TZ9, Rad6 Ubiquitin Inhibitor

TZ9 is a selective and cell permeable inhibitor of human E2 ubiquitin-conjugating enzyme Rad6B. It binds to the Rad6B catalytic site, inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin. It can induce G2/M arrest and apoptosis, and inhibit proliferation and migration of metastatic human breast cancer cells (IC50 ~6 µM).

Product information

CAS Number: 1002789-86-7

Molecular Weight: 366.33

Formula: C17H14N6O4

Chemical Name: (4-amino-6-(phenylamino)-1,3,5-triazin-2-yl)methyl 4-nitrobenzoate

Smiles: NC1N=C(COC(=O)C2C=CC(=CC=2)[N+]([O-])=O)N=C(NC2C=CC=CC=2)N=1

InChiKey: RRRDZFQRNJTKHL-UHFFFAOYSA-N

InChi: InChI=1S/C17H14N6O4/c18-16-20-14(21-17(22-16)19-12-4-2-1-3-5-12)10-27-15(24)11-6-8-13(9-7-11)23(25)26/h1-9H,10H2,(H3,18,19,20,21,22)

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 50 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: ≥360 days if stored properly.

Stock Solution Storage: Powder: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 1 year.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

TZ9 was used at 10-50 µM final concentration in vitro and in cellular assays.

References:

1. Sanders MA, et al. Novel inhibitors of Rad6 ubiquitin conjugating enzyme: design, synthesis, identification, and functional characterization. (2013) Mol Cancer Ther. 12(4):373-83.

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