VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation, potentiated the effect of radiation in tumor spheroids in a synergistic manner. VLX600 is preferentially active against quiescent cells in colon cancer 3-D microtissues. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation and displays tumour growth inhibition in vivo.
RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS) that targets deubiquitinating enzymes (DUB) without affecting 20S proteasome catalytic-core activity. Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors。
Col003 is a cell penetrant, selective and potent inhibitor of the interaction of Hsp47 with collagen. Col003 is the cleavage product of AK778.It competitively inhibited the interaction and caused the inhibition of collagen secretion by destabilizing the collagen triple helix.
STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis .
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .