GSK2879552 dihydrochloride

Name: GSK2879552 dihydrochloride
Brand: MedChemExpress
SKU: HY-18632A
Rating: 5.0 (16 reviews)

Cat. No.: HY-18632A Purity: 99.19%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

GSK2879552 dihydrochloride Chemical Structure

CAS No. : 1902123-72-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 97	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 97	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of GSK2879552 dihydrochloride:

GSK2879552 In-stock

15 Publications Citing Use of MCE GSK2879552 dihydrochloride

: GSK2879552 dihydrochloride 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.

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
Purity & Documentation
References
Customer Review

Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	> 10 μM 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 μM 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]
Kasumi 1	GI₅₀	0.02 μM 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	> 125 μM 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 μM 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 μM 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 μM 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]
MV4-11	IC₅₀	1.16 μM 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 μM 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]
PC-3	GI₅₀	> 10 μM 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 μM 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]

In Vitro

GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates 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 Viability 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.

In Vivo

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.

Clinical Trial

Molecular Weight

437.40

Formula

C₂₃H₃₀Cl₂N₂O₂

CAS No.

1902123-72-1

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.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (228.62 mM; Need ultrasonic)

DMSO : 31.25 mg/mL (71.44 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	2.2862 mL	11.4312 mL	22.8624 mL
5 mM	0.4572 mL	2.2862 mL	4.5725 mL
10 mM	0.2286 mL	1.1431 mL	2.2862 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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: ≥ 2.5 mg/mL (5.72 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 (5.72 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 (5.72 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 8.33 mg/mL (19.04 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.19%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (245 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[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 / H₂O	1 mM	2.2862 mL	11.4312 mL	22.8624 mL	57.1559 mL
	5 mM	0.4572 mL	2.2862 mL	4.5725 mL	11.4312 mL
	10 mM	0.2286 mL	1.1431 mL	2.2862 mL	5.7156 mL
	15 mM	0.1524 mL	0.7621 mL	1.5242 mL	3.8104 mL
	20 mM	0.1143 mL	0.5716 mL	1.1431 mL	2.8578 mL
	25 mM	0.0914 mL	0.4572 mL	0.9145 mL	2.2862 mL
	30 mM	0.0762 mL	0.3810 mL	0.7621 mL	1.9052 mL
	40 mM	0.0572 mL	0.2858 mL	0.5716 mL	1.4289 mL
	50 mM	0.0457 mL	0.2286 mL	0.4572 mL	1.1431 mL
	60 mM	0.0381 mL	0.1905 mL	0.3810 mL	0.9526 mL
H₂O	80 mM	0.0286 mL	0.1429 mL	0.2858 mL	0.7144 mL
H₂O	100 mM	0.0229 mL	0.1143 mL	0.2286 mL	0.5716 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.