1. Epigenetics
  2. Histone Demethylase
  3. Bomedemstat

Bomedemstat (Synonyms: IMG-7289)

Cat. No.: HY-109169
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Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic 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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Description

Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1].

In Vitro

Bomedemstat (IMG-7289) selectively inhibits proliferation and induces apoptosis of JAK2V617F cells by concomitantly increasing expression and methylation of p53, and, independently, the pro-apoptotic factor PUMA and by decreasing the levels of its antiapoptotic antagonist BCL-XL[1]
Bomedemstat (25  nM, 50  nM) and Ruxolitinib (175  nM) synergize in inhibiting JAK2V617F-driven proliferation[1].
Bomedemstat (50 and 100 nM) exerts a pro-apoptotic effect on 3 key regulators of programmed cell death, TP53, BCL-XL, and PUMA[1].

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

Cell Viability Assay[1]

Cell Line: The human cell lines SET-2 (ATCC 608) and HEK293
Concentration: 25  nM, 50 nM
Incubation Time: 96 hours
Result: 25 nM alone significantly reduced colony formation.

Western Blot Analysis[1]

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

Once-daily treatment with Bomedemstat (IMG-7289; 45  mg/kg) 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: Mx1cre-Jak2V617F mice[1]
Dosage: 45  mg/kg
Administration: Administered daily by oral gavage for either 14, 42, or 56 consecutive days
Result: In this Mx-Jak2V617F model of myeloproliferative neoplasm (MPN), mice developed severe splenomegaly (up to 10-fold increase in spleen weight). Splenic architecture was completely destroyed, eliminating demarcation of the white and red pulp. Treatment significantly reduced splenomegaly with a few treated mice normalizing their spleen weight. Remarkably, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.
Molecular Weight

519.61

Formula

C₂₈H₃₄FN₇O₂

CAS No.
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Bomedemstat
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