CCX140 (CCX140-B) is a potent CCR2 antagonist.

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity.

2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) acts as a potent fucosyltransferase (FUT) inhibitor.

trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.

Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.

Sangivamycin (NSC 65346), a nucleoside analog, is a potent inhibitor of protein kinase C (PKC) with an Ki of 10 μM. Sangivamycin has potent antiproliferative activity against a variety of human cancers.

R(+)-Methylindazone (R(+)-IAA-94) is a potentand specific indanyloxyacetic inhibitor of the renal epithelial chloride channel and exacerbates myocardial infarction by impairing mitochondrial calcium retention capacity (CRC), leading to mitochondrial permeability transition pore (mPTP) opening and increased cell death during ischemia-reperfusion injury.

Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.

TLR1 (compound 4a) is a low molecular weight, cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic. TLR1 inhibits IL-1 receptor-mediated responses.