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 是一种高效且选择性的 PROTAC 降解剂，靶向 SIRT2。PROTAC Sirt2 Degrader-2 在体外和体内均表现出极强的抗增殖活性。PROTAC Sirt2 Degrader-2 可显著提高 H4K16Ac 水平。PROTAC Sirt2 Degrader-2 可显著抑制克隆形成和迁移，诱导细胞周期阻滞，并促进细胞凋亡 (apoptosis)。PROTAC Sirt2 Degrader-2 通过间接降解 SIRT2 并阻断下游蛋白磷酸化来抑制 AKT/mTOR 信号通路，从而破坏信号级联反应并抑制肿瘤发展。PROTAC Sirt2 Degrader-2 可用于卵巢癌的研究。
(粉色: SIRT3 配体 (HY-19339)；蓝色: Cereblon 配体 (HY-A0003)；黑色: 连接子 (HY-B0236))。

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PROTAC Sirt2 Degrader-2

PROTAC Sirt2 Degrader-2 Chemical Structure

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PROTAC Sirt2 Degrader-2 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Sirtuin 亚型特异性产品:

查看所有亚型
Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 mTOR 亚型特异性产品:

查看所有亚型
mTOR mTORC1 mTORC2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 (HY-B0236)).

IC50 & Target

SIRT2

 

mTOR

 

Akt

 

体外研究
(In Vitro)

PROTAC Sirt2 Degrader-2 (Compound W10) (72 小时) 对多种卵巢癌细胞系表现出强效的抗增殖活性和高选择性，包括 SKOV3 (IC50 = 0.33 μM) 、OVCAR3 (IC50 = 0.25 μM) 和 A2780 (IC50 = 0.08 μM) 卵巢癌细胞，同时对正常细胞 IOSE80 的毒性较低 (CC50 = 2.64 μM)[1]。
PROTAC Sirt2 Degrader-2 (0.01-20 μM，6-48 小时) 能高效且选择性地降解 A2780 卵巢癌细胞中的 SIRT2 蛋白。其作用机制具有浓度和时间依赖性，但在高浓度下会出现钩状效应[1]。
PROTAC Sirt2 Degrader-2 (1 小时) 能提高 A2780 卵巢癌细胞中 SIRT2 蛋白的热稳定性，表明 PROTAC Sirt2 Degrader-2 直接与 SIRT2 结合并稳定其结构[1]。
PROTAC Sirt2 Degrader-2 (0.01-5 μM，14 天) 以浓度依赖的方式抑制 A2780 细胞的克隆形成[1]。
PROTAC Sirt2 Degrader-2 (0.01-10 μM，36 小时) 诱导 A2780 细胞在 S 期和 G2/M 期发生细胞周期阻滞[1]。
PROTAC Sirt2 Degrader-2 (0.01-10 μM，36 小时) 以浓度依赖的方式诱导 A2780 细胞的早期和晚期凋亡，其中晚期凋亡更为显著[1]。

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

PROTAC Sirt2 Degrader-2 相关抗体:

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.
体内研究
(In Vivo)

PROTAC Sirt2 Degrader-2 (Compound W10) (3-10 mg/kg，腹腔注射，每两天一次) 可显著抑制 A2780 荷瘤小鼠的肿瘤生长，且无明显毒性，并能有效降解体内的 SIRT2 蛋白[1]。

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.
分子量

682.83

Formula

C37H42N6O5S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PROTAC Sirt2 Degrader-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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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