OU749 is a competitive inhibitor of γ-glutamyl transpeptidase (GGT) . Expression of γ-glutamyl transpeptidase (GGT) in tumors contributes to the resistance to radiation and chemotherapy. GGT is inhibited by glutamine analogues which compete with the substrate for the γ-glutamyl binding site . OU749 inhibited human kidney GGT with an intrinsic Ki of 17.6 M . In 786-O cells, a human renal tumor cell line, OU749 showed more than 150-fold less toxic than the GGT inhibitor acivicin toward dividing cells. OU749 inhibited GGT isolated from human kidney in a dose-dependent manner . OU749 was 7-fold less potent as inhibitor of GGT isolated from rat kidney and 10-fold less potent inhibiting GGT from mouse kidney . OU749 did not inhibit degradation of glutathione by GGT from rat kidney. Inhibition of GGT by OU749 is species-specific . OU749 showed no inhibitory effect on GGT from pig cells. OU749 inhibited human GGT expressed in mouse fibroblasts by a similar extent to the GGT from human cells, indicated that the species specificity was determined by differences in the primary structure of the protein rather than species-specific, post-translational modifications .

Product information

CAS Number: 519170-13-9

Molecular Weight: 361.44

Formula: C16H15N3O3S2

Chemical Name: N-{5-[(4-methoxyphenyl)methyl]-1,3,4-thiadiazol-2-yl}benzenesulfonamide

Smiles: COC1C=CC(CC2=NN=C(NS(=O)(=O)C3C=CC=CC=3)S2)=CC=1

InChiKey: QCXWBMZVLJCKHF-UHFFFAOYSA-N

InChi: InChI=1S/C16H15N3O3S2/c1-22-13-9-7-12(8-10-13)11-15-17-18-16(23-15)19-24(20,21)14-5-3-2-4-6-14/h2-10H,11H2,1H3,(H,18,19)

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

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