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Cat. No.: HY-151190

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

Name: cis-4-Br-2,5-F2-PCPA
Brand: MedChemExpress
SKU: HY-151190
Availability: PreOrder

(Synonyms: S1024)

cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a K_i 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.

CAS No.: 2821068-03-3
Formula: C₉H₈BrF₂N
Molecular Weight:248.07

Storage:

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

Data Sheet (267 KB)

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

CAS No.: 2821068-03-3

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

KDM1/LSD1

All Histone Demethylase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	12 μM Compound: 7c	Anti-proliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay Anti-proliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay	[PMID: 36105323]
Jurkat	IC₅₀	16 μM Compound: 7c	Anti-proliferative activity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay Anti-proliferative activity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay	[PMID: 36105323]
WI-38	IC₅₀	>50 μM Compound: 7c	Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay Cytotoxicity against human WI-38 cells assessed as reduction in cell viability after 72 hrs by AlamarBlue assay	[PMID: 36105323]

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.

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.

Chemical Information

CAS No. 2821068-03-3
Molecular Weight 248.07
Formula C₉H₈BrF₂N
SMILES

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

S1024
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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

All Histone Demethylase Isoforms