2. PROTAC Neuronal Signaling GPCR/G Protein PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. PROTACs Cannabinoid Receptor Akt ERK Bcl-2 Family Apoptosis
  4. PROTAC CB1R Degrader-1

PROTAC CB1R Degrader-1 是一种强效且选择性的 CB1R PROTAC 降解剂，它利用泛素-蛋白酶体系统 (UPS) 介导对 CB1R 的降解，在 MCF-7 细胞中的 DC50 为 3.37 μM，且对 CB2R 无影响。PROTAC CB1R Degrader-1 可降低 CB1R 相关的下游信号通路 (p-AKT、p-ERK、BCL2 和 MCM5)，从而抑制乳腺癌细胞增殖并诱导细胞凋亡 (apoptosis)。PROTAC CB1R Degrader-1 可用于乳腺癌相关研究。(蓝色: CRBN 配体 (HY-41547); 黑色: 连接子 (HY-178198); 粉色: CB1R 配体 (HY-134497))。

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PROTAC CB1R Degrader-1

PROTAC CB1R Degrader-1 Chemical Structure

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Customer Review

PROTAC CB1R Degrader-1 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 Cannabinoid Receptor 亚型特异性产品:

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CB1 CB2

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497))[1].

体外研究
(In Vitro)

PROTAC CB1R Degrader-1 (Pro-CB8) (0.1-20 μM, 6-48 小时) 在 MCF-7 细胞中诱导 CB1R 显著降解，且呈剂量和时间依赖性 (DC50 = 3.37 μM)，在 MDA-MB-231 细胞中也观察到 CB1R水平的显著降低，表明其具有更广泛的适用性[1]。
PROTAC CB1R Degrader-1 (0-10 μM，6-48 小时) 可下调乳腺癌细胞 (包括 MCF-7 和 MDA-MB-231) 中关键的癌症相关蛋白 (p-AKT、p-ERK) 和基因 (BCL2、MCM5) 的表达[1]。
PROTAC CB1R Degrader-1 (0-10 μM，48 小时) 可选择性地降低乳腺癌细胞 (MCF-7 和 MDA-MB-231) 的活力和增殖，同时不损伤健康的成纤维细胞，并诱导两种癌细胞系 (MCF-7 和 MDA-MB-231) 发生显著的细胞凋亡[1]。
PROTAC CB1R Degrader-1 (10 μM) 在 3D 实验模型中导致 MCF-7 和 MDA-MB-231 肿瘤球体出现明显且持续的瓦解，此效应最早于第 3 天开始出现并在整个观察期内持续存在[1]。

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

PROTAC CB1R Degrader-1 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Significantly reduced CB1R levels by approximately 80 % at 10 μM.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1, 2, 5, 10, and 20 μM
Incubation Time: 6, 12, 24, and 48 h
Result: Reduced CB1R levels in a time-dependent manner, with the most potent effect observed after 48 h.
significantly reduced CB1R protein levels, achieving approximately 75 % degradation at 20 μM with a calculated degradation concentration (DC50 = 3.37 μM).

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 48 h
Result: Induced a significant reduction in CB1R levels, with a maximum decrease of approximately 90 % at 10 μM.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10 μM
Incubation Time: 6, 12, 24 and 48 h
Result: Markedly decreased levels of p-AKT and p-ERK by approximately 70 %.
Decreased BAL2 levels in a time-dependent manner at 10 μM, with a 56 % reduction after 48 h.

Real Time qPCR[1]

Cell Line: MCF-7 cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Decreased MCM5 and BCL2 mRNA levels at 1 and 10 μM.

Cell Viability Assay[1]

Cell Line: MCF-7 and fibroblast cells
Concentration: 0.1, 1, and 10 μM
Incubation Time: 48 h
Result: Decreased cell viability at 0.1, 1, and 10 μM in MCF-7 cells.
Showed no significant effect on fibroblast cells.

Cell Proliferation Assay[1]

Cell Line: MCF-7 and MDA-MB-231 cells
Concentration: 0, 1, and 10 μM for MCF-7 cells; 0, 0.01, 0.1, 1, and 10 μM for MDA-MB-231 cells
Incubation Time: 48 h
Result: Decreased MCF-7 cell proliferation at 1, and 10 μM.
Decreased MDA-MB-231 cell proliferation at 1 and 10 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 and MDA-MB-231 cells
Concentration: 10 μM for MCF-7 cells, 0.01, 0.1, 1, and 10 μM for MDA-MB-231 cells
Incubation Time: 48 h
Result: Resulted in a robust increase in apoptosis at 10 μM in MCF-7 cells.
Induced a dose-dependent marked increase in apoptosis in MDA-MB-231 cells at 1 and 10 μM.
体内研究
(In Vivo)

PROTAC CB1R Degrader-1 (5 mg/kg，腹腔注射，单次给药) 在小鼠体内表现出极低的脑组织渗透性，难以穿过血脑屏障[1]。

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

761.01

Formula

C35H28Cl3N9O5
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 CB1R Degrader-1 相关分类

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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 CB1R Degrader-1PROTACsCannabinoid ReceptorAktERKBcl-2 FamilyApoptosisPKBProtein kinase BExtracellular signal regulated kinasesCB1RUPSMCF-7p-AKTp-ERKBCL2MCM5apoptosisPROTACbreast cancerMDA-MB-231Inhibitorinhibitorinhibit

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