1. PI3K/Akt/mTOR
    Epigenetics
    Apoptosis
  2. AMPK
    Apoptosis
  3. EB-3D

EB-3D 

Cat. No.: HY-115463
Handling Instructions

EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor, with an IC50 of 1 μM. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.

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EB-3D Chemical Structure

EB-3D Chemical Structure

CAS No. : 1839150-63-8

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Description

EB-3D is a potent and selective choline kinase alpha 1 (ChoKα1) inhibitor, with an IC50 of 1 μM. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity[1][2][3].

IC50 & Target

IC50: 1 μM; Kd: 0.7 μM[3]

In Vitro

EB-3D displays (0-100 μM; 72 hours) excellent antiproliferative activity against a wide cohort of T-leukemic cell lines, with GI GI50s 13 values in the nanomolar range[1].
EB-3D (1.25-5μM; 24 hours) induced apoptosis in leukemia cell lines[1].
EB-3D (0.5-1 μM; 24 hours) induces a G0/G1 arrest that lead to apoptosis[1].
EB-3D (0.3 μM; 48 hours) shows a first spike of activation of AMPKα after 30 minutes and a later increase in the phosphorylation of T172[1].
EB-3D (1-40 μM; 48 hours) inhibits cell growth in HepG2 cells with a GI50 of 14.55 μM[2].

Cell Proliferation Assay[1]

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
Result: Inhibited JURKAT, CCRF-CEM, HSB-2, MOLT-16, DNA-41, LOUCY, PEER, and ALL-SIL cells growth with GI50s of 136.2, 478.8, 17.7, 0.9, 60.6, 200, 265, and 132 nM, respectively.

Apoptosis Analysis[1]

Cell Line: Jurkat, CCRF-CEM and HSB-2 cells
Concentration: 1.25, 2.5, 5 μM
Incubation Time: 24 hours
Result: Induced apoptosis in leukemia cell lines.

Cell Cycle Analysis[1]

Cell Line: Jurkat, CCRF-CEM and HSB-2 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Induces cell cycle arrest in G0/G1 phase.

Western Blot Analysis[1]

Cell Line: Jurkat cells
Concentration: 0.3 μM
Incubation Time: 48 hours
Result: Showed a first spike of activation of AMPKα after 30 minutes of treatment and a later increase in the phosphorylation of T172. The increase in S79 phosphorylation of its main target ACC (acetyl-coenzyme A (CoA) carboxylase), followed the same pattern. This rapid activation of AMPK, in turn induced a consequent reduction in mTOR phosphorylation that is visible already at 30’ and that becomes amplified at longer time probably due to the interruption of feedback loops that are characteristic of mTOR connecting pathways.
Molecular Weight

644.44

Formula

C₃₀H₃₆Br₂N₄O₂

CAS No.

1839150-63-8

SMILES

CN(C1=CC=[N+](CC2=CC=C(OCCOC3=CC=C(C[N+]4=CC=C(N(C)C)C=C4)C=C3)C=C2)C=C1)C.[Br-].[Br-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (77.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5517 mL 7.7587 mL 15.5173 mL
5 mM 0.3103 mL 1.5517 mL 3.1035 mL
10 mM 0.1552 mL 0.7759 mL 1.5517 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

EB-3DAMPKApoptosisAMP-activated protein kinasetumorigenesisTacutelymphoblasticleukemiadephosphorylationHepG2lipidhomeostasisInhibitorinhibitorinhibit

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