1. Epigenetics
  2. Histone Demethylase
  3. cis-4-Br-2,5-F2-PCPA

cis-4-Br-2,5-F2-PCPA (Synonyms: S1024)

Cat. No.: HY-151190
Handling Instructions

cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells.

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

cis-4-Br-2,5-F2-PCPA Chemical Structure

cis-4-Br-2,5-F2-PCPA Chemical Structure

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Description

cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells[1].

IC50 & Target

Ki: 94 nM (LSD1); 8.4 μM (LSD2)[1]

In Vitro

cis-4-Br-2,5-F2-PCPA (compound 7c) inhibits proliferation of the T-cell acute lymphoblastic leukemia (T-ALL) with IC50s of 12 μM (CCRF-CEM) and 16 μM (Jurkat), respectively, without inhibiting the human normal fibroblast cell line WI-38[1].
cis-4-Br-2,5-F2-PCPA (20 μM; 24 h) significantly increases the level of dimethylated H3K4 (H3K4me2), and exerts chemical inhibition on LSD1 and LSD2[1].

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

Western Blot Analysis[1]

Cell Line: T-cell acute lymphoblastic leukemia (T-ALL)
Concentration: 20 μM
Incubation Time: 24 hours
Result: Increased the level of dimethylated H3K4 (H3K4me2) 2.9-fold compared with control.
Molecular Weight

248.07

Formula

C9H8BrF2N

SMILES

N[[email protected]@H]1C[[email protected]@H]1C2=C(F)C=C(Br)C(F)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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cis-4-Br-2,5-F2-PCPA
Cat. No.:
HY-151190
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