目录号 | 产品详情 | 靶点 | |
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T76736 | |||
Abituzumab (DI17E6) 是一种人源化抗integrinαV 单克隆抗体 (IgG2 型)。Abituzumab 能有效减少FAK、Akt 和ERK 的磷酸化。Abituzumab 可用于癌症,尤其是前列腺癌的研究。 | |||
T41164 | PROTACs | ||
FC 11 is a highly potent focal adhesion Ki nase (FAK) PROTAC®Degrader (DC50 values are 40 to 370 pM depending on cell line), which is composed of the FAK inhibitor PF 562217 joined by a linker to the cereblon-binding ligand Pomalidomide. The effects of FC 11 are reversible upon compound wash out. FC 11 also degrades autophosphorylated FAK (pFAKtyr397), displaying near complete degradation after 3 hours at 100 nM in TM3 cells. | |||
T63174 | |||
FLT3-IN-17 是一种 FAK 抑制剂 (IC50: 12 nM)。FLT3-IN-17 能够抑制 CYPs 和 FLT3 突变体的活性,对 D835Y 的 IC50<0.5 nM。FLT3-IN-17 能够用于癌症的研究。 | |||
T35075 | |||
VSWRAPTA is a promoter of neuronal branching via transcellular activation of the focal adhesion kinase (FAK) and the ERK1/2 signaling pathway in vitro. | |||
T73039 | |||
CYP1B1-IN-3为选择性CYP1B1抑制剂,其IC50值分别针对CYP1B1、CYP1A1、CYP1A2为6.6, 347.3, >10000 nM。该化合物能够抑制细胞迁移与侵袭,并作用于P-gp、AKT/ERK、FAK/SRC及EMT信号通路。 | |||
T17133 | Others | ||
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker characterized by its PEG composition. This compound plays a crucial role in the synthesis of a range of PROTACs, including BI-3663, a highly selective PTK2/FAK PROTAC. It employs cereblon ligands to target E3 ligases for the degradation of PTK2, exhibiting potent inhibitory activity with an IC50 of 18 nM[1]. | |||
T70490 | |||
QD232 is a novel inhibitor of cell proliferation, adhesion, and migration, leading to pancreatic cancer cell death by apoptosis and exerting ROS-mediated decrease in Src/FAK and STAT3 phosphorylation. | |||
T80523 | |||
Azurin p28 peptide是一种具有肿瘤穿透能力和抗肿瘤活性的肽。它通过与p53结合形成p28:p53复合物,从而降低p53在蛋白酶体中的降解,进而诱导细胞凋亡(apoptosis)或使细胞周期停滞。此外,Azurin p28 peptide通过抑制VEGFR-2、FAK和Akt的磷酸化表现出抗血管生成效果,抑制p53阳性肿瘤的生长。 | |||
T19906 | |||
5'-O-Tritylthymidine is a blocker of the formation of the FAK/Mdm-2 complex. 5'-O-Tritylthymidine activates p53 and caspase-8. It also leads to increase detachment and apoptosis in breast and colon cancers. | |||
T70352 | |||
PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL-induced apoptosis poses a huge problem in establishing clinically efficient TRAIL therapies. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPH-02922 | SRPX2 Protein, Mouse, Recombinant (His & Myc) | Mouse | Baculovirus Insect Cells | ||
Acts as a ligand for the urokinase plasminogen activator surface receptor. Plays a role in angiogenesis by inducing endothelial cell migration and the formation of vascular network (cords). Involved in cellular migration and adhesion. Increases the phosphorylation levels of FAK. Interacts with and increases the mitogenic activity of HGF. Promotes synapse formation. Required for ultrasonic vocalizations. SRPX2 Protein, Mouse, Recombinant (His & Myc) is expressed in Baculovirus insect cells with N-10xHis and C-Myc tag. The predicted molecular weight is 54.5 kDa and the accession number is Q8R054.
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TMPH-02923 | SRPX2 Protein, Mouse, Recombinant (His & Myc & SUMO) | Mouse | E. coli | ||
Acts as a ligand for the urokinase plasminogen activator surface receptor. Plays a role in angiogenesis by inducing endothelial cell migration and the formation of vascular network (cords). Involved in cellular migration and adhesion. Increases the phosphorylation levels of FAK. Interacts with and increases the mitogenic activity of HGF. Promotes synapse formation. Required for ultrasonic vocalizations. SRPX2 Protein, Mouse, Recombinant (His & Myc & SUMO) is expressed in E. coli expression system with N-10xHis-SUMO and C-Myc tag. The predicted molecular weight is 70.5 kDa and the accession number is Q8R054.
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TMPY-03440 | Sts1 Protein, Human, Recombinant (His) | Human | E. coli | ||
UBASH3B contains a ubiquitin associated domain at the N-terminus, an SH3 domain, and a C-terminal domain with similarities to the catalytic motif of phosphoglycerate mutase. UBASH3B was found to inhibit endocytosis of epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor. UBASH3B interferes with CBL-mediated down-regulation and degradation of receptor-type tyrosine kinases. It promotes accumulation of activated target receptors, such as T-cell receptors and EGFR, on the cell surface. UBASH3B exhibits tyrosine phosphatase activity toward several substrates including EGFR, FAK, SYK, and ZAP7. Down-regulates proteins that are dually modified by both protein tyrosine phosphorylation and ubiquitination.
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TMPY-04084 | ANGPTL1 Protein, Canine, Recombinant (hFc) | Canine | HEK293 Cells | ||
Angiopoietin-like protein 1 (ANGPTL1) has been reported to suppress migration and invasion in lung and breast cancer, acting as a novel tumor suppressor candidate. Downregulation of tumor suppressor signaling plays an important role in the pathogenesis of hepatocellular carcinoma (HCC).The downregulation of the angiopoietin-like protein ANGPTL1 is associated with vascular invasion, tumor thrombus, metastasis, and poor prognosis in HCC. Ectopic expression of ANGPTL1 in HCC cells effectively decreased their in vitro and in vivotumorigenicity, cell motility, and angiogenesis. shRNA-mediated depletion of ANGPTL1 exerted opposing effects. ANGPTL1 promoted apoptosis via inhibition of the STAT3/Bcl-2-mediated antiapoptotic pathway and decreased cell migration and invasion via downregulation of transcription factors SNAIL and SLUG. Furthermore, ANGPTL1 inhibited angiogenesis by attenuating ERK and AKT signaling and interacted with integrin α1β1 receptor to suppress the downstream FAK/Src-JAK-STAT3 signaling pathway. Taken together, these results suggest ANGPTL1 as a prognostic biomarker and novel therapeutic agent in HCC. ANGPTL1 expression was down-regulated in CRC tissues and inversely correlated with poor survival. ANGPTL1 repressed migration and invasion of CRC cells, and microRNA-138 was involved in this process. Angiopoietin-like protein 1 (ANGPTL1) has been shown to act as a tumor suppressor by inhibiting angiogenesis, cancer invasion, and metastasis.
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