1. Epigenetics
    Apoptosis
  2. Histone Demethylase
    Apoptosis
  3. Bomedemstat

Bomedemstat  (Synonyms: IMG-7289)

Cat. No.: HY-109169
COA Handling Instructions

Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis.

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

Bomedemstat Chemical Structure

Bomedemstat Chemical Structure

CAS No. : 1990504-34-1

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Description

Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis[1][2].

In Vitro

Bomedemstat selectively inhibits proliferation and induces apoptosis of Jak2V617F cells by concomitantly increasing expression and methylation of p53[1].
Bomedemstat (50 nM-1 μM; 96 h) enhances survival, induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner, and leads to cell cycle arrest[1].

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

Apoptosis Analysis[1]

Cell Line: SET-2 cells
Concentration: 50 nM, 100 nM, and 1 μM
Incubation Time: 96 hours
Result: Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA.
In Vivo

Bomedemstat treatment (oral gavage; 45 mg/kg; once daily; 56 d) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].

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

Animal Model: Mx-Jak2V617F mice[1]
Dosage: 45 mg/kg
Administration: Oral gavage; 45 mg/kg; once daily; 56 days
Result: Reduced splenomegaly significantly with a few treated mice normalizing their spleen weight, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.
Clinical Trial
Molecular Weight

519.61

Formula

C28H34FN7O2

CAS No.
SMILES

O=C(N1CCN(CC1)C)[[email protected]@H](NC(C2=CC=C(N3C=CN=N3)C=C2)=O)CCCN[[email protected]]4[[email protected]@](C5=CC=C(C=C5)F)([H])C4

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Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (192.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9245 mL 9.6226 mL 19.2452 mL
5 mM 0.3849 mL 1.9245 mL 3.8490 mL
10 mM 0.1925 mL 0.9623 mL 1.9245 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bomedemstat
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HY-109169
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