Description
OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
Product information
CAS Number: 2260542-60-5
Molecular Weight: 555.62
Formula: C26H25N3O7S2
Chemical Name: methyl 2-[(2R)-2-(2-methoxyphenyl)-2-(2-oxo-1,2-dihydroquinoline-6-sulfonamido)-N-[(thiophen-2-yl)methyl]acetamido]acetate
Smiles: COC1=CC=CC=C1[C@@H](NS(=O)(=O)C1=CC2C=CC(=O)NC=2C=C1)C(=O)N(CC(=O)OC)CC1=CC=CS1
InChiKey: ACLDUOSWRUIOSB-RUZDIDTESA-N
InChi: InChI=1S/C26H25N3O7S2/c1-35-22-8-4-3-7-20(22)25(26(32)29(16-24(31)36-2)15-18-6-5-13-37-18)28-38(33,34)19-10-11-21-17(14-19)9-12-23(30)27-21/h3-14,25,28H,15-16H2,1-2H3,(H,27,30)/t25-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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-2 (Compound 1b; 20-50 μM; 4-24 hours; HCT116 cells) treatment reduces O-GlcNAc levels at short treatment times (<8h). However, O-GlcNAc levels begins to recover at longer treatment times with OSMI-2.A decrease in HCF-1 cleavage products and the appearance of uncleaved HCF-1 in cells treated with OSMI-2 (Compound 1b) is observed. Because OGT knockdown is known to decrease cell proliferation, the effects of OSMI-2 on cell growth in culture over 96h is also monitored. Although there is no evidence of apoptosis, the reduced growth of cells over time is observed, consistent with the knockdown results. A time course performed with 20 μM OSMI-2 (Compound 1b) shows reciprocal changes in the abundance of OGT and OGA, with a particularly large increase in OGT; this may explain the recovery in O-GlcNAc levels with OSMI-2. At 24h where O-GlcNAc levels fully recovered.
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