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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[1].

Product Specifications

CAS Number

[2821068-03-3]

Product Name Alternative

S1024

UNSPSC

12352005

Target

Histone Demethylase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cis-4-br-2-5-f2-pcpa.html

Solubility

10 mM in DMSO

Smiles

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

Molecular Formula

C9H8BrF2N

Molecular Weight

248.07

References & Citations

[1]Hideaki Niwa, et al. Structure–Activity Relationship and In Silico Evaluation of cis- and trans-PCPA-Derived Inhibitors of LSD1 and LSD2. ACS Med. Chem. Lett. 2022.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

KDM1/LSD1

Curated Selection

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