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

EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. 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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 354 In-stock
Solution
10 mM * 1 mL in DMSO USD 354 In-stock
Solid
1 mg USD 119 In-stock
5 mg USD 250 In-stock
10 mg USD 350 In-stock
50 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE EB-3D

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. 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].
EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
In Vivo

EB-3D (1 mg/kg; i.p.; every other day) impairs mammary tumor growth in syngeneic orthotopic E0771-C57BL/6 mouse model[4].
EB-3D (2.5 mg/kg; every other day for 4 weeks) shows a reduction of the number of spontaneous lung macro- and micrometastasis[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: E0771-C57BL/6 mice[4]
Dosage: I.p.; every other day for 4 weeks
Administration: 2.5 mg/kg
Result: A reduction of the number of spontaneous lung macro- and micrometastasis.
Molecular Weight

644.44

Formula

C30H36Br2N4O2

CAS No.
Appearance

Solid

Color

White to off-white

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (77.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 9.09 mg/mL (14.11 mM)

*"≥" means soluble, but saturation unknown.

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.5517 mL 7.7587 mL 15.5173 mL 38.7934 mL
5 mM 0.3103 mL 1.5517 mL 3.1035 mL 7.7587 mL
10 mM 0.1552 mL 0.7759 mL 1.5517 mL 3.8793 mL
DMSO 15 mM 0.1034 mL 0.5172 mL 1.0345 mL 2.5862 mL
20 mM 0.0776 mL 0.3879 mL 0.7759 mL 1.9397 mL
25 mM 0.0621 mL 0.3103 mL 0.6207 mL 1.5517 mL
30 mM 0.0517 mL 0.2586 mL 0.5172 mL 1.2931 mL
40 mM 0.0388 mL 0.1940 mL 0.3879 mL 0.9698 mL
50 mM 0.0310 mL 0.1552 mL 0.3103 mL 0.7759 mL
60 mM 0.0259 mL 0.1293 mL 0.2586 mL 0.6466 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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EB-3D
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