2. PROTAC Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. PROTACs Transglutaminase FAK Src Akt
  4. PROTAC TG2 Degrader-3

PROTAC TG2 Degrader-3 是一种 TG2 PROTAC 降解剂。PROTAC TG2 Degrader-3 可抑制卵巢癌细胞的黏附和迁移。PROTAC TG2 Degrader-3 可用于卵巢癌的研究。
(粉色: Transglutaminase 配体 (HY-128595)；蓝色: Ligands for E3 Ligase 和 VHL 配体 (HY-47851)；黑色: 连接子 (HY-W013731))。

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PROTAC TG2 Degrader-3

PROTAC TG2 Degrader-3 Chemical Structure

CAS No. : 3054388-18-7

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PROTAC TG2 Degrader-3 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Src 亚型特异性产品:

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC TG2 Degrader-3 is a TG2 PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer[1]. (Pink: Transglutaminase ligand (HY-128595); Blue: Ligands for E3 Ligase and VHL ligand (HY-47851); Black: linker (HY-W013731)).

IC50 & Target[1]

VHL

 

体外研究
(In Vitro)

PROTAC TG2 Degrader-3 (Compound P374) (0.1-10 μM; 24-72 h) 可在 SKOV3/OVCAR5 卵巢癌细胞中诱导 TG2 发生强效的、蛋白酶体依赖的降解[1]。
PROTAC TG2 Degrader-3 (0-30 μM; 24 h) 不会显著降低 SKOV3 或 OVCAR5 卵巢癌细胞的细胞活力[1]。
PROTAC TG2 Degrader-3 (10 μM; 6-18 h) 可抑制 SKOV3 和 OVCAR5 卵巢癌细胞对纤连蛋白的黏附和迁移能力[1]。
PROTAC TG2 Degrader-3 (1-10 μM) 可显著抑制 SKOV3 卵巢癌细胞中 FAKTyr397 和 SrcTyr416 的磷酸化，并通过降解 TG2 破坏下游整合素信号通路[1]。
PROTAC TG2 Degrader-3 (10 μM; 24 h) 可诱导 SKOV3 卵巢癌细胞发生广泛的蛋白质组学变化，包括 TG2、AKT、p-AKT、SOX2、ATRX 和 HER2/ErbB2 的水平降低，以及多个与细胞黏附和癌症进展相关的信号通路失调[1]。

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

PROTAC TG2 Degrader-3 相关抗体:

Western Blot Analysis[1]

Cell Line: SKOV3/OVCAR5 ovarian cancer cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h, 72 h
Result: Induced significant, time- and concentration-dependent TG2 degradation, reaching approximately 80% maximal degradation at 24 h at 10 μM, with TG2 levels remaining suppressed through 72 h.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUClast
Mice[1] 2 mg/kg i.p. 4.2 h 600.8 nM 1631.3 nM·h
体内研究
(In Vivo)

PROTAC TG2 Degrader-3 (55 μg/kg; i.p.; three times per week; 4 weeks) 可显著抑制卵巢肿瘤的生长与扩散，并在体内降低 TG2 的表达及酶活性[1]。

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

Animal Model: Athymic nude mice (6-8 weeks old, female; ovarian cancer model via intraperitoneal injection of OVCAR5 cells)[1]
Dosage: 55 μg/kg
Administration: i.p.; three times per week; 4 weeks
Result: Exhibited significantly reduced tumor weights, tumor volumes, and tumor numbers compared to vehicle controls.
Confirmed reduced TG2 expression in tumors from treated mice.
Significantly lowered TG2 enzymatic activity in ascites fluid compared to controls.
分子量

996.22

Formula

C51H62FN9O7S2
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 TG2 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 TG2 Degrader-33054388-18-7PROTACsTransglutaminaseFAKSrcAkt转谷氨酰胺酶PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasePKBProtein kinase BSKOV3 ovarian cancer cellsTG2OVCAR5 ovarian cancer cellscell adhesionproteasomecell migrationovarian cancerInhibitorinhibitorinhibit

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