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Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. Quercetin pentaacetate interacts with RSV and inhibit the viral adhesion on cell surface .
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders .
RIP1 kinase inhibitor 7 (compound 41) is a potent receptor interacting protein 1 kinase (RIP1) Inhibitor with an IC50 of <100 nM for human RIP1. RIP1 kinase inhibitor 7 has an EC50 of 1-100 nM in the cell necrosis assay .
ALLO-1, an autophagy receptor, is essential for autophagosome formation around paternal organelles and directly binds to the worm LC3 homologue LGG-1 through its LC3-interacting region (LIR) motif .
YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness .
KHS101 hydrochloride could selectively induce a neuronal differentiation phenotype and interacts with transforming acidic coiled-coil-containing protein 3 (TACC3).
Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction .
(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment .
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
(±)-WB 4101 is a potent antagonist of noradrenaline. (±)-WB 4101 interacts with protein in smooth muscle. (±)-WB 4101 makes drug and receptor bind tightly .
Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Roemerine, an aporphine alkaloid, isolated from the leaves of Fibraurea recisa Pierre, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells .
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity .
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
Gallichrome is an active peptide. Gallichrome can interact directly with the hydroxamate moieties of the siderophore. Gallichrome can be used for the research of the uptake of iron in many gram-positive and gramnegative bacteria .
TAB29 is a potent inhibitor of peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (Pin1) with an IC50 of 874 nM, possesses therapeutic potential for human cancers .
Jingzhaotoxin-XII (JzTx-XII) is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII interacts with the channels by modifying the gating behavior .
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively .
GMBS is a heterobifunctional cross-linker. GMBS can be used in chemical cross-linking of proteins coupled with mass spectrometry (CXMS) to study protein folding and to map the interfaces between interacting proteins .
Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of <1 µΜ (From patent WO2017136727A2, example 42) .
VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity .
Oditrasertib is a receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 value lower than 100 nM. Oditrasertib can be used for the research of diseases involving inflammation or cell death .
TNIK-IN-6 (Compound 9) is an inhibitor of Traf2 and Nck-interacting kinase (TNIK) and , with IC50 of 0.93 μM, that plays important roles in neurological and psychiatric disorders .
Antiviral agent 51 (compound a) is a potent antiviral agent. Antiviral agent 51 is a fucoidan. Antiviral agent 51 interacts with DENV-2 RNA Dependant RNA polymerase (RdRp) .
TINK-IN-1 (Compound 9) is a potent and selective Traf2- and Nck-interacting kinase (TNIK) inhibitor with an IC50 of 8 nM. TINK-IN-1 inhibits colorectal cancer cells viability .
Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas .
NDSB 256-4T is a non-washing sulfabetaine compound. NDSB-256-4T prevents protein aggregation and promotes protein folding by interacting with early folding intermediates .
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .
2-Quinoxalinol (2-hydroxyquinoxaline) is a 2-hydroxylated quinoxaline that possesses photocatalytic activity and interacts with various compounds, such as antioxidant vitamins and aromatic metabolites, including neurotransmitters and the pineal hormone melatonin .
Tezepelumab (anti-TSLP) is human monoclonal antibody (IgG2λ) that binds specifically to TSLP, blocking it from interacting with its heterodimeric receptor. Tezepelumab can be used for the research of severe, uncontrolled asthma .
GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer .
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
BYK 191023 is a highly selective inducible nitric-oxide synthase (iNOS) inhibitor. BYK 191023 interacts with the catalytic center of the enzyme. BYK 191023 can be used to study the in vivo and in vitro effects mediated by iNOS .
EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC50 of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation .
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting
protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome .
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
GSK2983559 is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 blocks many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples .
Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact .
IHC3 is a competitive and reversible MAO-B inhibitor (IC50: 1.672 μM). IHC3 can interact with the amino acid Cys172 of MAO-B. IHC3 can be used for neurological diseases research .
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
cRIPGBM, a proapoptotic derivative of RIPGBM, a cell type-selective inducer of apoptosis in GBM cancer stem cells (CSCs) by binding to receptor-interacting protein kinase 2 (RIPK2), with an EC50 of 68 nM in GBM-1 cells .
Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure .
Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects .
Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects .
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors[1][2].
(Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer .
(Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder .
Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257) .
Dodecyltrimethylammonium-d25 (bromide) is the deuterium labeled Dodecyltrimethylammonium (bromide)[1]. Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction[2].
Dodecyltrimethylammonium-d34 (bromide) is the deuterium labeled Dodecyltrimethylammonium (bromide)[1]. Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction[2].
KAT modulator-1 (Compound 3) is a KAT modulator. KAT modulator-1 can interact with p300 full-length but not with the catalytic domain. KAT modulator-1 can be used for epigenetics research .
Fasciculin-I is isolated from the mambas venom. Fasciculin-I exerts its toxic effects by inhibiting acetylcholinesterase (AChE). Fasciculin-I blocks α-neurotoxins of nicotinic acetylcholine receptors and cardiac toxins that interact with cell membranes .
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of agents by first binding to αv-integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM .
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide) .
[Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. [Hyp3]-Bradykinin interacts with B2-bradykinin receptors and stimulates inositol phosphate production in cultured human fibroblasts .
1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodium salt is a lipid molecule having one negative charge, which can interact with the positive charges of peptides .
Opipramol (Ensidon) is an atypical tricyclic antidepressant (TCA). Opipramol acts primarily as a sigma (σ) receptor agonist and can potently interact with sigma recognition sites with a Ki value of 50 nM. Opipramol can be used for the research of generalized anxiety disorder (GAD) .
Jasmonic acid ((-)-Jasmonic acid) is a plant growth regulator and a derivative of α-Linolenic acid (HY-N0728). Jasmonic acid signaling can also induce the MAP kinase cascade pathway, calcium channel, and many processes that interact with signaling molecules .
P-gp inhibitor 17 (compound 2g) is a P-gp inhibitor directly interacted with the transmembrane domain of P-gp. P-gp inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study .
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .
GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. FPA-124 interacts with both the pleckstrin homology (PH) and the kinase domains of Akt. FPA-124 induces apoptosis .
MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC50 of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1 .
HBV-IN-21 (Compound II-8b) is an HBV DNA replication inhibitor with an IC50 of 2.2 µM. HBV-IN-21 can interact HBV 4 capsid protein with good affinity (KD = 60.0 μM) .
Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor of ENL YEATS domain with an IC50 value of 14.5 nM. Eleven-Nineteen-Leukemia Protein IN-1 interacts with ENL protein and enhances the thermal stability of ENL protein in vitro .
Myoregulin (MLN peptide) is a member of the regulin family. Myoregulin regulates muscle performance by modulating intracellular calcium handling. Myoregulin interactes directly with sarcoplasmic reticulum Ca 2+-ATPase (SERCA) and impedinf Ca 2+ uptake into the sarcoplasmic reticulum .
GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples .
JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide) .
STC314 is a small polyanion that interact electrostatically with histones. STC314 blocks disruption of lipid-bilayers by histones that inhibits the cytotoxic, platelet-activating and erythrocyte-damaging effects of histones. STC314 has anti-infective effects and can be uesd for sepsis research .
Acridone-4-carboxylic acid (ACA) (Compound 2c) is a heme-interacting acridone derivatives that prevents free heme-mediated protein oxidation and degradation. Acridone-4-carboxylic acid inhibits protein carbonyl formation with an IC50 of 43 μM .
SL antagonist 1 (Compound D12) is strigolactones antagonists and can strongly interact with SL receptor proteins.SL antagonist 1 can combat root-parasitic weed infestations. SL antagonist 1 has no side effects on the germination or seedling growth .
LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .
Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth .
SRI-37330 hydrochloride is an orally bioavailable thioredoxin-interacting protein (TXNIP) inhibitor. SRI-37330 hydrochloride inhibits glucagon secretion and function, reduces hepatic glucose production and reverses hepatic steatosis. SRI-37330 hydrochloride can be used for type 2 diabetes research .
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model .
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .
Elinafide is an anticancer agent with a naphthalimide structure that targets DNA. Elinafide interferes with cell metabolism by inserting a planar ring into the DNA double helix and interacting with enzymes through its side chain. The IC50 value of Elinafide for HT-29 cells is 0.014 μM .
AIE-GA is a Golgi apparatus (GA) fluorescent probe (green channel: λex = 405 nm, λem = 500-700 nm). AIE-GA has a favourable binding ability to interact with COX-2. AIE-GA binds to the cyclooxygenase catalytic site of COX-2 .
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
Neuropeptide FF (NPFF), an octapeptide belonging to the RF-amide family of peptides, interacts with two distinct G-protein-coupled receptors, NPFF(1) and NPFF(2) and has wide variety of physiological functions in the brain including central cardiovascular and neuroendocrine regulation .
ZL-Pin01 is a high potent covalent Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) inhibitor. ZL-Pin01 shows potent disruption of the Pin1-substrate interaction with an IC50 of 1.33 μM .
H1PVAT is a potent and selective inhibitor of poliovirus serotypes (PV-1, PV-2, PV-3), and inhibits early stage of the replication. H1PVAT interacts with viral capsid directly and protects PV against heat inactivation .
RI-962 is a potent and selective receptor-interacting protein kinase 1 (RIPK1) inhibitor. RI-962 inhibits RIPK1 with an IC50 value of 35.0 nM. RI-962 can be used for the research of nervous system diseases and inflammatory diseases .
Ganglioside GM3 is a precursor of a-, b-, and c-series gangliosides, interacts with transmembrane receptors such as the epidermal growth factor and insulin receptors, and regulates receptor functions by creating a specialized lipid environment. Ganglioside GM3 is synthesized by GM3 synthase and can be used for the research of hypercholesterolemia .
TMV-IN-4 (compound 3) is a tobacco mosaic virus (TMV) inhibitor that effectively induces resistance and enhances plant tolerance to TMV infection by interacting with TMV helicase. TMV-IN-4 enhances peroxidase and superoxide dismutase activity, thereby increasing resistance to TMV in tobacco .
Crotamine is a Na + channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom .
Myoregulin (MLN peptide) TFA is a member of the regulin family. Myoregulin TFA regulates muscle performance by modulating intracellular calcium handling. Myoregulin TFA interactes directly with sarcoplasmic reticulum Ca 2+-ATPase (SERCA) and impedinf Ca 2+ uptake into the sarcoplasmic reticulum .
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent .
MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
Colcemid (Demecolcine) is a potent mitotic inhibitor with an IC50 value of 2.4 μM for inhibition of tubulin polymerization. Colcemid (Demecolcine) can interact with tubulin dimers to induce anti-mitotic action and inhibit microtubule growth. Colcemid (Demecolcine) can be used for inflammatory disorders and cancer research .
GSK854 is a potent Inhibitor of Troponin I-Interacting Kinase (TNNI3K). GSK854 is a suitable lead for identifying new cardiac medicines and have been employed as in vivo tools in investigational studies aimed at defining the role of TNNI3K within heart failure .
Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
T4 UvsY Protein is an accessory protein for in vitro catalysis of strand exchange. T4 UvsY Protein enhances strand exchange by UvsX protein by interacting specifically with UvsX protein. UvsY protein enhances the rate of single-stranded-DNA-dependent ATP hydrolysis by UvsX protein .
Tubulin polymerization-IN-56 (compound 8l), an indazole derivative, is a potent tubulin polymerization inhibitor through interacting with the colchicine site, resulting in cell cycle arrest and cellular apoptosis. polymerization-IN-56 reduces cell migration and leads to more potent inhibition of tumor growth in vivo .
(±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats .
Anti-melanoma agent 3 (compound 5cb) is a 2-aryl-4-benzoyl-imidazole (ABI) derivative and an inhibitor of melanoma xenogeneic tumors. Anti-melanoma agent 3 exerts anticancer activity by interacting with the colchicine binding site to inhibit tubulin polymerization .
JI051 is a stabilizer for the Hes1-PHB2 interaction. JI051 interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity .
TXNIP-IN-1 is TXNIP-TRX (thioredoxin-interacting protein- thioredoxin) complex inhibitor extracted from patent US20200085800A1, Compound 1. TXNIP-IN-1 can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease .
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells .
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
YG1702 is a potent ALDH18A1-specific inhibitor. YG1702 attenuates the growth of MYCN-amplified NB and down-regulates MYCN. YG1702 physically interacts with ALDH18A1 with a high affinity and might potentially affect its enzymatic activity .
Dermatan sulphate sodium is a glycosaminoglycan and thrombin inactivator with antithrombotic activity. Dermatan sulphate sodium selectively catalyzes the inactivation of thrombin by heparin cofactor II and does not interact with antithrombin III. Dermatan sulphate sodium is highly bioavailable and also reduces Bleomycin (HY-108345)-induced pulmonary fibrosis damage .
Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis .
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate . Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor .
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase .
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function .
Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1 .
NSC 405020 is a specific MMP14 inhibitor. NSC 405020 can directly interact with the hemopexin domain of MMP14. NSC 405020 reduces the expression of full length and active cleaved Notch3 (NICD3). NSC 405020 can be used to research vestibular schwannoma, hemostasis and thrombosis .
Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM .
BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons .
Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer .
CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer .
ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells .
Cinnabarinic acid (Standard) is the analytical standard of Cinnabarinic acid. This product is intended for research and analytical applications. Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis .
Transdermal Peptide Disulfide (TD 1 Disulfide(peptide)) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide can enhance the transdermal delivery of many macromolecules .
GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. GSK-843 can be used for the research of inflammation .
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models .
IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease . HBx: hepatitis B virus X protein.
TH1217 (ZINC1775962367) is a potent and selective dCTPase pyrophosphatase 1 (dCTPase) inhibitor, with an IC50 of 47 nM. TH1217 enhances the cytotoxic effect of cytidine analogues in leukemia cells. TH1217 also could modulate SARS-Cov-2 interactors, so it shows activity of against COVID-19 .
L-Tartaric acid (L-(+)-Tartaric acid) sodium hydrate is the enantiomer of D-tartaric acid. L-Tartaric acid (HY-Y0293) is a white crystalline dicarboxylic acid found in many plants, such as grapes, and is one of the main organic acids in wine. L-Tartaric acid sodium hydrate which acts as a flour bulking agent and as a food additive can interact with sodium bicarbonate to produce carbon dioxide .
PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism .
Trimethyloctylammonium bromide (TOAB) is used as a surfactant and phase transfer catalyst in various chemical reactions. TOAB can be used in the synthesis of nanomaterials due to its ability to selectively transfer ions across interfaces and as a surfactant in the production of emulsions and foams. It is valued for its amphiphilic properties, which allow it to interact with water and oils, stabilizing and dispersing mixtures.
μ-TRTX-Hd1a, a spider venom, is a selective NaV 1.7 inhibitor. μ-TRTX-Hd1a is a gating modifier that inhibits human NaV 1.7 by interacting with the S3b-S4 paddle motif in channel domain II .
13-HPOT, a linolenic fatty acid hydroperoxide, is an antibacterial agent. 13-HPOT has a strong dose response effect on three plant pathogen gram negative bacteria: Pectobacterium carotovorum, Pseudomonas syringae and Xanthomonas translucens. 13-HPOT can interact with the lipid representative of the inner bacterial plasma membrane .
Pomalidomide 4'-alkylC8-acid is an E3 ubiquitin ligase ligand-Linker conjugate containing Pomalidomide (HY-10984). Pomalidomide is a third-generation immunomodulator that acts like a molecular glue. Pomalidomide interacts with the E3 ligase cereblon to induce degradation of the essential Ikaros transcription factor .
PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis .
Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules .
GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC) .
Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 main protease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298 .
Phospholipid-PEG-Biotin (MW 1000) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
Phospholipid-PEG-Biotin (MW 3400) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
Phospholipid-PEG-Biotin (MW 10000) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
Phospholipid-PEG-Biotin (MW 20000) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
1-Methylisatin is a potent and selective CE (carboxylesterases) inhibitor, with Kis of 38.2 and 5.38 μM for hiCE and hCE1, respectively. 1-Methylisatin interacts with Hb (human adult hemoglobin) by hydrophobic binding and electrostatic attraction. 1-Methylisatin can be used in the study of regulation of agent metabolism in vivo .
SU056 is a YB-1 inhibitor. SU056 induces cell-cycle arrest, apoptosis, and inhibits cell migration in ovarian cancer cells. SU056 interacts with YB-1 and inhibits and its associated downstream proteins and pathways. SU056 can enhance the cytotoxic effects of Paclitaxel (HY-B0015) .
Exatecan Intermediate 4 dihydrochloride is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
RIPK1-IN-13 (compound 28) is a selective inhibitor for receptor-interacting serine/threonine-protein kinase 1 (RIPK1), the inhibitory activity is measured by ADP-Glo Kinase Assay with a pKi of 7.66. RIPK1-IN-13 inhibits human leukaemia cells U937 with a pIC50 of 7.2 .
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM .
PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM .
SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes .
Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia . Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion .
Anti-MERS-D12 mAb (MERS-D12; MERS Antibody-D12) is a human monoclonal IgG1. Anti-MERS-D12 mAb binds directly to the DPP4 interacting region of the MERS-CoV Spike receptor binding domain (RBD) and effect neutralization by directly blocking receptor binding .
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders .
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans) .
VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer .
CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools .
Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity .
ALPK1-IN-1 (Compound A001) is a potent inhibitor of alpha-kinase 1 (ALPK1). ALPK1 is an intracytoplasmic serine threonine protein kinase that plays an important role in activating the innate immune response to bacteria via TRAF-interacting protein with forkhead-associated domain (TIFA) dependent proinflammatory NF-κB signaling .
Cyclic GMP sodium (cGMP) is an important regulator of short-term changes in smooth muscle tone and longer-term responses to chronic drug research or proliferative signals, it is in response to atrial natriuretic peptide (ANP) or nitric oxide (NO). Cyclic GMP sodium interacts with cation channels to regulate ion transport or activate the cyclic GMP-dependent protein kinase to result in protein phosphorylation .
Dithiodipropionic acid can interact with CPUL1 (HY-151802, a TrxR inhibitor) to form nanoaggregates (CPUL1-DA NAs). CPUL1-DA NAs generates more abundant ROS to induce cell apoptosis than that of free CPUL1, and improves antitumor efficacy against HUH7 cancer cells .
Exatecan Intermediate 2 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
Exatecan Intermediate 2 hydrochloride (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
Exatecan Intermediate 4 (compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1) inhibitor with an IC50 of 15 nM. T863 has no inhibitory activity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells .
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively .
PD 90780 is a non peptide antagonist of nerve growth factor (NGF). PD 90780 interacts with NGF, prevents NGF binds with p75 NTR. PD 90780 inhibits NGF-p75 NTR interaction with IC50s of 23.1 and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions . EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane .
SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L .
KL001 is a first-in-class cryptochrome (CRY, a flavoproteins that are sensitive to blue light, and is involved in the circadian rhythms of plants and animals) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis .
Antitumor agent-109 (compound 6) is an inhibitor of hyaluronic acid (HY-B0633A) targeting to CD44, as well as an anti-tumor agent. Hyaluronic acid interacts with differentiation cluster 44 (CD44) and is involved in tumor growth and invasion. Antitumor agent-109 inhibits MDA-MB-231 cells with EC50 value of 0.59 μM .
mPEG-CHO (MW 1000) participates in the formation of a three-dimensional porous scaffold that carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
FIKK9.1-IN-1 (Compound 1) is a FIKK9.1 inhibitor. FIKK9.1-IN-1 interacts with the ATP?binding residues in FIKK9.1. FIKK9.1-IN-1 is an antimalarial agent (IC50: 2.68 μg/mL) and disrupts the parasite life cycle and leads to the death of parasites .
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
TI17 is an inhibitor of the thyroid hormone receptor-interacting protein Trip13 and has anticancer activity. TI17 effectively inhibits multiple myeloma (MM) cell proliferation and induces cell cycle arrest and apoptosis. Trip13 is an AAA-ATPase that mediates double-strand break (DSB) repair; TI17 inhibits Trip13 function and increases DNA damage .
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM .
1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol . 1-Caffeoylquinic acid has anti-oxidative stress ability . 1-Caffeoylquinic acid inhibits PD-1/PD-L1interact .
β-Boswellic acid is isolated from the gum resin of Boswellia serrata.
β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation . β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells .
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
(E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
mPEG-CHO (MW 350) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 550) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 750) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 2000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 3400) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 5000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 10000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 20000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer .
(R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer .
LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway .
TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry .
AV-153, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 has anti-cancer activity .
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 µM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue .
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 µM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation .
LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons .
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons .
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity .
NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interactingserine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression .
EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism .
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity .
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
AV-153 free base, a 1,4-dihydropyridine (1,4-DHP) derivative, is an antimutagenic. AV-153 free base intercalates to DNA in a single strand break and reduces DNA damage, stimulates DNA repair in human cells in vitro. AV-153 free base interacts with thymine and cytosine and has an influence on poly(ADP)ribosylation. AV-153 free base has anti-cancer activity .
PINT-87aa, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa suppresses glioblastoma cell proliferation in vitro and in vivo .
TNIK-IN-3 is a potent, selective and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK), with an IC50 of 0.026 μM. TNIK-IN-3 could also inhibit Flt4 (IC50=0.030 μM), Flt1 (IC50=0.191 μM) and DRAK1 (IC50=0.411 μM). TNIK-IN-3 can be used for the research of colorectal cancer .
EP39 is a potent HIV-1 maturation inhibitor. EP39 interacts with the SP1 domain of Gag. EP39 decreases the dynamics of CA-SP1 junction, by binding to the QVT motif of the SP1 domain, and perturbs the natural coil-helix equilibrium on both sides of the SP1 domain by stabilizing the transient alpha helical structure. EP39 acts by arresting maturation of HIV-1 thereby blocking its infectivity .
TH10785 is a DNA glycosylase 1 (OGG1) activator, TH10785 can interact with the phenylalanine-319 and glycine-42 amino acids of OGG1 and increase the enzyme activity, generates β, δ-lyase enzymatic function. TH10785 can control the catalytic activity mediated by a nitrogen base within its molecular structure. TH10785 can be used for the research of various diseases and aging connected with DNA oxidative lesions .
NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 activates receptor-interactingserine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression .
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4 .
Dodecyl β-D-glucopyranoside is a non-ionic detergent and surfactant commonly used to solubilize and purify membrane proteins in biochemical research. Dodecyl β-D-glucopyranoside also interacts with bovine serum albumin (BSA) to quench its intrinsic fluorescence. The critical micelle concentration (CMC) of Dodecyl β-D-glucopyranoside (DG) and DG/BSA complex is 2.0 mM and 2.34 mM, respectively. Micelles can be formed in aqueous solutions above this concentration .
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
β Amyloid(28-35) human is a β-amyloid peptide (Abeta), a lipid-induced amyloid core fragment. β Amyloid oligomers are neurotoxic, and β Amyloid(28-35) human can interact with neuronal membranes, regulate secondary structure and neurotoxicity, and cause Alzheimer's disease. β Amyloid(28-35) human has anisotropic effects on the acidic phospholipid DPH, resulting in enhanced internal fluidity of lipid membrane bilayers .
TCL1(10-24) is a encompassing the betaA strand of human TCL1. TCL1(10-24) is a Akt inhibitor. TCL1(10-24) interacts with the Akt PH domain prevented phosphoinositide binding and hence inhibits membrane translocation and activation of Akt. TCL1(10-24) inhibits cellular proliferation and anti-apoptosis. TCL1(10-24) has tumor growth in vivo .
Aβ42 agonist-1 (compound 7a) is a small molecule compound that can promote Aβ42 aggregation. Aβ42 agonist-1 can interact with Aβ42 oligomers and pentamers to promote nontoxic aggregate self-assembly and rapid fibril formation. Aβ42 agonist-1 prevents Aβ42-induced cytotoxicity in HT22 hippocampal neuronal cells .
Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
PINT-87aa TFA, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa TFA directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa TFA suppresses glioblastoma cell proliferation in vitro and in vivo .
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
Octyl thiomaltoside (OTM) is a nonionic detergent commonly used in the purification and crystallization of membrane proteins. It belongs to the family of maltoside detergents and has a hydrophilic head group and a lipophilic tail group, enabling it to interact with water-soluble and membrane-bound proteins. OTMs are known for their ability to solubilize integral membrane proteins without disrupting their structure or function, making them an invaluable tool in biochemical and biophysical research. In addition to protein research, OTMs are used in a variety of other applications, including drug delivery systems, nanotechnology, and diagnostic analysis.
TCEP-d16 (hydrochloride) is the deuterium labeled TCEP hydrochloride[1]. TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry[2][3][4][5].
cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models .
Aβ42 agonist-2 (compound 7b) is a small molecule compound that can promote Aβ42 aggregation. Aβ42 agonist-2 can interact with Aβ42 oligomers and pentamers to promote nontoxic aggregate self-assembly and rapid fibril formation. Aβ42 agonist-2 prevents Aβ42-induced cytotoxicity in HT22 hippocampal neuronal cells .
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke .
β-Boswellic acid (Standard) is the analytical standard of β-Boswellic acid. This product is intended for research and analytical applications. β-Boswellic acid is isolated from the gum resin of Boswellia serrata. β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation . β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells .
Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS .
IQ 1 is a Wnt/β-catenin/CBP signalling sustainer. IQ 1 maintains long-term expansion of Wnt/β-catenin-driven mouse embryonic stem cells (ESCs) and prevents spontaneous differentiation by enhancing β-catenin/CBP-mediated transcription and preventing conversion to β-catenin/p300-mediated transcription. IQ-1 regulates Wnt signalling by interacting with PR72/130. IQ 1 can be used in study of ESCs expansion .
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1' pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM) .
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS .
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putidacytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression .
Octaethylene glycol monodecyl ether, is a nonionic surfactant commonly used in various industrial and research applications. It belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail and is suitable for use in lotions, detergents and solubilizers. Octaethylene glycol monodecyl ether is particularly useful in the study of membrane proteins, where it is used to solubilize and stabilize proteins for structural analysis techniques. In addition, Octaethylene glycol monodecyl ether has the ability to interact with and penetrate cell membranes, so it has potential applications in drug delivery and other medical fields.
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
Polyethylene glycol trimethylnonyl ether, is a nonionic surfactant commonly used in various industrial and research applications. It belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail and is suitable for use in lotions, detergents and solubilizers. Polyethylene glycol trimethylnonyl ether is particularly useful in protein chemistry, where it is used to solubilize and stabilize proteins, such as membrane proteins, for structural analysis techniques. In addition, Polyethylene glycol trimethylnonyl ether has potential applications in drug delivery and other medical fields due to its ability to interact with and penetrate cell membranes.
CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery .
Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment .
Octaethylene glycol monohexadecyl ether, is a nonionic surfactant commonly used in various industrial and research applications. Octaethylene glycol monohexadecyl ether belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail, suitable for use in lotions, detergents and solubilizers. Octaethylene glycol monohexadecyl ether is particularly useful in the study of membrane proteins, where it is used to solubilize and stabilize proteins for structural analysis techniques. In addition, Octaethylene glycol monohexadecyl ether has the ability to interact with and penetrate cell membranes, so it has potential applications in drug delivery and other medical fields.
DDMAB, or didodecyldimethylammonium bromide, is a cationic surfactant commonly used in a variety of industrial and research applications. It belongs to the family of quaternary ammonium compounds and has a positively charged head and a hydrophobic tail, which allows it to be used as a detergent, emulsifier and antimicrobial. Known for its ability to disrupt cell membranes, DDMAB is commonly used in microbiology to selectively isolate and identify bacteria. It is also used in nanotechnology to synthesize metal nanoparticles and other materials. In addition, DDMAB has the ability to interact with and penetrate cell membranes, which has potential applications in drug delivery, gene therapy, and other medical fields.
Hexanolamino PAF C-16 (1-O-hexadecyl-2-acetyl-sn-glycero-3-phospho (N,N,N trimethyl) hexanolamine) is a Platelet-activating Factor Receptor (PAFR) Modulator with partial agonist activity. Hexanolamino PAF C-16 induces platelet aggregation and macrophage production but fails to increase [Ca2+]i in platelets, suggesting that PAF receptors may interact with PAF receptors through Ca 2+-dependent and -independent pathways. Related to platelet aggregation .
MG-1102 is first-in-class dual binder of monomeric tau and pre-miRNA-146a. MG-1102 shows specific inhibition of miRNA146a with IC50s of 0.21 mM and 0.36 mM specific inhibition of doublelabeled pre-miRNA146a and mono-labeled pre-miRNA146a, respectively. MG-1102 interacts with tau monomers with a Kd of 3.21 mM by surface plasmon resonance (SPR). MG-1102 is a potential multi-target-directed ligands (MTDLs) for Alzheimer’s disease (AD) .
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2(homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy .
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp .
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development .
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research .
Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection[1][2][3][4][5].
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division .
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp) inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitory activity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
A unique set of molecules containing mild electrophilic moieties that covalently interact with amino acid residues in the target protein. The diversity of our compounds for covalent drug discovery ranges from natural product-like scaffolds to macrocycles, creating multiple opportunities in hit generation for a selected target.
Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide: e.g. stability against proteolysis (duration of activity) and poor bioavailability. Certain other properties, such as receptor selectivity or potency, often can be substantially improved. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. Hence mimics have great potential in drug discovery.
MCE Peptidomimetic Library contains 376 compounds including peptoid, α-helix mimetics, β-turn/sheets mimetics, etc. This library is an indispensable tool of structure-activity relationships in drug discovery.
Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications.
MCE offers a unique collection of 491 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth .
9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
AIE-GA is a Golgi apparatus (GA) fluorescent probe (green channel: λex = 405 nm, λem = 500-700 nm). AIE-GA has a favourable binding ability to interact with COX-2. AIE-GA binds to the cyclooxygenase catalytic site of COX-2 .
NDSB 256-4T is a non-washing sulfabetaine compound. NDSB-256-4T prevents protein aggregation and promotes protein folding by interacting with early folding intermediates .
L-Tartaric acid (L-(+)-Tartaric acid) sodium hydrate is the enantiomer of D-tartaric acid. L-Tartaric acid (HY-Y0293) is a white crystalline dicarboxylic acid found in many plants, such as grapes, and is one of the main organic acids in wine. L-Tartaric acid sodium hydrate which acts as a flour bulking agent and as a food additive can interact with sodium bicarbonate to produce carbon dioxide .
Trimethyloctylammonium bromide (TOAB) is used as a surfactant and phase transfer catalyst in various chemical reactions. TOAB can be used in the synthesis of nanomaterials due to its ability to selectively transfer ions across interfaces and as a surfactant in the production of emulsions and foams. It is valued for its amphiphilic properties, which allow it to interact with water and oils, stabilizing and dispersing mixtures.
Plasmin is an important protease present in blood that degrades many plasma proteins, including fibrin clots. Plasmin can also act as a potent regulator of the immune process and can directly interact with various cell types, including monocytes, macrophages, and dendritic cells .
Phospholipid-PEG-Biotin (MW 1000) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
Phospholipid-PEG-Biotin (MW 3400) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
Phospholipid-PEG-Biotin (MW 10000) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
Phospholipid-PEG-Biotin (MW 20000) is a phospholipid PEG derivative that has a biotin and a phospholipid bridged by a linear PEG linker. Phospholipid-PEG-Biotin (MW 3400) can interact with avidinylated antibodies. Phospholipid-PEG-Biotin (MW 3400) can be used to modify liposome and cells surface, and pancreatic islets for cell transplantation .
mPEG-CHO (MW 1000) participates in the formation of a three-dimensional porous scaffold that carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 350) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 550) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 750) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 2000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 3400) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 5000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 10000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
mPEG-CHO (MW 20000) participates in the formation of a three-dimensional porous scaffold which carries active substances to form a delivery vehicle. The -CHO functional group interacts with the -NH2 functional group of the chitosan chain to form a glutaraldehyde-type adduct to functionalize mPEG. This functionalization and cross-linking can affect the rigidity of the delivery system, allowing slow release of the cross-linked conjugate system.
Dodecyl β-D-glucopyranoside is a non-ionic detergent and surfactant commonly used to solubilize and purify membrane proteins in biochemical research. Dodecyl β-D-glucopyranoside also interacts with bovine serum albumin (BSA) to quench its intrinsic fluorescence. The critical micelle concentration (CMC) of Dodecyl β-D-glucopyranoside (DG) and DG/BSA complex is 2.0 mM and 2.34 mM, respectively. Micelles can be formed in aqueous solutions above this concentration .
Octyl thiomaltoside (OTM) is a nonionic detergent commonly used in the purification and crystallization of membrane proteins. It belongs to the family of maltoside detergents and has a hydrophilic head group and a lipophilic tail group, enabling it to interact with water-soluble and membrane-bound proteins. OTMs are known for their ability to solubilize integral membrane proteins without disrupting their structure or function, making them an invaluable tool in biochemical and biophysical research. In addition to protein research, OTMs are used in a variety of other applications, including drug delivery systems, nanotechnology, and diagnostic analysis.
Octaethylene glycol monodecyl ether, is a nonionic surfactant commonly used in various industrial and research applications. It belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail and is suitable for use in lotions, detergents and solubilizers. Octaethylene glycol monodecyl ether is particularly useful in the study of membrane proteins, where it is used to solubilize and stabilize proteins for structural analysis techniques. In addition, Octaethylene glycol monodecyl ether has the ability to interact with and penetrate cell membranes, so it has potential applications in drug delivery and other medical fields.
Polyethylene glycol trimethylnonyl ether, is a nonionic surfactant commonly used in various industrial and research applications. It belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail and is suitable for use in lotions, detergents and solubilizers. Polyethylene glycol trimethylnonyl ether is particularly useful in protein chemistry, where it is used to solubilize and stabilize proteins, such as membrane proteins, for structural analysis techniques. In addition, Polyethylene glycol trimethylnonyl ether has potential applications in drug delivery and other medical fields due to its ability to interact with and penetrate cell membranes.
Octaethylene glycol monohexadecyl ether, is a nonionic surfactant commonly used in various industrial and research applications. Octaethylene glycol monohexadecyl ether belongs to the family of polyethylene glycol (PEG) ethers with a hydrophilic head and lipophilic tail, suitable for use in lotions, detergents and solubilizers. Octaethylene glycol monohexadecyl ether is particularly useful in the study of membrane proteins, where it is used to solubilize and stabilize proteins for structural analysis techniques. In addition, Octaethylene glycol monohexadecyl ether has the ability to interact with and penetrate cell membranes, so it has potential applications in drug delivery and other medical fields.
DDMAB, or didodecyldimethylammonium bromide, is a cationic surfactant commonly used in a variety of industrial and research applications. It belongs to the family of quaternary ammonium compounds and has a positively charged head and a hydrophobic tail, which allows it to be used as a detergent, emulsifier and antimicrobial. Known for its ability to disrupt cell membranes, DDMAB is commonly used in microbiology to selectively isolate and identify bacteria. It is also used in nanotechnology to synthesize metal nanoparticles and other materials. In addition, DDMAB has the ability to interact with and penetrate cell membranes, which has potential applications in drug delivery, gene therapy, and other medical fields.
IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
TAT-P4-(DATC5)2 is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 can inhibit addiction in rats .
TAT-P4-(DATC5)2 TFA is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 TFA can inhibit addiction in rats .
Hsp70-derived octapeptide is a conserved octapeptide of the C-terminal end of Hsp70, which physically interacts with tetratricopeptide repeat (TPR) motifs .
Jingzhaotoxin-XII (JzTx-XII) is a specific Kv4.1 channel inhibitor with an IC50 of 0.363 μM. Jingzhaotoxin-XII interacts with the channels by modifying the gating behavior .
HD5 is a biological active peptide. (a natural lectin-like human defensins-5 (HD5) peptide secreted by the Paneth cells in the crypts of Lieberkuhn, could interact with glycosylated proteins and lipid components)
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors .
Dynorphin B 29 (Leumorphin) (pig) is a petide. Dynorphin B 29 (pig) can interact with multiple receptors in the brain, as well as in isolated tissue systems. Dynorphin B 29 (pig) can be used for the research of immunoreaction .
TAT-NSF700 Fusion Peptide is a potent N-ethyl-maleimide-sensitive factor (NSF) inhibitor. TAT-NSF700 Fusion Peptide can readily permeate the cell membrane and interact with the intracellular organelle directly .
Fasciculin-I is isolated from the mambas venom. Fasciculin-I exerts its toxic effects by inhibiting acetylcholinesterase (AChE). Fasciculin-I blocks α-neurotoxins of nicotinic acetylcholine receptors and cardiac toxins that interact with cell membranes .
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide) .
[Hyp3]-Bradykinin, naturally occurring peptide hormone, is a bradykinin receptor agonist. [Hyp3]-Bradykinin interacts with B2-bradykinin receptors and stimulates inositol phosphate production in cultured human fibroblasts .
Myoregulin (MLN peptide) is a member of the regulin family. Myoregulin regulates muscle performance by modulating intracellular calcium handling. Myoregulin interactes directly with sarcoplasmic reticulum Ca 2+-ATPase (SERCA) and impedinf Ca 2+ uptake into the sarcoplasmic reticulum .
JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide) .
Neuropeptide FF (NPFF), an octapeptide belonging to the RF-amide family of peptides, interacts with two distinct G-protein-coupled receptors, NPFF(1) and NPFF(2) and has wide variety of physiological functions in the brain including central cardiovascular and neuroendocrine regulation .
Crotamine is a Na + channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom .
Myoregulin (MLN peptide) TFA is a member of the regulin family. Myoregulin TFA regulates muscle performance by modulating intracellular calcium handling. Myoregulin TFA interactes directly with sarcoplasmic reticulum Ca 2+-ATPase (SERCA) and impedinf Ca 2+ uptake into the sarcoplasmic reticulum .
F(N-Me)GA(N-Me)IL is a biological active peptide. (Double N-methylated derivatives of amyloidogenic and cytotoxic partial IAPP sequence were found to be devoid of β-sheet structure, amyloidogenicity and cytotoxicity, The derivatives were able to interact with the native sequences and inhibit amyloid formation)
Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl (compound (CPF(LL)) is an HIV-1 inhibitor. Carbomethoxycarbonyl-D-Pro-D-Phe-OBzl interacts with gp120 to block gp120 binding to CD4 and preserve CD4-dependent T cell function .
Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1 .
SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
Delta-hemolysin (Delta-lysin), a 26 amino acid peptide, is a hemolytic peptide produced by Staphylococcus. Delta-hemolysin may slightly perturb a membrane or lead to cell lysis. Delta-hemolysin is a model in the study of peptides interacting with membranes. Delta-hemolysin is poorly active against bacteria .
Transdermal Peptide Disulfide (TD 1 Disulfide(peptide)) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide can enhance the transdermal delivery of many macromolecules .
μ-TRTX-Hd1a, a spider venom, is a selective NaV 1.7 inhibitor. μ-TRTX-Hd1a is a gating modifier that inhibits human NaV 1.7 by interacting with the S3b-S4 paddle motif in channel domain II .
Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules .
Delta-hemolysin (Delta-lysin) TFA, a 26 amino acid peptide, is a hemolytic peptide produced by Staphylococcus. Delta-hemolysin TFA may slightly perturb a membrane or lead to cell lysis. Delta-hemolysin TFA is a model in the study of peptides interacting with membranes. Delta-hemolysin TFA is poorly active against bacteria .
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans) .
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
Decapeptide-12, a small oligopeptide, is a tyrosinase inhibitor that interacts with C-terminal residue of tyrosinase (Kd: 61.1 μM). Decapeptide-12 is a competitive inhibitor of mushroom tyrosinase (IC50: 40 µM). Decapeptide-12 also increases transcription of SIRT. Decapeptide-12 reduces melanin content in melanocytes. Decapeptide-12 is used for the research of melanogenesis, senescence, inflammation .
Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV) .
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity .
PINT-87aa, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa suppresses glioblastoma cell proliferation in vitro and in vivo .
CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1). CKLF1-C19 interacts with CCR4, and inhibits chemotaxis induced by both CKLF1 and CCL17. CKLF1-C19 can suppress allergic lung inflammation via inhibiting chemotaxis mediated by CCR3 and CCR4 .
FN-A208 is a biological active peptide. (This peptide is a fusion of A208, derived from murine laminin a1, and the active site of fibronectin (GRGDS), with a glycine spacer. This peptide forms amyloid-like fibrils and promotes formation of actin stress fibers that mediate fibroblast cell attachment, offering it potential as a bioadhesive for tissue regeneration and engineering. FN-A208 interacts with IKVAV receptors and integrins. Its activity is disrupted by the presence of EDTA.)
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
β Amyloid(28-35) human is a β-amyloid peptide (Abeta), a lipid-induced amyloid core fragment. β Amyloid oligomers are neurotoxic, and β Amyloid(28-35) human can interact with neuronal membranes, regulate secondary structure and neurotoxicity, and cause Alzheimer's disease. β Amyloid(28-35) human has anisotropic effects on the acidic phospholipid DPH, resulting in enhanced internal fluidity of lipid membrane bilayers .
TCL1(10-24) is a encompassing the betaA strand of human TCL1. TCL1(10-24) is a Akt inhibitor. TCL1(10-24) interacts with the Akt PH domain prevented phosphoinositide binding and hence inhibits membrane translocation and activation of Akt. TCL1(10-24) inhibits cellular proliferation and anti-apoptosis. TCL1(10-24) has tumor growth in vivo .
PINT-87aa TFA, an 87-amino acid (aa) peptide, is encoded by the circular form of the long intergenic non-protein-coding RNA p53-induced transcript (LINC-PINT). PINT-87aa TFA directly interacts with polymerase associated factor complex (PAF1c) and inhibits the transcriptional elongation of multiple oncogenes. PINT-87aa TFA suppresses glioblastoma cell proliferation in vitro and in vivo .
Tat-beclin 1 scrambled is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
Tat-beclin 1 scrambled TFA is the scrambled part and a scrambled control of Tat-beclin 1 (HY-P2260), which is derived from a region of the autophagy protein, beclin 1. beclin 1 induces autophagy via binding human immunodeficiency virus, HIV-1 Nef and interacting with negative regulator GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens, such as HIV-1. Tat-beclin 1 also reduces mortality in mice infected with chikungunya or West Nile virus .
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
Tezepelumab (AMG 157) is human monoclonal antibody (IgG2λ) that binds specifically to TSLP, blocking it from interacting with its heterodimeric receptor. Tezepelumab can be used for the research of severe, uncontrolled asthma .
Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects .
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
Anti-MERS-D12 mAb (MERS-D12; MERS Antibody-D12) is a human monoclonal IgG1. Anti-MERS-D12 mAb binds directly to the DPP4 interacting region of the MERS-CoV Spike receptor binding domain (RBD) and effect neutralization by directly blocking receptor binding .
Roemerine, an aporphine alkaloid, isolated from the leaves of Fibraurea recisa Pierre, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells .
Filipin III is the major component of Filipin, a 28-membered ring pentaene macrolide antifungal antibiotic produced by S. filipinensis, S. avermitilis and S. miharaensis. Filipin interacts with membrane sterols causing the alteration of membrane structure .
Stepharine, an natural alkaloid, directly interactes with TLR4 and binds to the TLR4/MD2 complex (TLR4 inhibitor). Stepharine possesses anti-aging, anti-viral and anti-hypertensive effects .
Antiviral agent 51 (compound a) is a potent antiviral agent. Antiviral agent 51 is a fucoidan. Antiviral agent 51 interacts with DENV-2 RNA Dependant RNA polymerase (RdRp) .
Jasmonic acid ((-)-Jasmonic acid) is a plant growth regulator and a derivative of α-Linolenic acid (HY-N0728). Jasmonic acid signaling can also induce the MAP kinase cascade pathway, calcium channel, and many processes that interact with signaling molecules .
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth .
Colcemid (Demecolcine) is a potent mitotic inhibitor with an IC50 value of 2.4 μM for inhibition of tubulin polymerization. Colcemid (Demecolcine) can interact with tubulin dimers to induce anti-mitotic action and inhibit microtubule growth. Colcemid (Demecolcine) can be used for inflammatory disorders and cancer research .
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate . Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor .
L-Tartaric acid (L-(+)-Tartaric acid) sodium hydrate is the enantiomer of D-tartaric acid. L-Tartaric acid (HY-Y0293) is a white crystalline dicarboxylic acid found in many plants, such as grapes, and is one of the main organic acids in wine. L-Tartaric acid sodium hydrate which acts as a flour bulking agent and as a food additive can interact with sodium bicarbonate to produce carbon dioxide .
Solasurine is a steroidal alkaloid that can be isolated from Solanum surrattence. Solasurine can interact with the C3-like protease (SARS-CoV-2 main protease) amino acids Phe8, Pro9, Ile152, Tyr154, Pro293, Phe294, Val297, and Arg298 .
Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity .
Cyclic GMP sodium (cGMP) is an important regulator of short-term changes in smooth muscle tone and longer-term responses to chronic drug research or proliferative signals, it is in response to atrial natriuretic peptide (ANP) or nitric oxide (NO). Cyclic GMP sodium interacts with cation channels to regulate ion transport or activate the cyclic GMP-dependent protein kinase to result in protein phosphorylation .
1-Caffeoylquinic acid is an effective NF-κB inhibitor, shows significant binding affinity to the RH domain of p105 with Ki of 0.002 μM and binding energy of 1.50 Kcal/mol . 1-Caffeoylquinic acid has anti-oxidative stress ability . 1-Caffeoylquinic acid inhibits PD-1/PD-L1interact .
β-Boswellic acid is isolated from the gum resin of Boswellia serrata.
β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation . β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells .
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons .
Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP) .
β-Boswellic acid (Standard) is the analytical standard of β-Boswellic acid. This product is intended for research and analytical applications. β-Boswellic acid is isolated from the gum resin of Boswellia serrata. β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation . β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells .
Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putidacytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression .
ZW10 interactor (ZWINT) is clearly involved in kinetochore function. ZWINT interacts with ZW10, a kinetochore protein, possibly regulating the association between ZW10 and kinetochores. ZWINT is required for kinetochore formation and spindle checkpoint activity and remains detectable on the kinetochore until late anaphase. ZWINT has a uniform distribution in the cytoplasm of interphase cells. ZWINT/ZW10 interactor Protein, Human (His) is the recombinant human-derived ZWINT/ZW10 interactor protein, expressed by E. coli , with N-6*His labeled tag. The total length of ZWINT/ZW10 interactor Protein, Human (His) is 277 a.a., with molecular weight of ~35 kDa.
ZWINT, a vital MIS12 complex component, is essential for kinetochore and spindle checkpoint activity. It plays a pivotal role in ZW10 targeting to the kinetochore in prometaphase, forming interactions with ZW10, MIS12, and NDC80 subunit of the NDC80 complex. ZWINT's engagement with KNL1, CETN3, DSN1, and PMF1 underscores its multifaceted role in orchestrating kinetochore complex assembly and functionality during mitosis. ZWINT/ZW10 interactor Protein, Human (GST) is the recombinant human-derived ZWINT/ZW10 interactor protein, expressed by E. coli , with N-GST labeled tag. The total length of ZWINT/ZW10 interactor Protein, Human (GST) is 277 a.a., with molecular weight of ~58.2 kDa.
The TRIP13 protein plays a key role in meiosis, affecting chromosome reorganization and structural development. It is critical for the formation of crossing and noncrossing pathways, homologous synapses, and synaptonemal complexes. TRIP13 Protein, Human (His, Strep) is the recombinant human-derived TRIP13 protein, expressed by E. coli , with N-Strep, N-6*His labeled tag. The total length of TRIP13 Protein, Human (His, Strep) is 432 a.a., .
The TRIP13 protein plays a key role in meiosis, affecting chromosome reorganization and structural development. It is critical for the formation of crossing and noncrossing pathways, homologous synapses, and synaptonemal complexes. TRIP13 Protein, Human is the recombinant human-derived TRIP13 protein, expressed by E. coli , with tag free. The total length of TRIP13 Protein, Human is 432 a.a., .
Pomalidomide-d3 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors[1][2].
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
Pomalidomide-d4 is the deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors<
Dodecyltrimethylammonium-d25 (bromide) is the deuterium labeled Dodecyltrimethylammonium (bromide)[1]. Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction[2].
Dodecyltrimethylammonium-d34 (bromide) is the deuterium labeled Dodecyltrimethylammonium (bromide)[1]. Dodecyltrimethylammonium bromide (DTAB) is a surfactant. Dodecyltrimethylammonium bromide interacts with DNA and changes the mechanical properties of DNA on binding and the specific binding parameters of the interaction[2].
Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
TCEP-d16 (hydrochloride) is the deuterium labeled TCEP hydrochloride[1]. TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry[2][3][4][5].
Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection[1][2][3][4][5].
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
EC359 is a potent, selective, high affinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions . EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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