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

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.

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Bomedemstat Chemical Structure

Bomedemstat Chemical Structure

CAS No. : 1990504-34-1

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Based on 3 publication(s) in Google Scholar

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Bomedemstat Related Antibodies

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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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].

IC50 & Target

KDM1/LSD1

 

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].

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

Bomedemstat Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Bomedemstat Related Classifications

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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.

Keywords:

Bomedemstat1990504-34-1IMG-7289IMG7289IMG 7289Histone DemethylaseApoptosisoral activitylysine-specific demethylase 1anti-cancer activityanti-proliferationinduce apoptosisSET-2Inhibitorinhibitorinhibit

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