Ubiquitination/ Proteasome

Inhibitor of Src/Syk tyrosine kinases

Chloroquine diphosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis.

DUBs-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor extracted from reference compound 22c with an IC50 of 0.56 μM for USP8.

P97 ATPase inhibitor

WP1130 (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. WP1130 has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.

NSC697923 is a potent, cell-permeable UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor.

proteasome inhibitor

Xanthohumol is the main prenylflavonoid in hops that inhibits diacylglycerol acyltransferase (DGAT) with IC 50 value of 50.3μM.

HBX 41108 is a potent inhibitor of USP7 with IC 50 value of 424nM . HBX 41108 is shown to affect USP7-mediated p53 deubiquitinating in vitro and in cells.

Dopamine D2 receptor inhibitor

Omeprazole is an inhibitor of gastric H + /K + ATPase (PPI) with an IC 50 value of 1.1μM for porcine ATPase. Omeprazole has competitive inhibitory effects on CYP2C19 activity with an inhibition constant (Ki) of 2 to 6μM.

SJB3-019A is a novel and potent USP1 inhibitor, exhibiting an IC₅₀ value of 0.0781μM in K562 cells.

Inhibitor of USP1/USF1 complex

Sulfonamide antibiotic

(±)-Bay K 8644 is a dihydropyridine compound that acts as a specific agonist of L-type calcium channels, with an EC₅₀ value of 17.3nM.

Valproic acid (VPA) sodium (2:1) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.

NMPRTase inhibitor

PYR-41 is an irreversible, cell-permeable inhibitor of ubiquitin-activating enzyme E1, with an IC 50 value less than 10μM and minimal effects on E2 and E3.

Chymotrypsin-like (CT-L) inhibitor

TAK-242 is a toll-like receptor 4 (TLR4) signaling inhibitor that inhibits NO, TNF-α and IL-6 production with IC 50 values of 1.8nM, 1.9nM and 1.3nM, respectively.

Nimodipine is a 1,4-dihydropyridine L-type calcium channel antagonist, mainly used to treat aneurysmal subarachnoid hemorrhage (aSAH) and prevent cerebral vasospasm.

DUBs-IN-2 is a highly selective and membrane-permeable inhibitor for USP8 with IC 50 value of 0.28μM.

VCP/p97 inhibitor,selective and allosteric

Concanamycin A, a macrolide antibiotic, is a specific inhibitor of vacuolar-type ATPase (V-ATPase) with an IC 50 value of 10nM.