2. Metabolic Enzyme/Protease
  3. Aminoacyl-tRNA Synthetase
  4. LysRs-IN-2

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.

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

LysRs-IN-2 Chemical Structure

LysRs-IN-2 Chemical Structure

CAS No. : 2170696-76-9

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1 mg USD 140 In-stock
5 mg USD 410 In-stock
10 mg USD 650 In-stock
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Based on 1 publication(s) in Google Scholar

LysRs-IN-2 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LysRs-IN-2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively[1].

IC50 & Target

IC50: 0.015 μM (PfKRS), 0.13 μM (CpKRS)[1]
In Vitro

LysRs-IN-2 is active against whole-cell bloodstream P. falciparum 3D7 (EC50=0.27 μM), HsKRS (IC50=1.8 μM), HepG2 cells (EC50=49 μM), and Cryptosporidium parvum (EC50=2.5 µM)[1].

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

LysRs-IN-2 Related Antibodies
In Vivo

LysRs-IN-2 (1.5 mg/kg; orally once a day for 4 days) reduces parasitemia by 90% in the murine P. falciparum SCID model. LysRs-IN-2 (20 mg/kg; orally once a day for 7 days) reduces parasite shedding in NOD SCID gamma mice and INF-γ-knockout mice (Cryptosporidium mouse models)[1].

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

Animal Model: Murine P. falciparum NODscidIL2Rγnull (SCID) model[1]
Dosage: 1.5 mg/kg
Administration: Orally once a day for 4 days
Result: Reduced parasitemia by 90% in the malaria SCID mouse model.
Animal Model: NOD SCID gamma and INF-γ–knockout mouse models (Cryptosporidium mouse models)[1]
Dosage: 20 mg/kg
Administration: Orally once a day for 7 days
Result: Reduced parasite shedding below detection level, and this reduction was sustained for 3 wk after treatment had stopped in INF-γ-knockout mice. Dosed orally at a concentration of 20 mg/kg once a day for 7 days showed 96% reduction of parasite shedding comparable to paromomycin in NOD SCID gamma mice.
Molecular Weight

355.31

Formula

C17H16F3NO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=C(OC(C(NCC2(O)CCC(F)(F)CC2)=O)=CC3=O)C3=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 60 mg/mL (168.87 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8144 mL 14.0722 mL 28.1444 mL
5 mM 0.5629 mL 2.8144 mL 5.6289 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.5 mg/mL (4.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

COA (245 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen). 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
DMSO 1 mM 2.8144 mL 14.0722 mL 28.1444 mL 70.3611 mL
5 mM 0.5629 mL 2.8144 mL 5.6289 mL 14.0722 mL
10 mM 0.2814 mL 1.4072 mL 2.8144 mL 7.0361 mL
15 mM 0.1876 mL 0.9381 mL 1.8763 mL 4.6907 mL
20 mM 0.1407 mL 0.7036 mL 1.4072 mL 3.5181 mL
25 mM 0.1126 mL 0.5629 mL 1.1258 mL 2.8144 mL
30 mM 0.0938 mL 0.4691 mL 0.9381 mL 2.3454 mL
40 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7590 mL
50 mM 0.0563 mL 0.2814 mL 0.5629 mL 1.4072 mL
60 mM 0.0469 mL 0.2345 mL 0.4691 mL 1.1727 mL
80 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
100 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.7036 mL
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LysRs-IN-2 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.

Keywords:

LysRs-IN-22170696-76-9Aminoacyl-tRNA SynthetasetRNA Synthetase, aaRSInhibitorinhibitorinhibit

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