OSMI-4

OSMI-4 is an inhibitor of O-GlcNAc transferase (OGT) with EC50 of 3 μM in cells.

Product information

CAS Number: 2260791-14-6

Molecular Weight: 604.09

Formula: C27H26ClN3O7S2

Chemical Name: ethyl 2-[[(2S)-2-[(7-chloro-2-oxo-1H-quinolin-6-yl)sulfonylamino]-2-(2-methoxyphenyl)acetyl]-(thiophen-2-ylmethyl)amino]acetate

Smiles: COC1=CC=CC=C1C(NS(=O)(=O)C1=CC2C=CC(=O)NC=2C=C1Cl)C(=O)N(CC(=O)OCC)CC1=CC=CS1

InChiKey: STPSLAZMEWZDAJ-UHFFFAOYSA-N

InChi: InChI=1S/C27H26ClN3O7S2/c1-3-38-25(33)16-31(15-18-7-6-12-39-18)27(34)26(19-8-4-5-9-22(19)37-2)30-40(35,36)23-13-17-10-11-24(32)29-21(17)14-20(23)28/h4-14,26,30H,3,15-16H2,1-2H3,(H,29,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 100 mg/mL (165.54 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

OSMI-4 reduces O-GlcNAc levels almost completely by 5 μM. A decrease in HCF-1 cleavage products and the appearance of uncleaved HCF-1 is observed in cells treated with OSMI-4. OSMI-4 is a kind of structure-based evolution of small molecule OGT inhibitors with low nanomolar binding affinities. OSMI-4 exhibits a ~3 μM EC50 in cells, making it especially attractive for probing OGT’s complex biology.

References:

1. Sara E S Martin, et al. J Am Chem Soc. 2018 Oct 24;140(42):13

Products are for research use only. Not for human use.