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Sigma-Aldrich

LSD1 Inhibitor III, CBB1007

The LSD1 Inhibitor III, CBB1007 controls the biological activity of LSD1. This small molecule/inhibitor is primarily used for Cell Structure applications.

Synonym(s):

LSD1 Inhibitor III, CBB1007, LSD Inhibitor III, BHC110 Inhibitor III, Methyl-3-(4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl)-5-((4-carbamimidoylpiperazin-1-yl)methyl)benzoate, 3TFA, KDM1 Inhibitor III, Histone Lysine Demethylase Inhibitor V, LSD Inhibitor III, Methyl-3-(4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl)-5-((4-carbamimidoylpiperazin-1-yl)methyl)benzoate, 3TFA, KDM1 Inhibitor III, Histone Lysine Demethylase Inhibitor V, BHC110 Inhibitor III

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About This Item

Empirical Formula (Hill Notation):
C27H34N8O4 · 3C2HF3O2
CAS Number:
1379573-92-8
Molecular Weight:
876.68
MDL number:
MFCD25976706
UNSPSC Code:
12352200

Quality Level

100

Assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

white

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

SMILES string

NC(N1CCN(CC2=CC(C(N3CCN(C(C4=CC=C(C(N)=N)C=C4)=O)CC3)=O)=CC(C(OC)=O)=C2)CC1)=N

General description

A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 >100 µM).

Note: the molecular weight is lot-specific and can be found on the vial label.
A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 µM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 µM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 µM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 µM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 >100 µM).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Wang, J., et al. 2011. Cancer Res.71, 7238.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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