1. Epigenetics
  2. Histone Demethylase

GSK2879552 

Cat. No.: HY-18632 Purity: 99.82%
Data Sheet SDS Handling Instructions

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

For research use only. We do not sell to patients.
GSK2879552 Chemical Structure

GSK2879552 Chemical Structure

CAS No. : 1401966-69-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $143 In-stock
5 mg $130 In-stock
10 mg $170 In-stock
50 mg $600 In-stock
100 mg $990 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

In Vitro

GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of sorafenib-resistant cells and attenuates stemness properties. GSK2879552 derepresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in sorafenib-resistant cells[1]. GSK2879552 is 280-fold selective over D-amino acid oxidase, allowing for direct comparison of inactivation efficiency (KIapp=520 ± 170 μM, kinact=0.12 ± 0.01 min−1, kinact/KIapp=2.3×10-4 ± 1.31×10-5 min-1 μM-1). GSK2879552 inhibits the growth of 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines, with EC50 of 2-240 nM[2].

In Vivo

GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft bearing mice. There is 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 demonstrate partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI is observed for SHP77 bearing mice[2].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

Viable cells are measured in Cell Counting Kit-8 (CCK8) assay. Briefly, cells are cultured in a 96-well plate overnight at a density of 5×103 cells per well and treated with the indicated concentrations of sorafenib (0 μM, 40 μM or 80 μM) for 24 h. Subsequently, the cells are incubated with 10 μL CCK8 for 60 min at 37°C, 5% CO2. The absorbance of optical density at 450 nm (A450) is determined with Varioskan Flash. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

364.48

Formula

C₂₃H₂₈N₂O₂

CAS No.

1401966-69-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
GSK2879552
Cat. No.:
HY-18632
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