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EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor (IC50: 1 μM) with anti-cancer activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $93 | In Stock | |
5 mg | $197 | In Stock | |
10 mg | $289 | In Stock | |
25 mg | $496 | In Stock | |
50 mg | $689 | In Stock | |
100 mg | $973 | In Stock | |
1 mL x 10 mM (in DMSO) | $292 | In Stock |
Description | EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor (IC50: 1 μM) with anti-cancer activity. |
Targets&IC50 | ChoKα1:1 μM |
In vitro | EB-3D?exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines and primary cultures of pediatric patients.?Moreover, the drug strongly induces apoptosis and more importantly it enhanced T-leukemia cell sensitivity to chemotherapeutic agents, such as dexamethasone and l-asparaginase.?In addition, the compound induces an early activation of AMPK, the main regulator of cellular energy homeostasis, by its phosphorylation at residue T712 of catalytic subunit α, and thus repressing mTORC1 pathway, as shown by mTOR S2448 dephosphorylation.?The inhibition of mTOR in turn affects the activity of several known downstream targets, such as 4E-BP1, p70S6K, S6 Ribosomal Protein and GSK3 that ultimately may lead to a reduction of protein synthesis and cell death[1]. |
Cell Research | Cell Line:JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, ALL-SIL cells. Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM.Incubation Time:72 hours |
Molecular Weight | 644.4 |
Formula | C30H36Br2N4O2 |
Cas No. | 1839150-63-8 |
Smiles | [Br-].[Br-].CN(C)c1cc[n+](Cc2ccc(OCCOc3ccc(C[n+]4ccc(cc4)N(C)C)cc3)cc2)cc1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (77.59 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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