ST 045849

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Cat.No. 6775 - ST 045849 | C23H27ClN2O3S | CAS No. 442665-87-4
Description: O-GlcNAc transferase (OGT) inhibitor
Chemical Name: 2-[(4-Chlorophenyl)imino]tetrahydro-4-oxo-3-(2-tricyclo[3.3.1.13,7]dec-1-ylethyl)-2H-1,3-thiazine-6-carboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

O-GlcNAc transferase (OGT) inhibitor (IC50 = 53 μM). Reduces proliferation and viability of prostate cancer cells in vitro. Depletes intracellular alanine and decreases glucose consumption by cancer cells. Decreases markers of ER stress and apoptosis in pregnant diabetic mice and reduces neural tube defects in embryos from diabetic mice.

Technical Data

M. Wt 446.99
Formula C23H27ClN2O3S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 442665-87-4
PubChem ID 4297469
InChI Key HLPZEZRNGAXCJH-UHFFFAOYSA-N
Smiles OC(C1CC(N(/C(S1)=N/C2=CC=C(C=C2)Cl)CCC34CC5CC(C4)CC(C3)C5)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.7 100
ethanol 44.7 100

Preparing Stock Solutions

The following data is based on the product molecular weight 446.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.24 mL 11.19 mL 22.37 mL
5 mM 0.45 mL 2.24 mL 4.47 mL
10 mM 0.22 mL 1.12 mL 2.24 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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References

References are publications that support the biological activity of the product.

Itkonen et al (2016) Inhibition of O-GlcNAc transferase activity reprograms prostate cancer cell metabolism. Oncotarget 7 12464 PMID: 26824323

Kim et al (2017) Impact of protein O-GlcNAcylation on neural tube malformation in diabetic embryopathy. Sci.Rep. 7 11107 PMID: 28894244

Kim et al (2014) Versatile O-GlcNAc transferase assay for high-throughput identification of enzyme variants, substrates, and inhibitors. Bioconjug.Chem. 25 1025 PMID: 24866374


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Keywords: ST 045849, ST 045849 supplier, ST045849, O-GlcNAc, O-linked, N-acetylglucosamine, transferase, OGT, inhibitors, inhibits, glycosylation, glycolysis, O-GlcNAcylation, hyperglycemia, Other, Transferases, 6775, Tocris Bioscience

Citations for ST 045849

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