1H-Indole-2-carboxylic acid, 4,6-bis(1-methylethoxy)-, methyl ester
- CAS No.
- 2607143-50-8
- Chemical Name:
- 1H-Indole-2-carboxylic acid, 4,6-bis(1-methylethoxy)-, methyl ester
- Synonyms
- XST-14;1H-Indole-2-carboxylic acid, 4,6-bis(1-methylethoxy)-, methyl ester
- CBNumber:
- CB58667228
- Molecular Formula:
- C16H21NO4
- Molecular Weight:
- 291.34
- MDL Number:
- MOL File:
- 2607143-50-8.mol
| Boiling point | 439.9±40.0 °C(Predicted) |
|---|---|
| Density | 1.144±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO : 250 mg/mL (858.10 mM; Need ultrasonic) |
| form | Solid |
| pka | 16.02±0.30(Predicted) |
| color | White to off-white |
1H-Indole-2-carboxylic acid, 4,6-bis(1-methylethoxy)-, methyl ester Chemical Properties,Uses,Production
Biological Activity
XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects[1]. XST-14 inhibits ULK1 (IC50=13.6 nM), MAP2K1/MEK1 (IC50=721.8 nM), MAPK14/p38 alpha (IC50=283.9 nM), TGFBR2 (IC50=809.3 nM), ACVR1/ALK2 (IC50=183.8 nM), ULK2 (IC50=70.9 nM) and CAMK2A (IC50=66.3 nM) by the 10-point titration results from SelectScreen Kinase Profiling Services[1]. XST-14 (20-80 μM; for 24 h) leads a decrease in cell proliferation activity[1]. XST-14 (5 μM; for 24 h) induces apoptosis in HepG2 and human primary HCC cells[1]. XST-14 (5 μM; for 12 h) strongly inhibits the conversion of LC3-I to LC3-II in CHO cells stably expressing GFP-LC3[1]. XST-14 (5 μM; for 12 h) inhibits the Ser249 phosphorylation of PIK3C3 and Ser15 phosphorylation of BECN1[1]. XST-14 (15, 30 mg/kg/day; IP; for 4 consecutive weeks) displays anti-HCC efficacies, resulting in decreased tumor weights and suppressed tumor growth of HCC cells in nude mice[1]. XST-14 (2 mg/kg for IV; 10 mg/kg for IP) has a T1/2 of 2.31 hours for IV and a T1/2 of 2.69 hours for IP[1].
References
[1]. Si-Tu Xue, et al. The role of the key autophagy kinase ULK1 in hepatocellular carcinoma and its validation as a treatment target . Autophagy. 2020 Oct;16(10):1823-1837.
1H-Indole-2-carboxylic acid, 4,6-bis(1-methylethoxy)-, methyl ester Preparation Products And Raw materials
Raw materials
Preparation Products
1H-Indole-2-carboxylic acid, 4,6-bis(1-methylethoxy)-, methyl ester Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
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