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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Bomedemstat hydrochloride, Bomedemstat dihydrochloride and Bomedemstat ditosylate) that retains the same biological activity.

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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Bomedemstat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Bomedemstat

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View All Isoforms
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

Oil

Color

Colorless to light yellow

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
Pure form -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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