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OSMI-1

Cat. No. M8587
OSMI-1 Structure
Synonym:

OSMI1

Size Price Availability
5mg USD 150  USD150 4-7 Days
10mg USD 250  USD250 4-7 Days
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Quality Control & Documentation
Biological Activity

OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.

Chemical Information
Molecular Weight 563.64
Formula C28H25N3O6S2
CAS Number 1681056-61-0
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Su-Jin Lee, et al. OSMI-1 Enhances TRAIL-Induced Apoptosis through ER Stress and NF-κB Signaling in Colon Cancer Cells

[2] Su Jin Lee, et al. O-GlcNAc Transferase Inhibitor Synergistically Enhances Doxorubicin-Induced Apoptosis in HepG2 Cells

[3] Anna Barkovskaya, et al. Inhibition of O-GlcNAc transferase activates tumor-suppressor gene expression in tamoxifen-resistant breast cancer cells

[4] Vivek Makwana, et al. Investigating the Impact of OGT Inhibition on Doxorubicin- and Docetaxel-Induced Cytotoxicity in PC-3 and WPMY-1 Cells

[5] Shan Lu, et al. Hyperglycemia Acutely Increases Cytosolic Reactive Oxygen Species via O-linked GlcNAcylation and CaMKII Activation in Mouse Ventricular Myocytes

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Keywords: OSMI-1, OSMI1 supplier, Transferase, inhibitors, activators


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