| Identification | Back Directory | [Name]
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione | [CAS]
667880-38-8 | [Synonyms]
IAC-8
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione | [Molecular Formula]
C24H23N3O3S | [MDL Number]
MFCD03699567 | [MOL File]
667880-38-8.mol | [Molecular Weight]
433.523 |
| Chemical Properties | Back Directory | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
62.5 mg/mL in DMSO | [form ]
Solid | [pka]
5.34±0.20(Predicted) | [color ]
Yellow to orange |
| Hazard Information | Back Directory | [Uses]
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM[1][2]. | [in vivo]
ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model[1]. | Animal Model: | Nude mice with MHCC-97H cells[1] | | Dosage: | 2?mg/kg, 1?mg/kg, 500?μg/kg, or 200?μg/kg | | Administration: | Intraperitoneal injection; every two days; for 20 days | | Result: | Inhibited tumor growth in nude HCC-bearing mice model. |
| [storage]
Store at -20°C | [References]
[1] Zhang Y, et al. Novel ADAM-17 inhibitor ZLDI-8 enhances the in vitro and in vivo chemotherapeutic effects of Sorafenib on hepatocellular carcinoma cells. Cell Death Dis. 2018 Jul 3;9(7):743. DOI:10.1038/s41419-018-0804-6
[2] Hou X, et al. Fast identification of novel lymphoid tyrosine phosphatase inhibitors using target-ligand interaction-based virtual screening. J Med Chem. 2014 Nov 26;57(22):9309-22. DOI:10.1021/jm500692u |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
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