2. PROTAC Membrane Transporter/Ion Channel Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation PI3K/Akt/mTOR
  3. PROTACs P-glycoprotein Apoptosis Reactive Oxygen Species (ROS) Akt Bcl-2 Family Na+/K+ ATPase PI3K
  4. PROTAC PI3K/110β degrader-2

PROTAC PI3K/110β degrader-2 是一种选择性 PI3K/p110β PROTAC 降解剂。PROTAC PI3K/110β degrader-2 可以显著降解 110β 蛋白并抑制 P-糖蛋白的表达。PROTAC PI3K/110β degrader-2 可以增加活性氧 (ROS) 的水平。PROTAC PI3K/110β degrader-2 通过激活内质网应激 (ERS) 介导的线粒体凋亡 apoptosis 通路和抑制 AKT/Bcl-2 信号通路发挥抗肿瘤作用。PROTAC PI3K/110β degrader-2 可用于癌症的研究。(粉色: PI3K/110β 配体 (HY-75124); 蓝色: VHL 配体 (HY-125845); 黑色: 连接子 (HY-W002042))。

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PROTAC PI3K/110β degrader-2

PROTAC PI3K/110β degrader-2 Chemical Structure

CAS No. : 3070438-79-5

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PROTAC PI3K/110β degrader-2 相关抗体

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer. (Pink: PI3K/110β Ligand (HY-75124); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W002042))[1].

IC50 & Target[1]

PI3K

 

Bax

 

Bcl-2

 

Akt

 

体外研究
(In Vitro)

PROTAC PI3K/110β degrader-2 (Compoud J-6) (24 小时) 在 A549 (IC50 = 58.2 μM)，A549/DDP (IC50 = 39.23 μM)，MCF-7 (IC50 = 53.99 μM) 和 MCF-7/ADM (IC50 = 38.73 μM) 细胞中具有显著的抗肿瘤活性[1]。
PROTAC PI3K/110β degrader-2 (0-50 μM，0-48 小时) 可以以时间和浓度依赖的方式选择性降解 MCF-7/ADM 和 A549/DDP 细胞中的 110β 蛋白[1]。
PROTAC PI3K/110β degrader-2 (0-25 μM，24 小时) 显著增加 MCF-7/ADM 和 A549/DDP 细胞中的 ROS 水平，降低线粒体膜电位，并激活 ERS 介导的凋亡[1]。
PROTAC PI3K/110β degrader-2 (0-25 μM，24 小时) 抑制 MCF-7/ADM 和 A549/DDP 细胞中 Na+/K+-ATP 酶活性并降低 P-糖蛋白表达[1]。

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

PROTAC PI3K/110β degrader-2 相关抗体:

Apoptosis Analysis[1]

Cell Line: MCF-7/ADM and A549/DDP cells
Concentration: 6.25, 12.5 and 25 μM
Incubation Time: 24 h
Result: Significantly increased the proportion of cell apoptosis and the level of Caspase3, Cyt-3 and Caspase12.

Western Blot Analysis[1]

Cell Line: MCF-7/ADM and A549/DDP cells
Concentration: 25 μM
Incubation Time: 24 h
Result: Increased the protein level of P-PERK, ATF4, CHOP,.PTEN and BAX and decreased the protein level of P-AKT and Bcl-2.

Western Blot Analysis[1]

Cell Line: MCF-7/ADM and A549/DDP cells
Concentration: 0.25, 2.5 and 25 μM
Incubation Time: 24 h
Result: Significantly reduced the level of P-Glycoprotein.
体内研究
(In Vivo)

PROTAC PI3K/110β degrader-2 (Compoud J-6) (50 mg/kg；腹腔注射；每隔一天一次；7 次) 通过降解雌性 MCF-7/ADM 肿瘤 BALB/c 小鼠中的 110β 蛋白，有效抑制肿瘤的生长[1]。

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

Animal Model: Female BALB/c mice (5-6 weeks) bearing MCF-7/ADM xenograft tumor[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection (i.p.); once every other day for 7 times
Result: Significantly reduced tumor volume.
Effectively downregulated the level of 110β in tumor tissue.
Significantly increased the level of ATF6, CHOP, GRP78, Caspase-12 and BAX inhibited caspase-8, P-AKT, Bcl-2 and P-Glycoprotein.
Did not significantly affect weight and did not cause organ damage.
分子量

948.18

Formula

C51H65N9O7S
CAS 号
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 PI3K/110β degrader-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

PROTAC PI3K/110β degrader-23070438-79-5PROTACsP-glycoproteinApoptosisReactive Oxygen Species (ROS)AktBcl-2 FamilyNa+/K+ ATPasePI3KP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243PKBProtein kinase BSodium potassium pumpPhosphoinositide 3-kinasePI3K/110βPROTACROScancerapoptosisBcl-2ERSInhibitorinhibitorinhibit

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