Bomedemstat dihydrochloride
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 592.54 |
| Molecular Formula | C28H36Cl2FN7O2 |
| 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.[H]Cl.[H]Cl |
Summary
Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 ( LSD1 ) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [1] [2] .
IC50 & Target
|
KDM1/LSD1 |
In Vitro
Bomedemstat dihydrochloride selectively inhibits proliferation and induces apoptosis of
Jak2
V617F
cells by concomitantly increasing expression and methylation of p53
[1]
.
Bomedemstat (50 nM-1 μM; 96 h; SET-2 cells) dihydrochloride 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 (oral gavage; 45 mg/kg; once daily; 56 d) dihydrochloride 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- Jak2 V617F 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
