependent, but a hook effect occurs at high concentrations[1].
PROTAC Sirt2 Degrader-2 (1 h) increases the thermal stability of the SIRT2 protein in A2780 ovarian cancer cells, indicating that PROTAC Sirt2 Degrader-2 directly binds to SIRT2 and stabilizes its structure[1].
PROTAC Sirt2 Degrader-2 (0.01-5 μM, 14 days) inhibits colony formation in A2780 cells in a concentration-dependent manner[1].
PROTAC Sirt2 Degrader-2 (0.01-10 μM, 36 h) induces cell cycle arrest in A2780 cells during the S and G2/M phases[1].
PROTAC Sirt2 Degrader-2 (0.01-10 μM, 36 h) induces early and late apoptosis in A2780 cells in a concentration-dependent manner, with late apoptosis being more significant[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780 ovarian cancer cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM
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Incubation Time:6 h, 9 h, 12 h, 24 h, 36 h, 48 h
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Result:Degradation was concentration-dependent (effective at 0.01 μmol/L, optimal at 1 μM, and exhibited a hook effect at 20 μM).
Degradation was time-dependent (significant effect after 36 hours).
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Cell Line:A2780 ovarian cancer cells
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Concentration:0.01 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:36 h
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Result:Induced cell cycle arrest in A2780 cells during the S and G2/M phases.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5 × 106 cells human ovarian cancer cell line A2780 were injected subcutaneously into the right axillary region of female BALB/c nude mice (4 weeks old)[1].
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Dosage:3 mg/kg, 5 mg/kg, 10 mg/kg
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Administration:I.p., once every two days
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Result:Significantly inhibited the growth of ovarian cancer xenografts.
Mice maintained stable body weight.
Effectively degraded SIRT2 protein in vivo.
The proportion of Ki-67 positive cells was significantly reduced, indicating that tumor cell proliferation was inhibited.
Chemical Information
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Molecular Weight 682.83
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Formula C37H42N6O5S
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SMILES
CC(C)(C)C1=CC=C(C(NC(NC2=CC=C(NC(CCCCCNC3=C(CN(C4C(NC(CC4)=O)=O)C5=O)C5=CC=C3)=O)C=C2)=S)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
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