Transcription Factor ERG
Transcription Factor ERG
The ETS-related gene (ERG) is a member of the E-26 transformation-specific (ETS) family of transcription factors. The full-length ERG protein consists of 486 amino acids and has a molecular weight of 54 kDa. Initially, ERG is highly expressed in the embryonic mesoderm and endothelium. It regulates vascular stability by modulating Wnt/β-catenin signaling and angiopoietin-1-dependent Notch signaling. Additionally, ERG maintains vascular homeostasis by suppressing the expression of proinflammatory genes, such as ICAM1 and IL8, and by preventing endothelial-to-mesenchymal transition.
ERG is crucial for endothelial homeostasis and plays a vital role in the development of the vascular system, the urogenital tract, and bone. Furthermore, ERG possesses oncogenic potential and is implicated in Ewing’s sarcoma and leukemia[1][2][3].
ERG is crucial for endothelial homeostasis and plays a vital role in the development of the vascular system, the urogenital tract, and bone. Furthermore, ERG possesses oncogenic potential and is implicated in Ewing’s sarcoma and leukemia[1][2][3].
References:
- [1]. Adamo P, et al. The oncogene ERG: a key factor in prostate cancer. Oncogene. 2016 Jan 28;35(4):403-14. [Content Brief]
- [2]. Kalna V, et al. The Transcription Factor ERG Regulates Super-Enhancers Associated With an Endothelial-Specific Gene Expression Program. Circ Res. 2019 Apr 26;124(9):1337-1349. [Content Brief]
- [3]. Shah AV, et al. Regulation of endothelial homeostasis, vascular development and angiogenesis by the transcription factor ERG. Vascul Pharmacol. 2016 Nov;86:3-13. [Content Brief]
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Transcription Factor ERG Related Products (4)
Related Products (4)
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DA-302168S
0 ImagesDA-302168S is an orally active and selective agonist targeting the GLP-1R, with EC50 value of 1.32 nM. DA-302168S reduces blood glucose levels and suppresses appetite, demonstrates minimal safety risks including low hERG channel inhibition and no significant off-target toxicity, and mitigates drug-drug interaction risk. DA-302168S can be used for the research of type 2 diabetes and obesity.
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PROTAC BRM/BRG1 degrader-3
0 ImagesCat. No.: HY-168251CAS No.: 2933125-05-2PROTAC BRM/BRG1 degrader-3 is a BRM/BRG1 PROTAC degrader, exhibiting a DC50 of less than 1 nM for BRM degradation and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 shows moderate inhibitory activity against CYP2D6 and hERG. PROTAC BRM/BRG1 degrader-3 inhibits cancer cell proliferation and tumor tissue growth, and exhibits favorable metabolic stability in liver microsomes. PROTAC BRM/BRG1 degrader-3 can be used in non-small cell lung cancer-related research.
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PROTAC RET Degrader 1
0 ImagesCat. No.: HY-178964CAS No.: 2760847-82-1PROTAC RET Degrader 1 is an orally active, blood-brain barrier-penetrant RET PROTAC degrader with a DC50 of 1.7 nM. PROTAC RET Degrader 1 binds to CRBN and forms a ternary complex with RET, mediating proteasomal degradation of RET, while also selectively mediating the degradation of SALL4. PROTAC RET Degrader 1 inhibits the RET signaling pathway, hERG channel activity, and Cyp3A4 enzyme activity; it suppresses cancer cell growth and induces tumor regression. PROTAC RET Degrader 1 can be used in research related to RET-driven cancers.
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DB1255
0 ImagesCat. No.: HY-187697CAS No.: 915978-94-8DB1255 is an ERG inhibitor that binds to the minor groove of DNA, with KD values of 26 nM and 86 nM for the ATGA and AATT sequences, respectively. DB1255 targets and binds to specific DNA minor grooves (single GC/AT-rich sequences), forming a hydrogen bond network with G bases and AT pairs via its thiophene group and amidino group, respectively, thereby blocking the binding of transcription factors. DB1255 can be used in the research of leukemia and prostate cancer.
