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

MedChemExpress (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].

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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (192.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9245 mL 9.6226 mL 19.2452 mL 48.1130 mL
5 mM 0.3849 mL 1.9245 mL 3.8490 mL 9.6226 mL
10 mM 0.1925 mL 0.9623 mL 1.9245 mL 4.8113 mL
15 mM 0.1283 mL 0.6415 mL 1.2830 mL 3.2075 mL
20 mM 0.0962 mL 0.4811 mL 0.9623 mL 2.4057 mL
25 mM 0.0770 mL 0.3849 mL 0.7698 mL 1.9245 mL
30 mM 0.0642 mL 0.3208 mL 0.6415 mL 1.6038 mL
40 mM 0.0481 mL 0.2406 mL 0.4811 mL 1.2028 mL
50 mM 0.0385 mL 0.1925 mL 0.3849 mL 0.9623 mL
60 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8019 mL
80 mM 0.0241 mL 0.1203 mL 0.2406 mL 0.6014 mL
100 mM 0.0192 mL 0.0962 mL 0.1925 mL 0.4811 mL
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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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