stasis

Toddalolactone ((+)-Toddalolactone) is an anti-inflammatory and analgesic.

ER proteostasis regulator-1 is an effective modulator of ER proteostasis. It balances the UPR pathway to reduce misfolded protein accumulation, protecting cells from proteotoxicity in neurodegenerative disease research.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

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.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

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.

AZ084 is a potent, selective, allosteric, and orally active CCR8 antagonist (Ki: 0.9 nM) with potential to treat asthma.

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

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

Flunisolide (Rhinalar) is a synthetic corticosteroid with anti-inflammatory and antiallergic properties.

NSC 405020 is a noncatalytic inhibitor of MT1-MMP.

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).

Oxysophocarpine is an alkaloid extracted from seaweed. It has neuroprotective and antinociceptive effects on the central and peripheral nervous systems.

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