GSK2879552

Name: GSK2879552
Brand: MedChemExpress
SKU: HY-18632
Rating: 5.0 (19 reviews)

製品番号: HY-18632 純度: 99.98%: Data Sheet SDS COA 取扱説明書
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GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity.

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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。

CAS 番号 : 1401966-69-5

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 96	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 96	在庫あり	Estimated Time of Arrival: December 31
Solid
1 mg	$41	在庫あり	Estimated Time of Arrival: December 31
5 mg	$88	在庫あり	Estimated Time of Arrival: December 31
10 mg	$140	在庫あり	Estimated Time of Arrival: December 31
25 mg	$270	在庫あり	Estimated Time of Arrival: December 31
50 mg	$450	在庫あり	Estimated Time of Arrival: December 31
100 mg	$850	在庫あり	Estimated Time of Arrival: December 31
1 g	$2750	在庫あり	Estimated Time of Arrival: December 31
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* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 19 publication(s) in Google Scholar

Other Forms of GSK2879552:

GSK2879552 dihydrochloride 在庫あり

顧客検証

Histological Imaging/Staining

In Vivo Efficacy Study

Bio/Physico-chemical Assay

Flow Cytometry

: GSK2879552 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327. [Abstract]; Principal component analysis (PCA) of RNA-seq data of mouse CD8⁺ T cells activated and expanded in vitro for 5 days with the treatment of GSK2879552 (GSK) or vehicle control (Veh) (n = 3 mice per group).

: GSK2879552 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 May 21;15(1):4327. [Abstract]; Flow cytometry analysis of frequencies of CD44⁺CD62L⁺ cells in GSK2879552- or Veh-treated CD8⁺ T cells (n = 3).

: GSK2879552 purchased from MedChemExpress. Usage Cited in: Natl Sci Rev. 2023 Feb 14;10(4):nwad028.; Images of H&E staining for individual lungs of KL mice treated with vehicle or GSK2879552.

: GSK2879552 purchased from MedChemExpress. Usage Cited in: Natl Sci Rev. 2023 Feb 14;10(4):nwad028.; Representative H&E staining in KL mice treated with vehicle (n = 5) or GSK2879552.

: GSK2879552 purchased from MedChemExpress. Usage Cited in: Natl Sci Rev. 2023 Feb 14;10(4):nwad028.; Quantification of AST incidence and tumor burden of KL mice treated with vehicle (n = 5) or GSK2879552 (1.5 mg/kg, ip, daily, 4 weeks).

: GSK2879552 purchased from MedChemExpress. Usage Cited in: Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287. [Abstract]; The protein expression of LSD1, PRB and H3K4me2 is detected through Western blot with GSK2879552 treatment in different cells.

Histone Demethylase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

生物活性
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

製品説明

GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity^[1]^[2].

IC₅₀ & Target

KDM1/LSD1

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	>10 3 Compound: GSk2879552; 2	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
ECa-109 cell line	IC₅₀	>50 3 Compound: GSK2879552	Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
HCT-116	IC₅₀	>64 3 Compound: GSK-2879552	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
Small cell lung cancer cell line	IC₅₀	24 1 Compound: GSK2879552	Antiproliferative activity against human SCLC cell Antiproliferative activity against human SCLC cell	[PMID: 35820351]
Kasumi 1	GI₅₀	0.02 3 Compound: 3; GSK2879552	Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay	[PMID: 32551003]
DU-145	GI₅₀	> 10 3 Compound: GSk2879552; 2	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
KYSE-450	IC₅₀	>64 3 Compound: GSK-2879552	Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
HCT-116	IC₅₀	> 64 3 Compound: GSK-2879552	Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human HCT-116 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
KYSE-450	IC₅₀	> 64 3 Compound: GSK-2879552	Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human KYSE-450 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
MGC-803	IC₅₀	>125 3 Compound: GSK2879552	Antiproliferative activity against human MGC803 cells after 5 days by MTT assay Antiproliferative activity against human MGC803 cells after 5 days by MTT assay	[PMID: 28435523]
MGC-803	IC₅₀	>64 3 Compound: GSK-2879552	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
Kasumi 1	GI₅₀	0.02 3 Compound: 3; GSK2879552	Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay	[PMID: 32551003]
MGC-803	IC₅₀	>50 3 Compound: GSK2879552	Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
MGC-803	IC₅₀	> 125 3 Compound: GSK2879552	Antiproliferative activity against human MGC803 cells after 5 days by MTT assay Antiproliferative activity against human MGC803 cells after 5 days by MTT assay	[PMID: 28435523]
MGC-803	IC₅₀	> 50 3 Compound: GSK2879552	Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
MV4-11	EC₅₀	0.023 3 Compound: 5; GSK2879552	Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis	[PMID: 35200034]
MV4-11	EC₅₀	0.054 3 Compound: 3; GSK2879552	Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method	[PMID: 32551003]
MGC-803	IC₅₀	> 64 3 Compound: GSK-2879552	Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay Antiproliferative activity against human MGC-803 cells incubated for 48 hrs measured by MTT assay	[PMID: 36881982]
MV4-11	IC₅₀	1.16 3 Compound: GSK2879552	Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay	[PMID: 30713023]
MV4-11	IC₅₀	1.19 3 Compound: 5; GSK2879552	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
MV4-11	EC₅₀	0.023 3 Compound: 5; GSK2879552	Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis	[PMID: 35200034]
MV4-11	EC₅₀	0.054 3 Compound: 3; GSK2879552	Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method	[PMID: 32551003]
PC-3	GI₅₀	>10 3 Compound: GSk2879552; 2	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
RPMI-8226	IC₅₀	>20 3 Compound: 5; GSK2879552	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
MV4-11	IC₅₀	1.16 3 Compound: GSK2879552	Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay	[PMID: 30713023]
MV4-11	IC₅₀	1.19 3 Compound: 5; GSK2879552	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
NCI-H1417	EC₅₀	0.8 31 Compound: Chemical Probe: GSK2879552	Antitumor activity against human NCI-H1417 cells xenografted in nude mouse assessed as decrease in GRP expression single administration measured after 24 hrs by by qRT-PCR analysis Antitumor activity against human NCI-H1417 cells xenografted in nude mouse assessed as decrease in GRP expression single administration measured after 24 hrs by by qRT-PCR analysis	[PMID: 26175415]
PC-3	GI₅₀	> 10 3 Compound: GSk2879552; 2	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
RPMI-8226	IC₅₀	> 20 3 Compound: 5; GSK2879552	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
Small cell lung cancer cell line	IC₅₀	24 1 Compound: GSK2879552	Antiproliferative activity against human SCLC cell Antiproliferative activity against human SCLC cell	[PMID: 35820351]

体外実験

GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of Sorafenib (HY-10201)-resistant cells and attenuating stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in Sorafenib-resistant cells^[1].

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

Cell Proliferation Assay^[2].

Cell Line:	9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
Concentration:	0-10000 nM.
Incubation Time:	6 days.
Result:	Inhibited cell proliferation.

RT-PCR^[1].

Cell Line:	Resistant HCC cells (PLC/PRF/5 and Huh7).
Concentration:	0, 1, 2 μM.
Incubation Time:	24 h.
Result:	Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

体内実験

GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft-bearing mice^[2].

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

Animal Model:	NCI-H526 and NCI-H1417 xenografts^[2].
Dosage:	1.5 mg/kg.
Administration:	PO daily for 25-35 days.
Result:	There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

分子量

364.48

分子式

C₂₃H₂₈N₂O₂

CAS 番号

1401966-69-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(CN2CCC(CN[C@H]3[C@H](C4=CC=CC=C4)C3)CC2)C=C1

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 : 25 mg/mL (68.59 mM; ultrasonic and warming and heat to 60°C; 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	2.7436 mL	13.7182 mL	27.4363 mL
5 mM	0.5487 mL	2.7436 mL	5.4873 mL
10 mM	0.2744 mL	1.3718 mL	2.7436 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: ≥ 2.75 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (7.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 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.

純度とドキュメンテーション

純度: 99.98%

Select Batch:

データシート (274 KB) SDS (393 KB)

COA (244 KB) HNMR (165 KB) RP-HPLC (256 KB) MS (69 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21 [Content Brief]

[2]. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7436 mL	13.7182 mL	27.4363 mL	68.5909 mL
	5 mM	0.5487 mL	2.7436 mL	5.4873 mL	13.7182 mL
	10 mM	0.2744 mL	1.3718 mL	2.7436 mL	6.8591 mL
	15 mM	0.1829 mL	0.9145 mL	1.8291 mL	4.5727 mL
	20 mM	0.1372 mL	0.6859 mL	1.3718 mL	3.4295 mL
	25 mM	0.1097 mL	0.5487 mL	1.0975 mL	2.7436 mL
	30 mM	0.0915 mL	0.4573 mL	0.9145 mL	2.2864 mL
	40 mM	0.0686 mL	0.3430 mL	0.6859 mL	1.7148 mL
	50 mM	0.0549 mL	0.2744 mL	0.5487 mL	1.3718 mL
	60 mM	0.0457 mL	0.2286 mL	0.4573 mL	1.1432 mL

GSK2879552 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

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:

GSK28795521401966-69-5GSK 2879552GSK-2879552Histone DemethylaseInhibitorinhibitorinhibit

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GSK2879552

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Other Forms of GSK2879552:

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Histone Demethylase アイソフォーム固有の製品をすべて表示:

生物活性

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

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK2879552 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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GSK2879552

カスタマーレビュー

Other Forms of GSK2879552:

GSK2879552 関連抗体

顧客検証

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:

Histone Demethylase アイソフォーム固有の製品をすべて表示:

生物活性

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

GSK2879552 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GSK2879552 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report