2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs FAK
  4. PROTAC FAK degrader 3

PROTAC FAK degrader 3 是一种选择性的 FAK PROTAC 降解剂 (DC50 = 1.08 nM)。PROTAC FAK degrader 3 诱导 FAK 降解依赖于泛素-蛋白酶体系统及其与 FAK 和 CRBN 的结合。PROTAC FAK degrader 3 通过对 FAK 非催化活性的抑制上调 MHC-I 的基因转录和肿瘤细胞表面表达，进而导致抗原呈递增加和细胞毒性 CD8 T 细胞的激活。PROTAC FAK degrader 3 通过促进 MHC-I 表达和增强 T 细胞活化来增强体内抗肿瘤活性。PROTAC FAK degrader 3 可用于卵巢癌、肝细胞癌等靶向 FAK 降解的癌症研究。(粉色: FAK-IN-3:HY-143407，蓝色: Thalidomide-4-OH:HY-103596，蓝色 + 黑色: FAK ligand-3: HY-W939883，黑色：连接子)。

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PROTAC FAK degrader 3

PROTAC FAK degrader 3 Chemical Structure

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PROTAC FAK degrader 3 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC FAK degrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). PROTAC FAK degrader 3-induced FAK degradation is dependent on the ubiquitin-proteasome system and its binding to FAK and CRBN. PROTAC FAK degrader 3 upregulates MHC-I gene transcription and tumor cell surface expression by inhibiting the non-catalytic activity of FAK, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. PROTAC FAK degrader 3 enhances in vivo anti-tumor activity by promoting MHC-I expression and enhancing T cell activation. PROTAC FAK degrader 3 can be used in cancer research targeting FAK degradation in ovarian cancer, hepatocellular carcinoma, and other cancers. (Pink: FAK-IN-3:HY-143407, Blue: Thalidomide-4-OH:HY-103596, Blue + Black: FAK ligand-3: HY-W939883, Black: Linker)[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

PROTAC FAK degrader 3 (Compound D4) (0-1000 nM，24 小时) 可诱导 PA-1、ID8、4T1、H22、HEY、MDA-MB-231 和 PLC/PRF5 细胞中的 FAK 降解，在 PA-1 细胞中，50 nM 时诱导 89% 的 FAK 降解，500 nM 时诱导 92% 的 FAK 降解[1]。
PROTAC FAK degrader 3 (1 μM) 可抑制 FAK (99%) (I 50 = 0.44 nM)、STK33 (92%)、CLK4 (87%) 和 Fes (86%) 激酶活性[1]。
PROTAC FAK degrader 3 (0.01-100 μM，72 小时) 对 PA-1、HEY 和 Huh-7 细胞表现出抗增殖活性[1]。
PROTAC FAK degrader 3 (0-3 μM，1-7 天) 可降低 PA-1 细胞中的菌落形成、迁移和侵袭[1]。
PROTAC FAK degrader 3 (3 μM，24 小时) 在 PA-1 细胞中可上调与肿瘤免疫原性相关的基因、抗原呈递相关基因 (HLA-B、HLA-F 和 B2M) 以及免疫蛋白酶体相关基因 (PSMB8 和PSMB9) [1]。
PROTAC FAK degrader 3 (3 μM, 24 小时) 可促进 ID8、PA-1、H22、PLC/PRF5 细胞中肿瘤细胞表面的抗原呈递和 MHC-I 表达[1]。
PROTAC FAK degrader 3 (3 μM, 72 小时) 可促进与活化的小鼠 CD8 T 细胞共培养的 ID8 细胞中抗原特异性 CD8 T 细胞的活化和增殖[1]。

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

PROTAC FAK degrader 3 相关抗体:

Western Blot Analysis[1]

Cell Line: PA-1 cells
Concentration: 0 nM, 0.14 nM, 0.41 nM, 1.23 nM, 3.7 nM, 11.1 nM, 33.3 nM, 100 nM
Incubation Time: 0 h, 1 h, 2 h, 4 h, 6 h, 12 h, 24 h
Result: Induced FAK degradation, with almost complete degradation at 11.1 nM and achieved almost complete degradation at 24 h.

Western Blot Analysis[1]

Cell Line: ID8, 4T1, H22, HEY, MDA-MB-231, and PLC/PRF5 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced FAK degradation.

Western Blot Analysis[1]

Cell Line: PA-1, H22 cells
Concentration: 3, 10, 30 nM
Incubation Time: 24 h
Result: Induced FAK degradation, showed comparable degradation activity to GSK215 (HY-132296) and was more effective than BI-3663 (HY-111546).

RT-PCR[1]

Cell Line: PA-1 cells
Concentration: 3 μM
Incubation Time: 24 h
Result: Had little effect on FAK mRNA levels.

Cell Migration Assay [1]

Cell Line: PA-1 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Reduced migration and invasion ability.

Western Blot Analysis[1]

Cell Line: ID8, PA-1, H22, PLC/PRF5 cells
Concentration: 3 μM
Incubation Time: 72 h
Result: Induced FAK degradation.
体内研究
(In Vivo)

PROTAC FAK degrader 3 (Compound D4) (15 mg/kg，腹腔注射，每日一次，8 天) 通过促进 MHC-I 表达和增强 T 细胞活化来提高 H22 肿瘤小鼠模型中的抗肿瘤活性[1]。

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

Animal Model: H22 (1 × 106) tumor-bearing syngeneic mice (6 week-old BALB/cJ) model[1]
Dosage: 15 mg/kg
Administration: i.p., once a day, 8 days
Result: Inhibited tumor growth without affecting the body weight, enhanced expression of H2-Kd/H2-Dd on CD45- tumor cells (3.19-fold versus vehicle), without affecting Pd-l1 expression, expressed a higher level of CD107a (2.82-fold versus vehicle), indicating enhanced cell cytotoxicity.
分子量

882.96

Formula

C48H50N8O9
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 FAK degrader 3 相关分类

  • 摩尔计算器

  • 稀释计算器

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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 FAK degrader 3PROTAC FAK degrader3PROTAC FAK degrader-3PROTACsFAKPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasePROTACdegraderovarian cancerhepatocellular carcinomaPA-1 cellsH22 cellsInhibitorinhibitorinhibit

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