LRRK2-IN-1

Name: LRRK2-IN-1
Brand: MedChemExpress
SKU: HY-10875
Rating: 5.0 (7 reviews)

製品番号: HY-10875 純度: 99.04%: Data Sheet SDS COA 取扱説明書
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LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC₅₀ of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

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CAS 番号 : 1234480-84-2

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 98	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 98	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$35	在庫あり	Estimated Time of Arrival: December 31
5 mg	$78	在庫あり	Estimated Time of Arrival: December 31
10 mg	$121	在庫あり	Estimated Time of Arrival: December 31
25 mg	$255	在庫あり	Estimated Time of Arrival: December 31
50 mg	$440	在庫あり	Estimated Time of Arrival: December 31
100 mg	$770	在庫あり	Estimated Time of Arrival: December 31
500 mg	$1815	在庫あり	Estimated Time of Arrival: December 31
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Based on 7 publication(s) in Google Scholar

Other Forms of LRRK2-IN-1:

LRRK2-IN-1 (Standard) お問い合わせ

顧客検証

•Harvard Medical School LINCS LIBRARY

: LRRK2-IN-1 purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2018 Aug 6;15(8):3252-3259. [Abstract]; Western blot analysis the expression of c-Myc and DCLK1 treated with or without LRRK2-IN-1 in Jurkat cells.

: LRRK2-IN-1 purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2018 Nov;38(11):6225-6230. [Abstract]; Effect of 5-FU, LRRK, or 5-FU and LRRK combined treatment on Chk1 phosphorylation.

: LRRK2-IN-1 purchased from MedChemExpress. Usage Cited in: Anticancer Res. 2018 Nov;38(11):6225-6230. [Abstract]; Effect of 5-FU, LRRK treatment, or combined treatment with 5-FU and LRRK on PARP-1 cleavage.

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製品説明

LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC₅₀ of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

IC₅₀ & Target

IC50: 13 nM (WT), 6 nM (G2019S)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	13 nM Compound: LRRK2IN1	Inhibition of wild-type GST-tagged LRRK2 (1326 to 2527 aa)(unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method Inhibition of wild-type GST-tagged LRRK2 (1326 to 2527 aa)(unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method	[PMID: 25791676]
HEK293	IC₅₀	13 nM Compound: LRRK2-IN-1	Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate Inhibition of wild-type LRRK2 expressed in HEK293 cells using nictide and [gamma32]ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	2450 nM Compound: LRRK2-IN-1	Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	3080 nM Compound: LRRK2-IN-1	Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 G2019S and A2016T mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	6 nM Compound: LRRK2-IN-1	Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate Inhibition of LRRK2 G2019S mutant expressed in HEK293 cells using nictide and ATP as substrate	[PMID: 22335897]
HEK293	IC₅₀	7.9 nM Compound: LRRK2IN1	Inhibition of LRRK2 G2019S mutant (1326 to 252 aa) (unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method Inhibition of LRRK2 G2019S mutant (1326 to 252 aa) (unknown origin) stably expressed in HEK293 cell lysate using [gamma-32P] after 15 mins by Cerenkov counting method	[PMID: 25791676]
HEK-293T	IC₅₀	2800 nM Compound: LRRK2-IN-1	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
MM1.S	IC₅₀	530 nM Compound: LRRK2-IN-1	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
U-87MG ATCC	EC₅₀	0.66 μM Compound: LRRK2IN1	Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human U87 cells compound pretreated for 30 mins before stimulation measured after 24 hrs by ELISA Inhibition of IL6 secretion in LPS/IL-1beta-stimulated human U87 cells compound pretreated for 30 mins before stimulation measured after 24 hrs by ELISA	[PMID: 25791676]

体外実験

Wild-type and G2019S transduction results in 2.5 fold higher TR-FRET signal which can be inhibited by LRRK2-IN-1 in a dose-dependent manner with IC₅₀ values of 0.08 μM and 0.03 μM, respectively^[1]. LRRK2-IN-1 possessed an IC₅₀ of 45 nM for inhibition of DCLK2 and exhibits an IC₅₀ of greater than 1 μM when evaluated in biochemical assays for AURKB, CHEK2, MKNK2, MYLK, NUAK1, and PLK1. LRRK2-IN-1 is confirmed to inhibit MAPK7 with an EC₅₀ of 160 nM. LRRK2-IN-1 induces a dose dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells^[2]. LRRK2-IN-1 is moderately cytotoxic with IC₅₀ of 49.3 μM in HepG2 cells. LRRK2-IN-1 exhibits genotoxicity in the presence and absence of S9 at 15.6 and 3.9 μM, respectively^[3]. LRRK2-IN-1 inhibits proliferation, migration, and induces cell death with hallmarks of apoptosis of HCT116 and AsPC-1 cells^[4].

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

体内実験

LRRK2-IN-1 (100 mg/kg, i.p.) induces dephosphorylation of LRRK2 in the kidney of the mice^[2]. Peritumoral injection of LRRK2-IN-1 (100 mg/kg) results in a significant decrease in tumor volume and weight of AsPC-1 tumor xenografts^[4].

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

分子量

570.69

分子式

C₃₁H₃₈N₈O₃

CAS 番号

1234480-84-2

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC(OC)=C(NC2=NC=C3C(N(C4=C(C(N3C)=O)C=CC=C4)C)=N2)C=C1)N5CCC(CC5)N6CCN(CC6)C

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	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 30 mg/mL (52.57 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	1.7523 mL	8.7613 mL	17.5226 mL
5 mM	0.3505 mL	1.7523 mL	3.5045 mL
10 mM	0.1752 mL	0.8761 mL	1.7523 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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 (4.38 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.38 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 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: ≥ 2.5 mg/mL (4.38 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

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(per animal)

Dosing volume
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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.

純度とドキュメンテーション

純度: 99.04%

Select Batch:

データシート (281 KB) SDS (393 KB)

COA (251 KB) HNMR (247 KB) LCMS (93 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Hermanson SB, et al. Screening for Novel LRRK2 Inhibitors Using a High-Throughput TR-FRET Cellular Assay for LRRK2 Ser935 Phosphorylation.PLoS One. 2012;7(8):e43580. Epub 2012 Aug 28. [Content Brief]

[2]. Deng, Xianming., et al. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nature Chemical Biology (2011), 7(4), 203-205.

[3]. Koshibu K, et al. Alternative to LRRK2-IN-1 for Pharmacological Studies of Parkinson's Disease. Pharmacology. 2015;96(5-6):240-7. [Content Brief]

[4]. Weygant N, et al. Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal and pancreatic cancer through inhibition of doublecortin-like kinase 1. Mol Cancer. 2014 May 6;13:103. [Content Brief]

キナーゼ実験 ^[2]	Active GST-LRRK2 (1326-2527), GST-LRRK2 [G2019S] (1326-2527), GST-LRRK2 [A2016T] (1326-2527) and GST-LRRK2 [A2016T+G2019S] (1326-2527) enzyme is purified with glutathione sepharose from HEK293 cell lysate 36 h following transient transfection of the appropriate cDNA constructs. Peptide kinase assays, performed in duplicate, are set up in a total volume of 40 µL containing 0.5 µg LRRK2 kinase (which at approximately 10% purity gives a final concentration of 8 nM) in 50 mM Tris/HCl, pH 7.5, 0.1 mM EGTA, 10 mM MgCl₂, 20 µM Nictide, 0.1 µM [γ-³²P]ATP (500 cpm/pmol) and the indicated concentrations of inhibitor dissolved in DMSO. After incubation for 15 min at 30°C, reactions are terminated by spotting 35 µL of the reaction mix onto P81 phosphocellulose paper and immersion in 50 mM phosphoric acid. Samples are washed extensively and the incorporation of [γ-³²P]ATP into Nictide is quantified by Cerenkov counting. IC₅₀ values are calculated with GraphPad Prism using non-linear regression analysis. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
細胞実験 ^[4]	Cells (10⁴ cells per well) are seeded into a 96-well tissue culture plate in triplicate. The cells are cultured in the presence of LRRK2-IN-1 with DMSO as a vehicle at 0, 0.31, 0.63, 1, 2, and 5, 10, and 20 μM. 48 h post treatment, 10 μL of TACS MTT Reagent is added to each well and the cells are incubated at 37°C until dark crystalline precipitate become visible in the cells. 100 μL of 266 mM NH₄OH in DMSO is then added to the wells and placed on a plate shaker at low speed for 1 minute. After shaking, the plate is allowed to incubate for 10 minutes protected from light and the OD550 for each well is read using a microplate reader. The results are averaged and calculated as a percentage of the DMSO (vehicle) control +/- the standard error of the mean. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[2]	LRRK2-IN-1 is dissolved in Captisol and administered by intraperitoneal injection into wild type male C57BL/6 mice at a dose of 100 mg/kg. Control mice are injected with an equal volume of Captisol. At 1 and 2 h time points, mice are extinguwashed by cervical dislocation and kidney and brain tissue rapidly dissected and snap-frozen in liquid nitrogen. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Hermanson SB, et al. Screening for Novel LRRK2 Inhibitors Using a High-Throughput TR-FRET Cellular Assay for LRRK2 Ser935 Phosphorylation.PLoS One. 2012;7(8):e43580. Epub 2012 Aug 28. [Content Brief] [2]. Deng, Xianming., et al. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nature Chemical Biology (2011), 7(4), 203-205. [3]. Koshibu K, et al. Alternative to LRRK2-IN-1 for Pharmacological Studies of Parkinson's Disease. Pharmacology. 2015;96(5-6):240-7. [Content Brief] [4]. Weygant N, et al. Small molecule kinase inhibitor LRRK2-IN-1 demonstrates potent activity against colorectal and pancreatic cancer through inhibition of doublecortin-like kinase 1. Mol Cancer. 2014 May 6;13:103. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7523 mL	8.7613 mL	17.5226 mL	43.8066 mL
	5 mM	0.3505 mL	1.7523 mL	3.5045 mL	8.7613 mL
	10 mM	0.1752 mL	0.8761 mL	1.7523 mL	4.3807 mL
	15 mM	0.1168 mL	0.5841 mL	1.1682 mL	2.9204 mL
	20 mM	0.0876 mL	0.4381 mL	0.8761 mL	2.1903 mL
	25 mM	0.0701 mL	0.3505 mL	0.7009 mL	1.7523 mL
	30 mM	0.0584 mL	0.2920 mL	0.5841 mL	1.4602 mL
	40 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	50 mM	0.0350 mL	0.1752 mL	0.3505 mL	0.8761 mL

LRRK2-IN-1 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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:

LRRK2-IN-11234480-84-2LRRK2ApoptosisLeucine-rich repeat kinase 2Inhibitorinhibitorinhibit

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LRRK2-IN-1

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Other Forms of LRRK2-IN-1:

LRRK2-IN-1 関連抗体

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おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

LRRK2-IN-1 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

LRRK2-IN-1 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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