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RepSox

inhibits TGF-beta signaling; structure in first source appears to be incorrect

Also Known As:

616452 compound; E 616452; E-616452; E616452

Networked: 13 relevant articles (0 outcomes, 2 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Pyrazoles: 61
      - RepSox: 13
  - Pyridines: 88
    - RepSox: 13

Experts

1.	Chen, Zhenzhong: 2 articles (11/2021 - 12/2018)
2.	He, Dengwei: 2 articles (11/2021 - 12/2018)
3.	Lou, Chao: 2 articles (11/2021 - 12/2018)
4.	Zheng, Lin: 2 articles (11/2021 - 12/2018)
5.	Wiraja, Christian: 2 articles (12/2018 - 12/2018)
6.	Xu, Chenjie: 2 articles (12/2018 - 12/2018)
7.	Beausang, Alan: 1 article (01/2022)
8.	Behan, Claire: 1 article (01/2022)
9.	Betsholtz, Christer: 1 article (01/2022)
10.	Bolger, Isobel: 1 article (01/2022)

Related Diseases

1.	Chromosome Aberrations (Chromosome Abnormalities) 08/01/2021 - "In the present study, it was demonstrated that RepSox caused the visible morphological transformation of sheep fibroblasts; however, no significant alterations in cell proliferation, apoptosis or chromosome aberrations were observed. "
2.	Bone Resorption 12/01/2018 - "Together, our data suggest that RepSox regulates osteoclast differentiation, bone resorption, and OVX-induced OP via the suppression of the Smad3 and JNK/AP-1 pathways." 12/01/2018 - "The aim of our study is to evaluate the effects of RepSox on the differentiation and bone resorption of osteoclasts in vitro and in vivo in an ovariectomy (OVX)-induced OP model. " 12/01/2018 - "In the in vitro study, RepSox inhibited the receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclast differentiation and bone resorption activity. " 12/01/2018 - "Small molecule inhibitor RepSox prevented ovariectomy-induced osteoporosis by suppressing osteoclast differentiation and bone resorption."
3.	Neoplasms (Cancer) 11/01/2021 - "Our in vivo findings using a xenograft model also revealed that RepSox markedly inhibited the growth of tumors. " 01/01/2020 - "Tumor cell implantation (TCI) technology was used to generate a model of cancer-induced bone pain (CIBP) in rats; intrathecal (i.t.) injections of small interfering (si) RNAs targeting CXCR4 and the ALK5-specific inhibitor, RepSox, were performed. " 08/08/2017 - "A combination of valproic acid sodium salt, CHIR99021, E-616452, tranylcypromine, and 3-Deazaneplanocin A causes stem cell-like characteristics in cancer cells."
4.	Fibrosis (Cirrhosis) 12/01/2020 - "The increased adhesion and fibrosis activities by HOXC8 were significantly inhibited by E-616452, a selective inhibitor of TGF-β receptor type I kinases. " 11/01/2017 - "In addition, Repsox could attenuate skin fibrosis by bleomycin in vivo, via the downregulation of CTGF or collagen. " 11/01/2017 - "Transforming growth factor β-inhibitor Repsox downregulates collagen expression of scleroderma dermal fibroblasts and prevents bleomycin-induced mice skin fibrosis."
5.	Cicatrix (Scar) 12/14/2018 - "Utilizing this probe, we can distinguish abnormal fibroblasts derived from abnormal scars and assess the effectiveness of anti-scarring drugs like Repsox and transforming growth factor-beta type I receptor (TGF-βRI) siRNA." 12/17/2018 - "The identified drug candidates (RepSox and Thiazovivin) show similar potent anti-scarring activity as the existing anti-scarring compounds and further suppress the expression of other scar biomarkers including connective tissue growth factor (CTGF), alpha-smooth muscle actin (α-SMA), and collagen type 1 (COL1A1)."

Related Drugs and Biologics

1.	Ligands
2.	Transforming Growth Factors (Transforming Growth Factor)
3.	Claudin-5
4.	Connective Tissue Growth Factor
5.	Mucin-3
6.	Small Interfering RNA (siRNA)
7.	Collagen Type I (Type I Collagen)
8.	Biomarkers (Surrogate Marker)
9.	Valproic Acid (Depakote)
10.	Tranylcypromine (Parnate)

Related Therapies and Procedures

1.	Ovariectomy (Oophorectomy)
2.	Injections