製品番号: HY-12659

LX7101

3 Cited Publications

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.54%
CAS 番号: 1192189-69-7
分子式: C₂₃H₂₉N₇O₃
分子量:451.52

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LX7101 構造式

CAS 番号: 1192189-69-7

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体内実験
- 臨床実験
化学情報
Publications (3)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

LIMK2

1.6 nM (IC₅₀)

LIMK1

24 nM (IC₅₀)

ROCK2

10 nM (IC₅₀)

PKA

<1 nM (IC₅₀)

LIM Kinase (LIMK) アイソフォーム固有の製品をすべて表示 :

LIMK1
LIMK2

ROCK アイソフォーム固有の製品をすべて表示 :

PKA アイソフォーム固有の製品をすべて表示 :

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	55 μM Compound: LX7101	Cytotoxicity against human HeLa cells assessed as induction of cell death measured after 48 hrs by celltiter glo luminescent cell viability assay Cytotoxicity against human HeLa cells assessed as induction of cell death measured after 48 hrs by celltiter glo luminescent cell viability assay	[PMID: 38669909]
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]

体内実験

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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1192189-69-7
性状 Solid
分子量 451.52
分子式 C₂₃H₂₉N₇O₃
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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

All Cell Proliferation/Viability AssayWB

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Journal Impact Factor

Oncogene

LIMK2 promotes melanoma tumor growth and metastasis through G3BP1-ESM1 pathway-mediated apoptosis inhibition. [Abstract]

2023 May;42(18):1478-1491. PMID: 36922679

LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 May;42(18):1478-1491. [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 May;42(18):1478-1491. [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.
Sci Rep

Loss of the fragile X mental retardation protein causes aberrant differentiation in human neural progenitor cells. [Abstract]

2018 Aug 2;8(1):11585. PMID: 30072797

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.
SSRN

2025 Sep 6.

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	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

Keywords

LX7101

3 Cited Publications

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LX7101

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MedChemExpress（MCE）の使用を引用している文献 LX7101

LIM Kinase (LIMK) アイソフォーム固有の製品をすべて表示

ROCK アイソフォーム固有の製品をすべて表示

PKA アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (3)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

LX7101 関連分類

HY-12659 関連分類