interaction

12-oxo-N-[1-(propan-2-yl)piperidin-4-yl]-6H,7H,8H,9H,10H,12H-azepino[2,1-b]quinazoline-3-carboxamide available as a molecular structural unit, it is used in the synthesis of various compounds.

B7/CD28 interaction inhibitor 1 (CTLA-4 inhibitor) is a potent CTLA-4 inhibitor.

Beclin1-ATG14L Interaction Inhibitor 1 (COM 19) is a selective inhibitor targeting the specific interaction between Beclin1 and ATG14L. It impedes the formation of complex I in the lipid kinase VPS34, thus inhibiting autophagy, while leaving complex II intact, which relies on the Beclin 1-UVRAG interaction for its integrity and is essential for vesicle transport [1].

Antitumor Agent-108 (Compound 5), an inhibitor of the Hyaluronic Acid (HA)-CD44 interaction, effectively disrupts cancer spheroid integrity and exhibits antiproliferative activity against cancer cells [1].

SORT-PGRN Interaction Inhibitor 2 is a compound that downregulates SORT1 protein expression and enhances extracellular progranulin (PGRN) secretion in various mammalian cell lines, and is utilized in the study of neurological diseases [1].

Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].

Antitumor agent-109 (compound 6) is a dual-function inhibitor that targets hyaluronic acid and CD44, which are involved in tumor progression and invasion. It demonstrates potent antitumor activity, specifically inhibiting MDA-MB-231 cells with an EC50 of 0.59 µM [1].

NusB-NusE interaction inhibitor-1 is a modulator of the NusB-NusE interaction.

p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.

SORT-PGRN interaction inhibitor 1 is a potent sortilin-progranulin interaction inhibitor(IC50 of 2 μM).

SORT-PGRN Interaction Inhibitor 3 (Compound 13), with an IC50 value of 0.17 μM, acts as an inhibitor of the SORT-PGRN interaction, and is utilized in the study of neurodegenerative diseases [1].

VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.

Alrizomadlin (APG-115) is an orally active inhibitor of MDM2 with IC50 of 3.8 nM and Ki of 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM.

Atezolizumab (anti-PD-L1) is a fully humanized IgG1 monoclonal antibody that blocks the interaction of PD-L1 with both PD-1 and B7.1 but not the interaction of PD-L2 with PD-1.

Rhosin hydrochloride is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin hydrochloride does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin h

Y16 is a G-protein–coupled Rho GEFs inhibitor; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.

Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

4EGI-1, a competitive eIF4E/eIF4 g interaction inhibitor, binds to eIF4E(KD=25 μM).

Triheptanoin (IND 106011) is a fatty acid metabolic modulator. It potentially for the treatment of fatty acid oxidation disorders and GLUT1.

1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effects, seems to be dependent on its interaction with the dopaminergic system, but not with the serotonergic and noradrenergic systems.

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

NSC 122393 is a fluorescent dye that inhibits the interaction between Bax and Bcl-X and induces apoptosis in Bcl-X overexpressing breast cancer cells.

YAP-TEAD-IN-1 acetate is an effective and competitive inhibitor of YAP–TEAD interaction with an IC50 of 25 nM.

NAcM-OPT HCL is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor that targets N-Acetyl-UBE2M (E2 conjugating enzyme, UBC12) interaction with DCN1 with IC50 of 79 nM.

PP7 is a potent inhibitor of PB1-PB2 interaction(IC50 of 8.6 μM).

pep2m aceate is a Peptide inhibitor of the interaction between the C-terminus of the GluR2 subunit and N-ethylmaleimide-sensitive fusion protein

Pep2-EVKI acetate is a cell-permeable peptide. Pep2-EVKI acetate interferes the interaction between protein interacting with C-kinase (PICK1) and GluR2 AMPA receptor subunits.

BMS202 hydrochloride (1675203-84-5(free base)) (PD-1/PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1/PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1/ PD1 interaction.

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

P11 acetate is an integrin αvβ3-vitronectin interaction antagonist(IC50 = 2.74 nM).

MoTPS1-IN-1 is a potent MoTPS1 inhibitor with antifungal and potentially anti-inflammatory activity that acts through interaction with Glu396 and can be used to study ulcerative colitis.

Guanosine 5'-diphosphate (GDP) as Potential Iron Mobilizer, Preventing the Hepcidin-Ferroportin Interaction and Modulating the Interleukin-6/Stat-3 Pathway.

ZINC12409120 (R-4584) is a selective ERK inhibitor.ZINC12409120 inhibits ERK with an IC50 of 5.0 μM.ZINC12409120 inhibits ERK activity by interfering with FGF23:α-Klotho interaction.

5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione (5-bromo-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) is a synthetic compound. It has been used as a catalyst and as a tool in enzyme kinetic studies; it has also been used in studies of enzyme inhibition, as well as in drug receptor interaction studies.

(R)-STU104 is a novel TAK1-MKK3 protein-protein interaction (PPI) inhibitor that inhibits TNF-α and suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signalling pathway by binding to MKK3 and disrupting TAK1 phosphorylation of MKK3. (R)-STU104 is a candidate compound for the treatment of ulcerative colitis.

Jamaicin (AnCoA4), an isoflavone derived from the chickweed plant, is an inhibitor of the STIM1-Orai1 channel that blocks calcium influx, reduces its interaction with STIM1, and inhibits T-cell activation.

PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor(IC50 of 92.3 nM).

Tat-NR2B9c acetate (NA-1 acetate) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c acetate disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c acetate also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.

Disitertide acetate (P144 acetate) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide acetate is also a PI3K inhibitor and an apoptosis inducer.

FM04 is an orally active and highly potent inhibitor of P-glycoprotein (P-gp) with an EC50 value of 83 nM. FM04 can interact with Q1193 and I1115 in human P-gp nucleotide binding domain 2 (NBD2). Thereby disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling the ICL2-NBD2 interaction, thereby inhibiting P-gp. FM04 can be used in the treatment of cancer and tumors.

Trifluoromethyl-tubercidin (TFMT) inhibits host MTr1 and suppresses virus replication. TFMT inhibits MTr1 through interaction at its S-adenosyl-l-methionine binding pocket to restrict influenza virus replication. TFMT was effective in inhibiting viral replication in mice, displayed little toxicity.

WDR5-47 is a potent small molecule to disturb the interaction of MLL1-WDR5 with IC50 value of 0.3μM.

IMM-01 is a novel class of small-molecule agonists of the mammalian Diaphanous (mDia)-related formins, which act downstream of Rho GTPases to assemble actin filaments, and their organization with microfilaments to establish and maintain cell polarity during migration and asymmetric division. GTP-bound Rho activates mDia family members by disrupting the interaction between the DID and DAD autoregulatory domains, which releases the FH2 domain to modulate actin and microtubule dynamics[1].

Pep2m, myristoylated acetate is a Cell-permeable, myristoylated form of pep2m. Peptide inhibitor of the interaction between the C-terminus of the GluA2 (AMPA receptor) subunit and N-ethylmaleimide-sensitive fusion protein (NSF), a protein that regulates A

Compound 1T-0219 (SC) is a blocker of AKT1-FAK interaction reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation.

Corrector C4, a corrector commonly used to study cystic fibrosis mutants, works by alleviating the interaction between CFTR transmembrane domain mutants and protein homeostasis.

Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensure the efficacy of cyclosporin, we suggest that the coadministration of Phellamurin or Phellode