2. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis PI3K/Akt/mTOR
  3. PROTACs Sirtuin Apoptosis Akt mTOR
  4. 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.

PROTAC Sirt2 Degrader-2

PROTAC Sirt2 Degrader-2 Chemical Structure

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PROTAC Sirt2 Degrader-2 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7 SIRT4

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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  • References

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Description

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[1]. (Pink: SIRT3 ligand (HY-19339); Blue: Cereblon ligand (HY-A0003); Black: linker).

IC50 & Target[1]

SIRT2

 

Cereblon

 

In Vitro

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.

PROTAC Sirt2 Degrader-2 Related Antibodies

Western Blot Analysis[1]

Cell Line: A2780 ovarian cancer cells
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM
Incubation Time: 6 h, 9 h, 12 h, 24 h, 36 h, 48 h
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).

Cell Cycle Analysis[1]

Cell Line: A2780 ovarian cancer cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 36 h
Result: Induced cell cycle arrest in A2780 cells during the S and G2/M phases.
In Vivo

PROTAC Sirt2 Degrader-2 (Compound W10) (3-10 mg/kg, i.p., once every two days) significantly inhibits tumor growth in A2780 xenograft mice without showing significant toxicity, and also effectively degrades SIRT2 protein in vivo[1].

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

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].
Dosage: 3 mg/kg, 5 mg/kg, 10 mg/kg
Administration: I.p., once every two days
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.
Molecular Weight

682.83

Formula

C37H42N6O5S
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
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
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PROTAC Sirt2 Degrader-2 Related Classifications

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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:

PROTAC Sirt2 Degrader-2PROTACsSirtuinApoptosisAktmTORPKBProtein kinase BMammalian target of RapamycinSIRT2AKT/mTOR signaling pathwayPROTACOvarian cancerOCDrug resistanceInhibitorinhibitorinhibit

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