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SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria .
DCAF1 binder 1 is a selective for the CRL4 DCAF1 E3 ligase complex. DCAF1 binder 1 is a ligands for E3 Ligase, involving in targeted protein degradation (TPD) .
α-Synuclein aggregate binder 1 (Compound C05-05) is a collective binder and an inhibitor for α-synuclein aggregation. α-Synuclein aggregate binder 1 is utilized in Positron Emission Tomography (PET) imaging and fluorescence microscope, that can diagnose and ameliorate the neurodegenerative disease .
JAK2 JH2 binder-1 (compound 11) is a potent and selective JAK2 JH2binder, with a Kd of 37.1 nM. JAK2 JH2 binder-1 has the potential for various myeloproliferative neoplasms research .
Phosphatase Binder-1 (comppund i-196) provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Phosphatase Binder-1 plays an important role in cancer .
TSLP binder-1 (compound 46) is a bicyclic peptide, which binds to thymic stromal lymphopoietin (TSLP) at the site used by IL-7Rα subunit, shows high affinity for TSLP, with KD of 13 nM. TSLP binder-1 reveals good stability in rat plasma and rat lung S9 fraction .
YEATS4 binder-1(4e) is a potent and selective YEATS4binder that binds to the KAc recognition site of the YEATS structural domain with a Ki value of 37 nM .
Colestilan (MCI-196) is a non-absorbed, non-calcium-based phosphate binder and is also a non-metallic, anion exchange resin. Colestilan is orally active and can be used for hypercholesterolaemia research .
PSMA binder-2 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
Ferric citrate (Iron(III) citrate), an orally active iron supplement, is an efficacious phosphate binder. Ferric citratee can be used for iron deficiency anemia and chronic kidney disease (CKD) research .
PSMA binder-1 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or it can be labeled with 225Ac (to obtain Actinium-225-PSMA-Trillium (BAY 3563254)), which has a radioactive killing effect; it can be used as a Macropa chelator for targeted radionuclide therapy (TRT) , has a strong inhibitory effect on metastatic castration-resistant prostate cancer (mCRPC) .
Sevelamer carbonate is an orally active and non-calcium-based phosphate binding agent and used for the hyperphosphatemia of chronic kidney disease (CKD)research. Sevelamer carbonate effectively lowers serum phosphorus levels hile having minimal effect on serum calcium or serum chloride levels in vivo. Sevelamer carbonate is considered as an improved, buffered form of sevelamer (HY-13995) .
Sevelamer (carbonate) (Standard) is the analytical standard of Sevelamer (carbonate). This product is intended for research and analytical applications. Sevelamer carbonate is an orally active and non-calcium-based phosphate binding agent and used for the hyperphosphatemia of chronic kidney disease (CKD)research. Sevelamer carbonate effectively lowers serum phosphorus levels hile having minimal effect on serum calcium or serum chloride levels in vivo. Sevelamer carbonate is considered as an improved, buffered form of sevelamer (HY-13995) .
Patiromer is an orally active and potent hyperkalemia inhibitor and a nonabsorbed potassium binder. Patiromer polymer is bound with calcium which is released in the colon in exchange for binding potassium .
NHS-Modified MMAF (WO2012143499A2, intermediat 210) is an intermediate which can be used for producing the anti-mesothelin binder-agent conjugates (ADCs) .
MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker .
YEATS4-IN-1 (Compound 4d) is a potent and selective YEATS4binder that binds to the KAc recognition site of the YEATS structural domain with a Ki value of 33 nM .
Calcium acetate, United States Pharmacopeia (USP) Reference Standard (Calcium acetate (Pharmaceutical primary standard, USP)), a phosphate binder that can reduce phosphorus content, United States Pharmacopeia (USP) reference standard .
DNA crosslinker 3 (dihydrochloride) (compound 1) is a potent DNA minor groovebinder with DNA binding affinity (ΔTm) of 1.4 °C. DNA crosslinker 3 (dihydrochloride) can be used for researching anticancer .
DNA crosslinker 1 dihydrochloride (Compound 4) is a potent DNA minor groovebinder with DNA binding affinity (ΔTm) of 1.1 °C. DNA crosslinker 1 dihydrochloride can be used for researching anticancer .
PROTAC RIPK degrader-6 (example 1) is a Cereblon-based PROTAC targeting RIP Kinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder .
Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.
Acetyl-cyclosporin A aldehyde is an acetylated Cyclosporin A (HY-B0579) derivative with a reducing aldehyde group. Cyclosporin A is a potent calmodulin inhibitor and cyclophilin binder that can target the nuclear translocation of NF-AT and cause mitochondrial damage.
3,5,7-Trihydroxychromone is the analogue of galangin. 3,5,7-Trihydroxychromone is also the binder of bovine serum albumin. 3,5,7-Trihydroxychromone undergoes multiple antioxidant pathways .
Netropsin dihydrochloride is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei . Netropsin dihydrochloride exhibits antiviral activity against the vaccinia virus .
Pamaqueside (CP148623) is a cholesterol absorption inhibitor and a potent binder of the SARS-CoV-2 receptor-binding domain (RBD), which may inhibit viral cellular entry. Pamaqueside can be utilized in metabolic and antiviral research .
GID4 Ligand 3 (compound 16) is a binder of GID4 with an Kd value of 110 μM in vitro and an IC50 value of 148.5 μM. GID4 Ligand 3 can be used for the research related to cereblon and Von Hippel-Lindau .
Distamycin A (NSC-82150), an oligopeptide antibiotic, is a minor groove binder which binds to B-form DNA, preferentially at A/T rich sites.Distamycin A can change Enediyne-induced DNA cleavage sites and enhances apoptosis .
Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groovebinder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].
PROTAC BRD9-binding moiety 5 is a selective BRD9binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells .
Vapendavir diphosphate (BTA798 diphosphate) is a potent enteroviral capsid binder (CB). Vapendavir diphosphate (BTA798 diphosphate) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
XL44, an hRpn13 binder, induces hRpn13-dependent apoptosis and also restricts cell viability by a PCLAF-dependent mechanism. XL44 induces ubiquitin-dependent loss of hRpn13 Pru and ubiquitin-independent loss of select KEN box containing proteins .
4-PQBH is a potent Nur77binder (KD=1.17 μM). 4-PQBH extensively induces caspase-independent cytoplasmic vacuolization and paraptosis through Nur77-mediated ER stress and autophagy. 4-PQBH can be used for cancer research .
AGPS-IN-1 (Compound 2i) is an effective AGPS binder. AGPS-IN-1 reduces ether lipids levels and cell migration rate. AGPS-IN-1 inhibits epithelial-mesenchymal transition (EMT) in prostate PC-3 and breast MDA-MB-231 cancer cells .
MYC-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) to MYC internal ribosome entry site (IRES).MYC-RIBOTAC contains a MYC mRNA-binder and a small molecule that recruits and locally activates RNase L1 and decreases the mRNA and protein expression levels of MYC, induces apoptosis. MYC-RIBOTAC can be used for anticancer research .
Vapendavir-d5 is the deuterium labeled Vapendavir. Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
GID4 Ligand 1 (compound 88) is a cell-permeable and high-selective GID4binder (IC50=5.4 μM; Kd=5.6 μM), binds to GID4 in cells (EC50=558 nM). GID4 Ligand 1 can be used for the synthesis of PROTACs .
Dextrins are a group of low molecular weight carbohydrates produced by the hydrolysis of starch. Dextrin is commonly used as a thickener, stabilizer or binder in a variety of foods including baked goods, beverages and confectionary. In addition, it is used in the production of adhesives, paper and textiles. Its unique chemical properties make it an important ingredient in a variety of industrial processes, especially in construction and packaging.
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groovebinder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
Nur77 modulator 1 is a good Nur77binder (KD = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .
Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
S-MGB-234 is a minor groove binder of Animal African Trypanosomiasis (AAT). S-MGB-234 displays excellent in vitro activities against the principal causative organisms of AAT; Trypanosoma congolense, and Trypanosoma vivax. S-MGB-234 does not show cross-resistance with the current diamidine agents and are not internalized via the transporters used by diamidines .
HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation .
Starch (from corn) is a carbohydrate extracted from the kernel of the corn plant. It contains two main components, namely amylose and amylopectin. Starches from corn have various applications in the food industry as thickeners, stabilizers and binders. It is commonly used in the production of products such as baked goods, snacks, sauces and soups. In addition, it can be used as a raw material for the production of biofuels and bioplastics.
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
BRD32048 is a direct binder of ETV1 with a KD of 17.1 μM. BRD32048 modulates both ETV1-mediated transcriptional activity and invasion of ETV1-driven cancer cells. BRD32048 inhibits ETV1 acetylation and promotes its degradation. BRD32048 acts as a top candidate ETV1 perturbagen .
PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγbinder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects .
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
VIP236 is a small-molecule-drug conjugates (SMDCs) consisting of an αvβ3 integrin binder linked to an optimized Camptothecin (HY-16560) topoisomerase I (TOP1) inhibitor payload. VIP236 exerts anticancer activity by targeting αvβ3 integrins, and it can release payload upon cleavage by neutrophil elastase in the tumor microenvironment .
S-MGB-234 TFA is a minor groove binder used for African Animal Trypanosomiasis (AAT). S-MGB-234 exhibits excellent in vitro activity against the primary pathogens of AAT: Trypanosoma congolense and Trypanosoma vivax. S-MGB-234 TFA does not show cross-resistance with current diamidine active molecules and is not internalized via the transporters used by diamidines .
RA839 is a noncovalent small molecule binder to Keap1 with a Kd of ∼6 μM and selective activator of Nrf2 signaling. RA839 prevents the induction of both inducible nitric-oxide synthase expression and nitric oxide release in response to lipopolysaccharides in macrophages. RA839 is a selective inhibitor of the Keap1/Nrf2 interaction and a useful tool compound to study the biology of Nrf2 .
Luviquat FC 550 is a cationic polymer commonly used in a variety of personal care and cosmetics. It is a viscous liquid containing quaternary ammonium groups which give it a positive charge. Luviquat FC 550 has a variety of properties suitable for these applications including its ability to provide conditioning, antistatic and film-forming properties to hair and skin. In addition, it is used as a binder in oral care products and as a flocculant in industrial water treatment.
RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2 inhibitor that inhibits the RAD51 BRCA2 protein protein interaction. RAD51-IN-8 also is a protein−protein interaction (PPI) inhibitor. RAD51-IN-8 has inhibitory activity for H4A4 with an EC50 value of 19 μM .
1,4-Anhydro-D-xylitol is a compound belonging to the class of sugar alcohols. It is derived from xylitol, a natural sweetener found in many fruits and vegetables. 1,4-Anhydro-D-xylitol is commonly used as a low-calorie sweetener and excipient in the food and pharmaceutical industries, and as a filler or binder in pharmaceutical formulations. It has also been investigated for its potential use in the development of biodegradable plastics and other sustainable materials.
LHF418 is an effective SOS1 PROTAC degrader with a DC50 value of 209.4 nM in A549 cells. LHF418 can effectively inhibit RAS signaling and colony formation in KRAS-driven cancer cells. (Structural note: (Blue: Cereblon ligand (HY-A0003), Black: linker; Pink: SOS1 binder SOS1 Ligand intermediate-3 (HY-161452)) .
Starch pregelatinized can be used as an excipient, such as Glidants, diluents, disintegrants, binders, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Permanent Orange (Standard) is the analytical standard of Permanent Orange. This product is intended for research and analytical applications. Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research . (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
GQN-B37-E is a potent selective binder and inhibitor of MCL-1. GQN-B37-E binds to the BH3-domain-binding pocket in MCL-1. GQN-B37-E exhibits binding affinity for MCL-1 at the submicromolar range (Ki = 0.6 μM) without apparent binding to BCL-2 or BCL-XL .
N-Methylmesoporphyrin IX (NMM), a widely used G-quadruplex DNA specific fluorescent binder, is an efficient probe for monitoring Aβ fibrillation. N-Methylmesoporphyrin IX is an in situ inhibitor and an ex situ monitor for Aβ amyloidogenesis both in vitro and in cells. N-Methylmesoporphyrin IX is sensitive to G-quadruplexes DNA but has no response to duplexes, triplexes and single-stranded forms DNA. N-Methylmesoporphyrin IX is nonfluorescent alone or in monomeric Aβ environments, but emits strong fluorescence through stacking with the Aβ assemblies .
GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders .
SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 can be used for the research of biological functions and disease associations of SETDB1-TTD .
Ethyl acrylate-methyl methacrylate copolymer can be used as an excipient, such as sustained-release coating materials, matrix sustained-release tablet binders and retarders. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Aluminum magnesium silicate can be used as an excipient, such as adsorbent, stabilizer, suspending agent, disintegrant for tablet and capsule, binder for tablet, thickener. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer copolymer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer homopolymer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer interpolymer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
SETDB1-TTD-IN-1 TFA is a potent, selective and endogenous binder competitive ligand of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD) that binds to TTD, with a Kd of 88 nM. SETDB1-TTD-IN-1 TFA increases SETDB1 methyltransferase activity. SETDB1-TTD-IN-1 TFA can be used for the research of biological functions and disease associations of SETDB1-TTD .
EV-A71-IN-1 is a human enterovirus A71 (EV-A71) capsid protein inhibitor with an EC50 of 0.27 μM against EV-A71. EV-A71-IN-1 is a capsid binder that blocks the interaction between the viral VP1 and the host receptor hSCARB2. EV-A71-IN-1 inhibits a series of different human enteroviruses without significant cytotoxicity (CC50>56.2 μM) .
PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC50=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .
PSMA-trillium is a PSMA targeting compound, consisting of a PSMA targeting molecule (PSMA binder), a Macropa chelating molecule, and a group that regulates pharmacokinetics (PK modifier). PSMA-trillium is a non-radioactive form of Actinium-225-PSMA-Trillium (BAY 3563254) with improved PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind Ac through the Macropa chelating molecule, or the radioactive isotope 225Actinium. Actinium-225-PSMA-Trillium is a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC) .
Conalbumin (Ovotransferrin), also known as ovotransferrin, is a monomeric glycoprotein consisting of 686 amino acids, encoded by the avian transferrin gene in the oviduct, and a prominent component of chicken egg white. Exhibiting a unique glycosylation pattern that differentiates it from serum transferrin, Conalbumin is a potent iron binder that plays a crucial role in iron transport to developing embryos. Additionally, it possesses a range of biological activities, including antimicrobial, antifungal, antiviral, anticancer, antioxidative, antihypertensive, and immunoregulatory properties, making it valuable in numerous applications such as infant formula ingredients, food additives, and agents for enhancing animal health.
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM .
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) .
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
(R)-Phe-A110/B319, a hapten, is a selective binder to tumor-associated antigens. (R)-Phe-A110/B319 has a 20-fold higher affinity towards the H1047R mutant of p110α in the p110α/p85α PI3K complex. (R)-Phe-A110/B319 can be used for the research of conditional chimeric antigen receptor T (CAR-T) cell activation and tumor targeting .
GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC) .
ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
Croscarmellose sodium is a commonly used pharmaceutical additive approved by the US Food and Drug Administration (FDA). Croscarmellose sodium is used in injectable preparations as a suspending agent to promote solubilization of compounds with poor water solubility. Croscarmellose sodium is also present in tablets as binder, glidant and antiadherent, in bulk laxatives as active principle and as an additive in food products. Croscarmellose sodium can be used as an excipient, such as excipients, disintegrants, aids in disintegration. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
MS182 (compound 11) is an acetylation targeting chimera (AceTAC) designed based on p53 Y220C stabilizer and targeting p53 Y220C. MS182 is composed of p53 Y220C and p300/CBP binders, respectively, coupled by a linker. MS182 forms a ternary complex with p300/CBP acetyltransferase and p53 Y220C in a time- and concentration-dependent manner, effectively acetylating lysine at position 382 of p53 Y220C (ACE50: 1.52 μM). MS182 also exhibited considerable bioavailability in mice, with GI50 values of 2.16 μM and 1.83 μM for BxPC3 (p53 Y220C/-) and NUGC (p53 Y220C/+), respectively .
NC-182 is a novel antitumor compound with a benzo[a]phenazine ring. The interaction mode of the agent with DNA and its effect on DNA conformation were systematically investigated by fluorescence, absorption and circular dichroism spectroscopy as well as viscosity titration measurements, and were compared with those of the DNA minor groove binder distamycin and the DNA base intercalator daunomycin. NC-182 was found to be a strong DNA intercalator, especially for B-form DNA, although without specificity for base pairs. The binding of NC-182 to B-DNA exhibited a biphasic behavior depending on the molar ratio of agent to DNA (r): at relatively low r values, NC-182 made the B-form structure rigid, and at higher r values, promoted the transition from B- to non-B-forms. NC-182 was also shown to promote the unwinding of Z-form DNA into B-form. Viscosity, UV 'melting' and circular dichroism experiments further showed that: (1) NC-182 intercalates to stabilize the DNA double helix structure; (2) NC-182 intercalates into the poly(dA) 2poly(dT) DNA structure to stabilize the triple helix structure, resulting in a melting point close to that of the double helix structure; the melting curves of the triple helix and double helix structures overlap at r > 0.06. These observations make an important contribution to our understanding of the biological properties of this novel benzo[a]phenazine derivative, which is a new antitumor agent suitable for both multiagent-resistant and sensitive tumors.
The most prominent mechanism of action of kinase inhibitors is their competition with ATP by binding to the hinge region of the kinase protein. Once the kinase is blocked by an inhibitor, it loses the ability to transfer phosphate groups from ATP to other molecules, resulting in the loss of kinase activity.
The hinge-binding region of kinase inhibitors mimics the interaction pattern between the ATP nucleobase and the kinase. MCE extracted thousands of kinase inhibitors from the ChEMBL database and isolated their molecular fragments. In certain cases, the amino and amide groups on the molecular fragments are crucial for binding in the hinge region. Therefore, we enhanced the diversity of the collected results by adding these two groups to unoccupied positions on the ring system. Subsequently, the fragments were assessed for their hinge region binding ability via docking at distinct kinases, we also applied pharmacophore constraints to ensure interactions with key amino acids in the kinase hinge region, ultimately obtaining kinase-related molecular fragments.
MCE provides over 10,000 kinase fragment molecules that meet the above requirements and are available off the shelf, serving as an effective tool for screening and developing drugs targeting kinases.
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.
MCE carefully prepared a unique collection of 43 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.
Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).
MCE carefully prepared a unique collection of 55 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.
N-Methylmesoporphyrin IX (NMM), a widely used G-quadruplex DNA specific fluorescent binder, is an efficient probe for monitoring Aβ fibrillation. N-Methylmesoporphyrin IX is an in situ inhibitor and an ex situ monitor for Aβ amyloidogenesis both in vitro and in cells. N-Methylmesoporphyrin IX is sensitive to G-quadruplexes DNA but has no response to duplexes, triplexes and single-stranded forms DNA. N-Methylmesoporphyrin IX is nonfluorescent alone or in monomeric Aβ environments, but emits strong fluorescence through stacking with the Aβ assemblies .
Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
Permanent Orange (Standard) is the analytical standard of Permanent Orange. This product is intended for research and analytical applications. Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
Dextrins are a group of low molecular weight carbohydrates produced by the hydrolysis of starch. Dextrin is commonly used as a thickener, stabilizer or binder in a variety of foods including baked goods, beverages and confectionary. In addition, it is used in the production of adhesives, paper and textiles. Its unique chemical properties make it an important ingredient in a variety of industrial processes, especially in construction and packaging.
Calcium acetate, United States Pharmacopeia (USP) Reference Standard (Calcium acetate (Pharmaceutical primary standard, USP)), a phosphate binder that can reduce phosphorus content, United States Pharmacopeia (USP) reference standard .
Starch (from corn) is a carbohydrate extracted from the kernel of the corn plant. It contains two main components, namely amylose and amylopectin. Starches from corn have various applications in the food industry as thickeners, stabilizers and binders. It is commonly used in the production of products such as baked goods, snacks, sauces and soups. In addition, it can be used as a raw material for the production of biofuels and bioplastics.
Luviquat FC 550 is a cationic polymer commonly used in a variety of personal care and cosmetics. It is a viscous liquid containing quaternary ammonium groups which give it a positive charge. Luviquat FC 550 has a variety of properties suitable for these applications including its ability to provide conditioning, antistatic and film-forming properties to hair and skin. In addition, it is used as a binder in oral care products and as a flocculant in industrial water treatment.
1,4-Anhydro-D-xylitol is a compound belonging to the class of sugar alcohols. It is derived from xylitol, a natural sweetener found in many fruits and vegetables. 1,4-Anhydro-D-xylitol is commonly used as a low-calorie sweetener and excipient in the food and pharmaceutical industries, and as a filler or binder in pharmaceutical formulations. It has also been investigated for its potential use in the development of biodegradable plastics and other sustainable materials.
3,5,7-Trihydroxychromone is the analogue of galangin. 3,5,7-Trihydroxychromone is also the binder of bovine serum albumin. 3,5,7-Trihydroxychromone undergoes multiple antioxidant pathways .
Netropsin dihydrochloride is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei . Netropsin dihydrochloride exhibits antiviral activity against the vaccinia virus .
Distamycin A (NSC-82150), an oligopeptide antibiotic, is a minor groove binder which binds to B-form DNA, preferentially at A/T rich sites.Distamycin A can change Enediyne-induced DNA cleavage sites and enhances apoptosis .
The ARL2BP protein cooperates with ARL2 to play a crucial role in the nuclear translocation, retention, and transcriptional activity of STAT3, highlighting its cellular involvement. As a potential effector of ARL2, ARL2BP forms a complex with ARL2, SLC25A6, and ARL3. ARL2BP Protein, Human (His) is the recombinant human-derived ARL2BP protein, expressed by E. coli , with N-6*His labeled tag.
MOB-Like Protein Phocein; 2C4D; Class II mMOB1; Mob1 Homolog 3; Mob3; Mps One binder Kinase Activator-Like 3; Preimplantation Protein 3; MOB4; MOB3; MOBKL3; PHOCN; PREI3
The MOB4 protein may be involved in membrane trafficking, specifically the membrane budding reaction, highlighting its role in vesicle formation and trafficking.MOB4 interacts with STRN4, suggesting involvement in protein-protein interactions.MOB4 Protein, Human (His) is the recombinant human-derived MOB4 protein, expressed by E.coli , with N-6*His labeled tag.
The TCN1 protein is critical for mitochondrial processes and binds to the mitochondrial light chain promoter to regulate mitochondrial transcription. As a key component of the mitochondrial transcription initiation complex (including TFB2M and POLRMT), TCN1 plays a crucial role in the basal transcription of mitochondrial DNA. TCN1 Protein, Human (P.pastoris, His) is the recombinant human-derived TCN1 protein, expressed by P. pastoris , with N-His labeled tag. The total length of TCN1 Protein, Human (P.pastoris, His) is 410 a.a., with molecular weight of ~47.6 kDa.
The ARL2BP protein cooperates with ARL2 to play a crucial role in the nuclear translocation, retention, and transcriptional activity of STAT3, highlighting its cellular involvement. As a potential effector of ARL2, ARL2BP forms a complex with ARL2, SLC25A6, and ARL3. ARL2BP Protein, Human (GST) is the recombinant human-derived ARL2BP protein, expressed by E. coli , with N-GST labeled tag.
In the Hippo signaling pathway, MOB1A acts as an important activator to control organ size and suppress tumors by regulating proliferation and apoptosis. MOB1A participates in the kinase cascade together with STK3/MST2 and STK4/MST1 to phosphorylate and activate LATS1/2, thereby affecting YAP1 oncoprotein and WWTR1/TAZ. MOB1A Protein, Human (His) is the recombinant human-derived MOB1A protein, expressed by E. coli , with C-6*His labeled tag.
Lurbinectedin-d3 is deuterium labeled Lurbinectedin. Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively[1].
Vapendavir-d5 is the deuterium labeled Vapendavir. Vapendavir (BTA798) is a potent enteroviral capsid binder (CB). Vapendavir (BTA798) possesses potent antiviral activity for enterovirus 71 (EV71) replication, with EC50 values of 0.5-1.4 μM in different EV71 strains .
GAB1; GRB2-associated-binding protein 1; GRB2-associated binder 1; Growth factor receptor bound protein 2-associated protein 1
WB, IHC-P, IHC-F, ICC/IF, ELISA
Human, Mouse, Rat
Phospho-GAB1 (Tyr627) Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 77 kDa, targeting to Phospho-GAB1 (Tyr627). It can be used for WB、IHC-P、IHC-F、ICC、IF、ELISA assays with tag free, in the background of Human, Mouse and Rat.
Croscarmellose sodium is a commonly used pharmaceutical additive approved by the US Food and Drug Administration (FDA). Croscarmellose sodium is used in injectable preparations as a suspending agent to promote solubilization of compounds with poor water solubility. Croscarmellose sodium is also present in tablets as binder, glidant and antiadherent, in bulk laxatives as active principle and as an additive in food products. Croscarmellose sodium can be used as an excipient, such as excipients, disintegrants, aids in disintegration. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Starch (from corn) is a carbohydrate extracted from the kernel of the corn plant. It contains two main components, namely amylose and amylopectin. Starches from corn have various applications in the food industry as thickeners, stabilizers and binders. It is commonly used in the production of products such as baked goods, snacks, sauces and soups. In addition, it can be used as a raw material for the production of biofuels and bioplastics.
Starch pregelatinized can be used as an excipient, such as Glidants, diluents, disintegrants, binders, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Aluminum magnesium silicate can be used as an excipient, such as adsorbent, stabilizer, suspending agent, disintegrant for tablet and capsule, binder for tablet, thickener. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer copolymer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer homopolymer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
Carbomer interpolymer can be used as an excipient, such as Bioadhesives, emulsifiers, release modifiers, suspending agents, tablet binders, viscosity enhancers, etc. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
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