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

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.

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

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

CAS No. : 2821068-03-3

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Other Forms of cis-4-Br-2,5-F2-PCPA:

cis-4-Br-2,5-F2-PCPA Related Antibodies

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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

KDM1/LSD1

 

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].

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

cis-4-Br-2,5-F2-PCPA Related Antibodies

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
CAS No.
SMILES

N[C@@H]1C[C@@H]1C2=C(F)C=C(Br)C(F)=C2
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Purity & Documentation
References
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cis-4-Br-2,5-F2-PCPA Related Classifications

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Keywords:

cis-4-Br-2,5-F2-PCPA2821068-03-3S1024S 1024S-1024Histone Demethylasedemethylates mono- and dimethylated lysineH3K4H3K9T-cell acute lymphoblastic leukemiaT-ALL2-phenylcyclopropylaminePCPAInhibitorinhibitorinhibit

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