5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
- Product Name
- 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
- CAS No.
- 667880-38-8
- Chemical Name
- 5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
- Synonyms
- IAC-8;ZLDI-8, 10 mM in DMSO;5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione;4,6(1H,5H)-Pyrimidinedione, 5-[[1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl]methylene]dihydro-2-thioxo-;pithelial-mesenchymal,ZLDI8,transition,anti-tumor,inhibit,Phosphatase,Sorafenib,E-Cadherin,N-Cadherin,Apoptosis,Notch,Survivin,ZLDI 8,Inhibitor,NICD,ADAM-17,cIAP1/2,Vimentin,ZLDI-8
- CBNumber
- CB32060973
- Molecular Formula
- C24H23N3O3S
- Formula Weight
- 433.52
- MOL File
- 667880-38-8.mol
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Property
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- 62.5 mg/mL in DMSO
- pka
- 5.34±0.20(Predicted)
- form
- Solid
- color
- Yellow to orange
N-Bromosuccinimide Price
- Product number
- CS-0087510
- Product name
- ZLDI-8
- Purity
- 98.53%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0087510
- Product name
- ZLDI-8
- Purity
- 98.53%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0087510
- Product name
- ZLDI-8
- Purity
- 98.53%
- Packaging
- 50mg
- Price
- $1650
- Updated
- 2021/12/16
- Product number
- CS-0087510
- Product name
- ZLDI-8
- Purity
- 98.53%
- Packaging
- 100mg
- Price
- $2250
- Updated
- 2021/12/16
- Product number
- DC11017
- Product name
- ZLDI-8
- Purity
- >98%
- Packaging
- 1g
- Price
- $1900
- Updated
- 2021/12/16
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Chemical Properties,Usage,Production
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. |
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
5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione Preparation Products And Raw materials
Raw materials
Preparation Products
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