2. Protein Tyrosine Kinase/RTK
  3. Src
  4. Lck Inhibitor

Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.

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Lck Inhibitor Chemical Structure

Lck Inhibitor Chemical Structure

CAS No. : 847950-09-8

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 166 In-stock
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10 mg USD 226 In-stock
50 mg USD 907 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Lck Inhibitor:

Lck Inhibitor Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lck Inhibitor

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Lck Fyn Blk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis[1].

Cellular Effect
Cell Line Type Value Description References
Jurkat IC50
0.49 μM
Compound: 25
Cytotoxicity against human Jurkat T cells assessed as cell viability after 72 hrs
Cytotoxicity against human Jurkat T cells assessed as cell viability after 72 hrs
[PMID: 18278858]
Lymphocyte IC50
0.047 μM
Compound: 25
Inhibition of T cell activation in human peripheral blood lymphocytes by mixed lymphocyte reaction
Inhibition of T cell activation in human peripheral blood lymphocytes by mixed lymphocyte reaction
[PMID: 18278858]
In Vitro

Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC50=0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC50=0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT)[1].

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

Lck Inhibitor Related Antibodies
In Vivo

Lck Inhibitor (0-60 mg/kg; p.o.; once daily; from day 9 today 17) shows a dose-dependent inhibition of arthritis[1].
? Lck Inhibitor (p.o.; 5 mg/kg) treatment shows the Cmax, AUC0-∞, tmax and F% are 82 ng/mL, 862 ng h/mL, and 17%, respectively[1].

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

Animal Model: Male Lewis rat (adjuvant-inducedarthritis model) [1]
Dosage: 0, 30, and 60 mg/kg
Administration: P.o.; once daily; from day 9 today 17
Result: Showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg.
Animal Model: Sprague-Dawley Rats[1]
Dosage: P.o. (Pharmacokinetic Analysis)
Administration: 5 mg/kg
Result: The Cmax, AUC0-∞, tmax and F% were 82 ng/mL, 862 ng h/mL, and 17%, respectively.
Molecular Weight

530.62

Formula

C31H30N8O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C2=C(C)C=CC=C2C)C3=NC4=CC=CC=C4N3C5=NC(NC6=CC=C(N7CCN(C)CC7)C=C6)=NC=C15
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (188.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8846 mL 9.4229 mL 18.8459 mL
5 mM 0.3769 mL 1.8846 mL 3.7692 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 mg/mL (4.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).
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: 99.45%

SDS (252 KB)

COA (264 KB) LCMS (97 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8846 mL 9.4229 mL 18.8459 mL 47.1147 mL
5 mM 0.3769 mL 1.8846 mL 3.7692 mL 9.4229 mL
10 mM 0.1885 mL 0.9423 mL 1.8846 mL 4.7115 mL
15 mM 0.1256 mL 0.6282 mL 1.2564 mL 3.1410 mL
20 mM 0.0942 mL 0.4711 mL 0.9423 mL 2.3557 mL
25 mM 0.0754 mL 0.3769 mL 0.7538 mL 1.8846 mL
30 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5705 mL
40 mM 0.0471 mL 0.2356 mL 0.4711 mL 1.1779 mL
50 mM 0.0377 mL 0.1885 mL 0.3769 mL 0.9423 mL
60 mM 0.0314 mL 0.1570 mL 0.3141 mL 0.7852 mL
80 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5889 mL
100 mM 0.0188 mL 0.0942 mL 0.1885 mL 0.4711 mL
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Lck Inhibitor 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:

Lck Inhibitor847950-09-8SrcTcellproliferationarthritisoralselectiveInhibitorinhibitorinhibit

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