LX7101

Name: LX7101
Brand: MedChemExpress
SKU: HY-12659
Rating: 5.0 (5 reviews)

Cat. No.: HY-12659 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

LX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC₅₀s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC₅₀ values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research.

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

LX7101 Chemical Structure

CAS No. : 1192189-69-7

Size	Stock	Quantity

Free Sample (0.1 - 0.5 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of LX7101:

LX7101 monohydrochloride Get quote

2 Publications Citing Use of MCE LX7101

Proliferation Assay

: LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Mar 16. [Abstract]; Both LX7101 (5 μM) and TH-257 (5 μM) inhibits the colony-forming ability of melanoma cells (A375-MA2, MeWo, and SK-MEL-147 cells) in soft-agar.

: LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Mar 16. [Abstract]; Both LX7101 (5 μM; 24 h) and TH-257 (5 μM; 24 h) reduces the phosphorylation of G3BP1 in A375-MA2 and SK-MEL-147 cells.

: LX7101 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Aug 2;8(1):11585. [Abstract]; Western blot analysis of GFAP protein levels in LX7101 and DMSO-treated iNPC-KO lines. GAPDH is used as a loading control.

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•Related Screening Libraries:

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View All LIM Kinase (LIMK) Isoform Specific Products:

View All Isoforms

LIMK1 LIMK2

View All ROCK Isoform Specific Products:

View All Isoforms

ROCK ROCK1 ROCK2

View All PKA Isoform Specific Products:

View All Isoforms

PKA PKAR

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

LIMK2

1.6 nM (IC₅₀)

LIMK1

24 nM (IC₅₀)

ROCK2

10 nM (IC₅₀)

PKA

<1 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A7R5	EC₅₀	2300 nM Compound: LX-7101	Inhibition of ROCK in rat A7r5 cells assessed as reduction in MLC Thr18/Ser19 phosphorylation by direct-ELISA method Inhibition of ROCK in rat A7r5 cells assessed as reduction in MLC Thr18/Ser19 phosphorylation by direct-ELISA method	[PMID: 26233434]
HeLa	EC₅₀	8.7 nM Compound: LX-7101	Inhibition of LIMK in human HeLa cells assessed as reduction in cofilin Ser3 phosphorylation by sandwich immunoassay Inhibition of LIMK in human HeLa cells assessed as reduction in cofilin Ser3 phosphorylation by sandwich immunoassay	[PMID: 26233434]

In Vivo

LX7101 (200 μg/40 μL eye drop) displays a significant intraocular pressure (IOP) reduction at time points ranging from 1 h to 6 h post administration in ocular normotensive New Zealand White (NZW) rabbits^[1].

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

Clinical Trial

Molecular Weight

451.52

Formula

C₂₃H₂₉N₇O₃

CAS No.

1192189-69-7

Appearance

Solid

Color

White to off-white

SMILES

NCC1(C(NC2=CC(OC(N(C)C)=O)=CC=C2)=O)CCN(C3=C4C(NC=C4C)=NC=N3)CC1

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 : 150 mg/mL (332.21 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	2.2147 mL	11.0737 mL	22.1474 mL
5 mM	0.4429 mL	2.2147 mL	4.4295 mL
10 mM	0.2215 mL	1.1074 mL	2.2147 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 7.5 mg/mL (16.61 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (16.61 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 7.5 mg/mL (16.61 mM); Clear solution

This protocol yields a clear solution of ≥ 7.5 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 (75.0 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)

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: 99.75%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (254 KB) LCMS (263 KB)

Handling Instructions (2659 KB)

References

[1]. Boland S, et al. Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorganic & Medicinal Chemistry Letters (2015), 25(18), 4005-4010. [Content Brief]

[2]. Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2147 mL	11.0737 mL	22.1474 mL	55.3685 mL
	5 mM	0.4429 mL	2.2147 mL	4.4295 mL	11.0737 mL
	10 mM	0.2215 mL	1.1074 mL	2.2147 mL	5.5369 mL
	15 mM	0.1476 mL	0.7382 mL	1.4765 mL	3.6912 mL
	20 mM	0.1107 mL	0.5537 mL	1.1074 mL	2.7684 mL
	25 mM	0.0886 mL	0.4429 mL	0.8859 mL	2.2147 mL
	30 mM	0.0738 mL	0.3691 mL	0.7382 mL	1.8456 mL
	40 mM	0.0554 mL	0.2768 mL	0.5537 mL	1.3842 mL
	50 mM	0.0443 mL	0.2215 mL	0.4429 mL	1.1074 mL
	60 mM	0.0369 mL	0.1846 mL	0.3691 mL	0.9228 mL
	80 mM	0.0277 mL	0.1384 mL	0.2768 mL	0.6921 mL
	100 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5537 mL

LX7101 Related Classifications

Endocrinology

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:

LX71011192189-69-7LX 7101LX-7101LIM Kinase (LIMK)ROCKPKALIMKsRho-associated protein kinaseRho-associated kinaseRho-kinaseROKProtein kinase Aocular hypertensionglaucomaInhibitorinhibitorinhibit

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LX7101

Customer Review

Other Forms of LX7101:

LX7101 Related Antibodies

2 Publications Citing Use of MCE LX7101

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All LIM Kinase (LIMK) Isoform Specific Products:

View All ROCK Isoform Specific Products:

View All PKA Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

LX7101 Related Classifications

Keywords:

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Customer Review

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