786-o

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

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.

BAY-876 is an orally active, selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM), exhibiting over 130-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4. It also inhibits glycolytic metabolism and ovarian cancer growth.

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.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

Colchicine (Colcin) is a natural product that is an inhibitor of microtubule polymerization (IC50=3 nM) and blocks microtubule polymerization by binding to microtubule proteins. Colchicine can be used in the treatment of ventilation and rheumatic diseases.

Ferroptosis-IN-15 (compound 12) serves as an effective inhibitor of ferroptosis, exhibiting EC50 values of 0.76 μM and 0.67 μM in A375 cells and 786-O cells, respectively. It acts as a potential iron chelator and radical-scavenging antioxidant.

Anilopam HCl is a benzomorphan class compound that functions as an opioid analgesic. It acts as an agonist at opioid receptors.

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.

(S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9 μM.

Ceforanide lysine is an Anti-Infective.

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.

IR-Crizotinib is a conjugate of the near-infrared dye IR-786 and Crizotinib, an NF-κB-inducing kinase (NIK) inhibitor, with an IC50 of 3.381 μM for intracranial glioblastoma (GBM) localization in mice. It has the ability to cross the blood-brain barrier and fluorescently mark GBM, and demonstrates efficacy in inhibiting glioma proliferation and invasion both in vitro and in vivo, making it significant in cancer research [1].

3,5-Dimethoxy-2,7-phenanthrenediol (compound 2), extracted from Combretum laxum roots, exhibits cytotoxicity against various human cancer cell lines, including 786-0, MCF-7, and NCI ADR-RES, with IC50 values of 73.26 μM, 118.40 μM, and 83.99 μM, respectively. Additionally, this phenanthrene compound demonstrates free radical scavenging activity, presenting an IC50 of 20.4 μM [1].

Tilvestamab (BGB149) is a humanized antibody targeting AXL with anti-tumor and anti-fibrotic activity, inhibiting Gas6-stimulated AXL activation and tumor progression in 786-0 RCC cells, used in cancer research.

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.

PC786 is a potent and selective non-nucleoside RSV L-protein polymerase inhibitor for inhalation therapy of RSV infections, with antiviral activity against RSV-A (IC50=0.09-0.71 nM) and RSV-B (IC 50=1.3-50.6 nM), and the ability to inhibit RSV RNA-dependent RNA polymerase in HEp-2 cells ( RdRp).

CK2-IN-14 (Compound 10b) is an inhibitor of cyclin-dependent kinase 2α with an IC50 of 36.7 nM. It effectively hinders the growth of cancer cell lines 786-O and U937, with GI50 values of 7.3 μM and 7.5 μM, respectively.

Emb-06 is a tetravalent CD3 × BCMA bispecific antibody in the form of Fabs-In-Tandem-Ig, which possesses four active antigen-binding sites. It targets BCMA on tumor cells and CD3 on T cells, enhancing immune activation and antitumor efficacy. The molecular weight is 241.36 KD.

NYY-6a is a ferroptosis (Ferroptosis) inhibitor, demonstrating significant suppression of RSL3-induced ferroptosis in 786-O and HT-1080 cells, with EC50 values of 52 nM and 50 nM, respectively. As a radical-trapping antioxidant (RTA), NYY-6a effectively reduces lipid peroxidation, comparable to ferrostatin-1 and liproxstatin-1, making it useful for research into ferroptosis-related pathologies.

hCAXII-IN-7 (compound 6e) functions as an inhibitor of human carbonic anhydrase XII (hCA XII), possesses blood-brain barrier (BBB) permeability, and promotes apoptosis in 786-0, SF-539, and HS 578 T cell lines [1].