786-o

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

HIF-2α agonist 2 is an HIF-2α agonist with an EC50 value of 1.68 μM for HIF-2α. HIF-2α agonist 2 can promote the stability of the ARNT A B ring in the 3z structure of HIF-2a-ARNT complex without cytotoxicity to 786-o-Reha-Luc cells. HIF-2α agonist 2 can be used in the study of oxygen metabolism and is closely related to the occurrence of cancer.

M1001 is a HIF-2α agonist.

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

Gramicidin A is a peptide antibiotic isolated from B. brevis.Gramicidin A is a highly hydrophobic channel-forming ion carrier that forms monovalent cation-permeable channels in artificial membranes.Gramicidin A induces the degradation of hypoxia-inducible factor 1 alpha (HIF-1 alpha) and reduces the growth of a mouse xenograft model of human renal cell carcinoma. Gramicidin A has antibacterial, antimalarial and hemolytic activities.

Compound 6h (Anticancer Agent 139) exhibits potent anticancer activity, engaging in a π-cationic interaction with Lys352 of Tubulin and demonstrating high efficacy against SNB-19, OVCAR-8, and NCI-H460 with PGIs of 86.61, 85.26, and 75.99, respectively. Moreover, it shows moderate activity against a range of other cancer cell lines — HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 — with PGIs between 51.88 and 67.55 [1].

DIM-C-pPhOH (CDIM8) is a nur77 (NR4A1) antagonist,inhibits TGF-β induced cell migration of breast cancer cell lines,promotes ROS/endoplasmic reticulum stress and proapoptotic pathways in pancreatic cancer cell lines,mimics effects of Nur77 RNAi silencing.

Fenoldopam mesylate (Corlopam mesylate) is a selective dopamine-1 receptor (DA1) agonist with natriuretic diuretic properties. It lowers blood pressure through arteriolar vasodilation.

C-02, a proteolysis-targeting chimera (PROTAC) that combines the hexokinase inhibitor lonidamine with the cereblon ligand thalidomide, effectively induces the degradation of hexokinase 2 in 786-O and PANC-1 cells at a concentration of 20 µM. This compound exhibits cytotoxicity to a range of cancer cells, including 786-O, 4T1, PANC-1, HGC-27, and MCF-7, with IC50 values of 34.07 µM, 5.08 µM, 31.53 µM, 6.11 µM, and 21.65 µM, respectively. Additionally, at 20 µM, C-02 diminishes both the extracellular acidification rate (ECAR) and oxygen consumption rate (OCR) in 4T1 cells, suggesting a suppression of glycolysis and mitochondrial damage. In vivo studies reveal that at a dosage of 50 mg/kg, C-02 not only reduces tumor volume but also promotes intratumoral cytokine accumulation and triggers pyroptosis in a 4T1 murine mammary carcinoma model.

PERK-IN-5 is a highly selective, potent, orally active inhibitor of protein kinase R-like endoplasmic reticulum (ER) kinase (PERK), displaying inhibition with IC50 values of 2 nM for PERK and 9 nM for p-eIF2α. PERK-IN-5 significantly inhibited tumor growth in the 786-O renal cell carcinoma xenograft tumor model.

UC2288 is a relatively selective p21 attenuator which is synthesized based Sorafenib. UC2288 attenuates p21 protein levels with minimal effect on p21 protein stability.