T2399

Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.

(Rac)-PT2399 is a potent and specific inhibitor of hypoxia-inducible factor 2a (HIF-2α)(IC50 of 0.01 μM).

PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2α antagonist, which directly binds to the HIF-2α PAS B domain (IC50: 6 nM).

Diazobenzenesulfonic acid (a component of Pauly's reagent) is a classical chemical modification probe for proteins. It specifically labels surface-exposed histidine and tyrosine residues via diazotization, widely utilized for probing protein tertiary structure accessibility and analyzing enzyme active site conformations.

Dibenzo(a, i)pyrene is a polycyclic aromatic hydrocarbon with potent carcinogenic activity.

Diftalone is an anti-Inflammatory agent.

Bortezomib-D8 is the deuterated form of Bortezomib. Bortezomib (T2399) (PS-341) is a reversible and selective proteasome inhibitor that effectively targets threonine residues, inhibiting the 20S proteasome (Ki=0.6 nM). It disrupts the cell cycle, induces apoptosis, and inhibits the nuclear factor NF-κB. Bortezomib (T2399) is noted as the first proteasome inhibitor with anticancer activity.