2. Neuronal Signaling PI3K/Akt/mTOR Autophagy
  3. Beta-secretase PI3K Amyloid-β Autophagy
  4. LX2343

LX2343 

Cat. No.: HY-111383 Purity: 99.74%
COA Handling Instructions

LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.

For research use only. We do not sell to patients.

LX2343 Chemical Structure

LX2343 Chemical Structure

CAS No. : 333745-53-2

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Solution
10 mM * 1 mL in DMSO USD 109 In-stock
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10 mM * 1 mL
ready for reconstitution
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10 mg USD 165 In-stock
50 mg USD 539 In-stock
100 mg USD 825 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

LX2343 Related Antibodies

Top Publications Citing Use of Products

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BACE1 BACE2

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.

IC50 & Target[1]

BACE1

11.43 μM (IC50)

PI3K

15.99 μM (IC50)

Aβ

 

Autophagy

 

In Vitro

LX2343 (5-20 μM) dose-dependently decreased Aβ accumulation in HEK293-APPsw and CHO-APP cells, and promotes Aβ clearance in SH-SY5Y cells and primary astrocytes. LX2343 ameliorates cognitive dysfunction in APP/PS1 transgenic mice via both Aβ production inhibition and clearance promotion, which highlights the potential of LX2343 in the treatment of AD. Western blot results in both HEK293-APPsw cells and CHO-APP cells demonstrate that LX2343 fails to regulate BACE1 protein levels, while in vitro BACE1 enzymatic activity assays indicated that LX2343 dose-dependently decreases BACE1 activity (TDC as a positive control) with an IC50 of 11.43±0.36 μM. To test whether competition exists between LX2343 and ATP, we investigated the effects of ATP at different concentrations on the inhibitory activity of LX2343. The result demonstrated that the inhibition of LX2343 against PI3K is virtually unaffected by ATP. Thus, this result suggested that LX2343 is a non-ATP competitive inhibitor of PI3K. In the presence of 10 μM of ATP, the IC50 of LX2343 is 13.11±1.47 μM, in the presence of 50 μM ATP, the IC50 of LX2343 is 13.86±1.12 μM, in the presence of 100 μM ATP, the IC50 of LX2343 is 15.99±3.23 μM [1].

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

LX2343 Related Antibodies
In Vivo

APP/PS1 mice express chimeric human Swedish mutant APP and a mutant human presenilin 1 protein and are widely used as an effective animal model for AD dementia. The amelioration of memory impairment by LX2343 is evaluated t in this model using the MWM test. In 8-d training trials, the path lengths and escape latencies used to find the platform for APP/PS1 transgenic mice are remarkably longer than those for non-transgenic mice, while 10 mg/kg LX2343 administration obviously antagonizes the prolonged path lengths and escape latencies at d 7 and 8. In the probe trial assay, the LX2343-administered transgenic mice cross over the hidden location of the platform more frequently compared with the vehicle-administered transgenic mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

474.91

Appearance

Solid

Formula

C22H19ClN2O6S
CAS No.
SMILES

O=C(NC1=CC=C(OCO2)C2=C1)CN(C3=CC(Cl)=CC=C3OC)S(=O)(C4=CC=CC=C4)=O
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 : ≥ 100 mg/mL (210.57 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1057 mL 10.5283 mL 21.0566 mL
5 mM 0.4211 mL 2.1057 mL 4.2113 mL
10 mM 0.2106 mL 1.0528 mL 2.1057 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.80%

COA (252 KB) HNMR (191 KB) LCMS (347 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Inhibition of BACE1 enzyme by LX2343 is assayed using BACE1 activity kits in vitro. Briefly, BACE1 substrate (250 nM), BACE1 enzyme (0.35 U/mL), and varied concentrations of LX2343 (5, 10, and 20 μM) are sequentially incubated for 1 h at 37°C in the dark. Fluorescence intensity is measured with excitation and emission wavelengths at 545 and 585 nm, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

SH-SY5Y cells are transfected with mRFP-GFP-LC3 plasmids via an adenovirus. The cells are treated without or with Streptozotocin (0.8 mM) in combination with 5 or 20 μM LX2343 for 4 h and then fixed with 4% paraformaldehyde and observed using an Olympus Fluoview FV1000 confocal microscope[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
APP/PS1 [B6C3-Tg(APPswe, PS1dE9)] transgenic mice are used. Genotyping to confirm APP/PS1 DNA sequences in their offspring is performed by assaying the DNA from tail biopsies, with Tg-negative mice as a negative control. Twenty male APP/PS1 mice are divided into two groups with ten non-transgenic mice in one group to serve as a negative control. The two 6-month transgenic groups are administered 10 mg/kg per day of LX2343 or vehicle, and the 6-month non-transgenic group is administered the vehicle for 100 d via intraperitoneal injection. After 100 d of administration, MWM assays are applied to evaluate the cognitive abilities of the mice for 8 d under continuous LX2343 treatment. Upon completion of the MWM test, the mice are euthanized, and the brains are removed and bisected at the mid-sagittal plane. The right hemispheres are frozen and stored at -80°C, and the left hemispheres are fixed in 4% paraformaldehyde[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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LX2343 Related Classifications

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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Keywords:

LX2343333745-53-2LX 2343LX-2343Beta-secretasePI3KAmyloid-βAutophagyBACEβ-Secretase Phosphoinositide 3-kinaseβ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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