metastasis

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

MMP-9-IN-1 is an inhibitor of specific matrix metalloproteinase-9 (MMP-9).

NP-G2-044 is an orally active fascin inhibitor, with an IC50 of ~2 μM. It blocks tumor metastasis and increases antitumor immune response.

Phenytoin sodium (Diphantoine) is an inactive stabilizer for voltage-gated sodium channel .

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

KGP94 is an inhibitor of cysteine protease Cathepsin L(CTSL).

MSX-127 elicites positive response in peptide CXCR4.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

PTUPB is a potent dual inhibitor of sEH and COX-2 enzymes with IC50 values of 0.9 nM and 1.26 μM, respectively.

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

Galloflavin is a lactate dehydrogenase inhibitor that inhibits the activity of lactate dehydrogenase. Galloflavin inhibits both human LDH isoforms (type A and type B) by preferentially binding to the free enzyme without competing with substrates or cofactors, with Ki values ​​calculated by pyruvate of 5.46 μM (LDH-A) and 15.06 μM (LDH-B).

Xanthone (Xanthenone) is currently used as ovicide for codling moth eggs and as a larvicide.

CAIX Inhibitor S4 (S4) is an effective inhibitor of carbonic anhydrase IX/XII with a Ki of 7 nM and 2 nM, respectively. The Kis for CA II and CA I are 546 and 5600 nM.

Isoliquiritin apioside, isolated from Glycyrrhizae radix rhizome, significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis o

Irigenin mediates its antimetastatic effect by specifically and selectively blocking the α9β1 and α4β1 integrin binding sites on the C-C loop of the Extra Domain A domain. It can sensitize TRAIL-induced apoptosis by enhancing the expression of pro-apoptotic molecules in gastric cancer cells and has anti-cancer effects.

MSX-130 is CXCR4 Antagonist.

KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.

1. Obtusifolin has antioxidant properties and improves chemically induced diabetes and its complications by modulation of oxidative stress. 2. Obtusifolin suppresses phthalate esters-mediated bone resorption, thus may be a novel anti-breast-cancer bone me

PF-5274857 (PF-5274857 free base) is an effective and selective hedgehog signaling pathway inhibitor (IC50: 5.8 nM and a Ki: 4.6 nM). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo.

CCG-222740 is an inhibitor of Rho/MRTF pathway

WSB1 Degrader 1 is a potent, orally active degrader of WD repeat and SOCS box-containing 1, exhibiting anti-cancer metastatic effects.

MPT0B390 is an inhibitor of HDAC and a TIMP3 inducer inhibiting tumor growth, metastasis, and angiogenesis.

Murrayone, a coumarin-containing compound derived from M. paniculata, stands out as the most bioactive substance within this species, primarily due to its unique pharmacological attributes that notably suppress cancer metastasis, positioning it as an effective chemopreventive agent.