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NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism .
(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011), a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemoresearch of drug-resistant hepatocellular carcinoma.
AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate .
Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
Phyllalbine is an alkaloid compound found in the roots of Convolvulus subhirsutus, exhibiting both central and peripheral sympathomimetic effects, making it a promising candidate for neurological disease research .
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders .
Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent .
PPO-IN-4 (compond 2i) is a potent Protoporphyrinogen oxidase (PPO) inhibitor. PPO-IN-4 can be used as a candidate herbicide for wheat, corn, and paddy fields .
Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents .
Vanin-1-IN-4 (compound (S)-1) is vanin-1 inhibitor with a chiral methyl substituent, with profils as potent drug-candidate but exist as an amorphous solid .
EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC .
ADPM06, a lead candidate azadipyrromethene, is a novel nonporphyrin photodynamic therapeutic (PDT) agent. ADPM06 exhibits IC50 values in the micro-molar range in human tumor cells and induces apoptosis .
Iboxamycin is a potent antibioticcandidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice .
Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .
PYR14-TFSI is a room temperature ionic liquid (RTIL) with a wide electrochemical window (5.5V) and a high viscosity, making it a useful candidate for electrochemical energy applications .
Antimicrobial photosensitizer-1 is a promising candidate as the antimicrobial photosensitizer for combating pathogenic microorganism infections. Antimicrobial photosensitizer-1 exhibits an impressive antimicrobial efficacy in S. aureus-infected mice wounds .
Amitifadine (DOV-21947) is an antidepressant drug candidate that functions as a triple reuptake inhibitor, targeting the reuptake of serotonin, norepinephrine, and dopamine, and has been shown to decrease binge drinking and alleviate negative emotions in animal models.
SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer .
MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 of 1.9±0.5 nM. MAO-B-IN-28 can be used as a candidate for neurodegenerative diseases research .
Sophoridine is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting agent candidate for treating cryptosporidiosis.
TAK-218 is a promising candidate as an agent tor central nervous system trauma and ischemia. TAK-218 exhibits potent scavenging activity and antioxidative activity. TAK-218 also inhibits dopamine release .
Rehmannic acid (lantadene A) is a compound isolated from Lantana camara. Rehmannic acid shows considerable in vitro antioxidant, free radical scavenging capacity activities in a dose dependant manner. Rehmannic acid is a promising candidate for use as an antioxidant and hepatoprotective agent .
GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation .
Cinnabarin is an antibiotic which can be extracted from Polystiotus cinnabarinus, P. versicolo and Trametes cinnabarinus. Cinnabarin exhibits antibacterial activity against Gram-positive bacteria as well as antiviral activity, making it a potential candidate for infectious disease research .
BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC50s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy .
Tracheloside (Standard) is the analytical standard of Tracheloside. This product is intended for research and analytical applications. Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
Antitumor photosensitizer-2 (Compound 11) is a potent photosensitizer. Antitumor photosensitizer-2 has outstanding photodynamic anti-tumor effects without obvious skin photo-toxicity, and can act as new agent candidates for photodynamic research .
Antitumor photosensitizer-1 (Compound 8) is a potent photosensitizer. Antitumor photosensitizer-1 has outstanding photodynamic anti-tumor effects without obvious skin photo-toxicity, and can act as new agent candidates for photodynamic research .
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .
sEH inhibitor-20 is an orally active and metabolically stable sEH inhibitor (IC50: 0.2 nM). sEH inhibitor-20 has significant analgesic and anti-inflammatory activities and is expected to become a potential candidate compound for the study of neuropathic pain .
Dihydrokaempferol (Standard) is the analytical standard of Dihydrokaempferol. This product is intended for research and analytical applications. Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents .
HN37 as a potent and chemically stable antiepileptic agent candidate, with an EC50 of 37 nM for KCNQ2 . HN37 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
H3B10-27(13/17αF) is an excellent scaffold for further developing reagent candidates and an important tool for understanding the physiological functions of the neuropeptide G protein-coupled receptor RXFP3, and it's very stable in serum .
Cariprazine hydrochloride is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Antibacterial agent 249 demonstrates broad-spectrum antimicrobial properties, effectively inhibiting the growth of Aspergillus niger, Bacillus subtilis, Pseudomonas albicans, Escherichia coli, and Staphylococcus aureus, while also exhibiting anti-inflammatory activity in vitro, making it a potential candidate for treating bacterial infections.
Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
M2e, human, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A, which is a valid and versatile vaccine candidate to protect against any strain of human influenza A .
Cyclobenzaprine b-D-glucuronide is a metabolite of Cyclobenzaprine. Cyclobenzaprine b-D-glucuronide can be used to treat diseases associated with coronavirus infection. Cyclobenzaprine b-D-glucuronide can be used to study the metabolic pathways of Cyclobenzaprine in the body and as a potential candidate for studying coronavirus treatment .
DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic agent (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin .
Tetradecanedioic acid-d24 is the deuterium labeled Tetradecanedioic acid . Tetradecanedioic acid is an endogenous metabolite and belongs to the class of organic compounds known as long-chain fatty acids. Tetradecanedioic acid can act as a candidate biomarker for organic anion-transporting polypeptide mediated agent-agent interactions .
KDU731, an orally active C. parvumPI4K inhibitor with an IC50 value of 25 nM, blocks Cryptosporidium infection in vitro and in vivo . KDU731 is a promising agent candidate for the treatment of diarrhea caused by Cryptosporidium and meets a broad range of safety .
2-Fluoropalmitic acid, an acyl-CoA synthetase inhibitor, acts as a candidate anti-glioma agent. 2-Fluoropalmitic acid suppresses the viability and stem-like phenotype of glioma stem cells (GSCs). 2-Fluoropalmitic acid also inhibits proliferation and invasion of glioma cell lines .
FAUC 3019 is a partial agonist of dopamine D(4) receptors and has the activity of promoting penile erection. FAUC 3019 has a strong stimulatory effect on penile erection in male rats at low concentrations. The biological activity of FAUC 3019 makes it a promising compound candidate .
Erythrodiol (Standard) is the analytical standard of Erythrodiol. This product is intended for research and analytical applications. Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .
PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget agent candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD agent development .
Gly-β-MCA (Standard) is the analytical standard of Gly-β-MCA. This product is intended for research and analytical applications. Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders[1].
Desmethyl cariprazine is an active metabolite of Cariprazine . Cariprazine, an antipsychotic agent candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM) .
d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
Sophoridine (Standard) is the analytical standard of Sophoridine. This product is intended for research and analytical applications. Sophoridine is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
LASSBio-1985 is an NHLd inhibitor (nucleoside hydrolase from Leishmania donovani), with a Ki of 79 μM and an IC50 of 84.6 μM. LASSBio-1985 exhibits selective toxicity against Leishmania parasites, with no toxicity to mammalian cells, making it a promising candidate for research in the field of anti-infective therapies .
I-BET567 is a potent and orally active inhibitor of pan-BETcandidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation .
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
M2e, human TFA, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A. M2e, human TFA is a valid and versatile vaccine candidate to protect against any strain of human influenza A .
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310) . Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
hMAO-B-IN-3 (Compound 15) is a potent inhibitor of hMAO-B with an IC50 of 47.4 nM. hMAO-B-IN-3 is playing favourable agent-like properties and a broad safety window. hMAO-B-IN-3 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands .
BAR-072 is a small-molecule inhibitor targeting TraE, with a KD of 2.7 µM. It significantly inhibits the transfer of the antibiotic resistance-associated plasmid pKM101. BAR-072 shows promise as a candidate compound for blocking the spread of bacterial resistance genes and holds potential for research in infectious disease and antimicrobial resistance control .
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
5-Methyl-2-thiophenecarboxaldehyde (Standard) is the analytical standard of 5-Methyl-2-thiophenecarboxaldehyde. This product is intended for research and analytical applications. 5-Methyl-2-thiophenecarboxaldehyde acts as a candidate to microscopic third order non-linear optical (NLO) material[1].
NSC-79887 is a nucleoside hydrolase (NH) inhibitor with activity against Bacillus anthracis. NSC-79887 is considered a good candidate inhibitor of nucleoside hydrolases for biological testing and further development. The pharmacokinetic (ADMET) prediction of NSC-79887 showed that all physicochemical parameters were within the acceptable range for human use .
USP7-IN-16 (Compound 61) is a selective USP7 inhibitor with IC50 values of 5.5 nM in the FLINT assay and 2.1 nM in MM.1S cells. USP7-IN-16 exhibits antitumor activity in mice and is a promising candidate for research in the field of oncology .
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic agent candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor .
GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM .
YIAD-0205 is an orally available Aβ(1?42) aggregation inhibitor. YIAD-0205 demonstrated in vivo efficacy in an AD transgenic mouse model with five familial AD mutations (5XFAD) .
Sanazole (AK-2123) is a hypoxic cell radiosensitizer. Sanazole enhances radiation-induced DNA strand breaks. In mouse fibroblast tumors, Sanazole increases nuclear condensation and fragmentation, as well as elevates caspase-3 activity, thereby enhancing radiation-induced apoptosis. These characteristics make Sanazole a promising candidate for research in tumor therapy .
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion .
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
mTOR inhibitor-26 (Compound HPT-11) is an inhibitor of mTOR with an IC50 of 0.7 nM. It effectively inhibits the proliferation of AML cell lines Molm-13 and MV-4-11. mTOR inhibitor-26 exhibits antitumor activity and favorable metabolic stability, making it a promising candidate for cancer research .
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Chitinase-IN-6 (Compound 4h) is a potent dual-Chitinase inhibitor, with Ki values of 1.82 and 2.00 μM against OfChtI and OfChi-h, respectively. Chitinase-IN-6 exhibits certain growth inhibition effects against Ostrinia furnacalis. Chitinase-IN-6 is a potential novel insecticide candidate friendly to nontarget organisms .
Naphthacene (Benz[b]anthracene) is a fused polycyclic aromatic compound exhibiting an electron field-effect mobility of approximately 10 cm2/Vs; it is an ethylnylated acene that functions as a conducting polymer, making it suitable for use as a donor material. Its exceptional photoluminescence and quantum yield position naphthacene as a highly promising candidate for the advancement of single crystal electronic materials.
TLK1-IN-1 (Compound 5n) is a TLK1 inhibitor with an IC50 of 7.2 μM against TLK1B and a GI50 of 2.7 μM in LNCaP cells. TLK1-IN-1 induces DNA damage and apoptosis in cancer cells, making it a potential candidate for prostate cancer research .
DBIBB is a specific nonlipid agonist of the type 2 G protein coupled receptor for lysophosphatidic acid (LPA2). DBIBB mitigates the gastrointestinal radiation syndrome, increases intestinal crypt survival and enterocyte proliferation, and reduces apoptosis. DBIBB represents a agent candidate capable of mitigating acute radiation syndrome caused by high-dose γ-radiation to the hematopoietic and gastrointestinal system .
Cariprazine (Standard) is the analytical standard of Cariprazine. This product is intended for research and analytical applications. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
OfChi-h-IN-1 is a potent OfChi-h inhibitor with a Ki value of 0.33 μM. OfChi-h-IN-1 dramatically inhibit the growth and development of Ostrinia nubilalis larvae, and it shows higher insecticidal activity than Hexaflumuron (HY-B1848). OfChi-h-IN-1 serves as novel candidates for insect growth regulator .
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
CH401 peptide is a HER2-derived antigen peptide. After being bound to the artificial viral capsid by a self-assembled β-cyclic peptide, CH401 peptide is encapsulated in a lipid bilayer containing the lipid adjuvant α-GalCer, and can be studied as a self-adjuvant anti-breast cancer vaccine candidate .
HSV-1-IN-1 (compound 1b) is a drug candidate for herpes simplex virus HSV-1(IC50=0.5 nM) and HSV-2(IC50=16 nM) infection. HSV-1-IN-1 inhibits the helicase-primase complex to prevent viral replication, thereby inhibiting HSV infection .
GSK812397 is a CXCR4 antagonist with potential for the treatment of HIV infection. To evaluate the clinical potential of GSK812397, kilogram-scale agent candidates are needed. Here, an improved, scalable synthetic route for the CXCR4 antagonist GSK812397 is described. This new route has been scaled up in a 50-liter stationary facility to obtain 1.2 kg of agent substance in 20% overall yield and >99% chemical and enantiomeric purity in five steps. CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein that functions in part as a host co-receptor for multiple strains of HIV-1. It is thought that targeting CXCR4 will help inhibit the replication of several late cytopathic viruses; therefore, CXCR4 antagonists are one of the most promising new classes of experimental anti-HIV agents. GSK812397 is a potent CXCR4 antagonist and is therefore a candidate for investigation for the treatment of HIV infection.
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 .
Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC50 value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .
NLRP3-IN-33 (Compound 12o) is a blood-brain barrier permeable inhibitor of AChE and BChE, with IC50 values of 1.02 μM and 7.03 μM against hAChE and hBChE respectively. NLRP3-IN-33 possesses antioxidant, anti-inflammatory, and metal chelating activities, making it a potential candidate for research in Alzheimer's disease (AD) .
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
(4-(Bromomethyl)phenyl)(4-(prop-2-yn-1-yloxy)phenyl)methanone is a compound with anticancer activity that can effectively inhibit the growth of tumor cells and shows potential application value in compound development. The compound has also been studied for the improvement of certain neuropathological conditions and as a candidate compound for anti-inflammatory inhibition.
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases .
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
N-Formylfortimicin A (SF-1854) is an aminoglycoside antibiotic with broad-spectrum antibacterial activity. It primarily acts on bacterial ribosomes to inhibit protein synthesis and exhibits notable inhibitory effects against various Gram-positive and Gram-negative bacteria (e.g., E. coli with a MIC of 12.5-50 μg/mL), making it a potential candidate for research on bacterial infection-related diseases .
AMPA-IN-2 is an orally active AMPA inhibitor that can cross the blood-brain barrier. AMPA-IN-2 improves epileptic seizures by inhibiting the intrinsic excitability of neurons and inhibiting the excitability of glutamatergic transmission. AMPA-IN-2 exerts anti-epileptic effects in the pentylenetetrazol (PTZ) model and can be used as a promising candidates with high broad-spectrum anti-epileptic potential .
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones .
HPV16-E711-20 epitope is a well-known HLA-A *0201-restricted human cytotoxic T lymphocyte (CTL) epitope of the HPV16 E7 protein that shows high-affinity binding to HLA-A2 in vitro. HPV16 CTL epitopes may be good candidates for the development of an effective peptide-based antitumor vaccine .
Casein kinase 1δ-IN-6 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 23 nM. Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory properties both in vitro and in vivo. Casein kinase 1δ-IN-6 is a promising drug candidate and can be used for neurodegenerative diseases research.
(Rac)-DNDI-8219 is an antituberculosis compound with potent anti-leishmanial activity. (Rac)-DNDI-8219 demonstrated superior efficacy in the Leishmania donovani mouse model. (Rac)-DNDI-8219 showed promising activity in the Leishmania infantum hamster model. (Rac)-DNDI-8219 candidate compound R-6 provided excellent oral efficacy in the same hamster model .
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
Acridine-9-carboxaldehyde (Acridine-9-carbaldehyde) is a bioactive compound with potential antibacterial and antitumor activities. Acridine-9-carboxaldehyde is widely used as a building block in compound development to synthesize various bioactive derivatives. Acridine-9-carboxaldehyde exhibits significant cytotoxicity against certain cancer cells, making it an important candidate in cancer inhibition research.
Dodecanedioyl dichloride, Dodecanedioyl dichloride is commonly used in organic synthesis as a general building block for the preparation of various polymers and plastics, including nylon 12 and polyester resins, it can be used to introduce acid chloride groups into other organic molecules, which can then be further reaction to form more complex compounds, moreover, it has been used in medicinal chemistry as a starting material for the synthesis of various drugs and drug candidates.
N-Acetyl-D-mannosamine (ManNAc) is an oral active sialic acid precursor that can prevent hypertension by increasing sialylation of IgG, making it a promising candidate for cardiovascular disease research. Additionally, N-Acetyl-D-mannosamine can activate hypocretin (HCRT) gene expression in orexin neurons and improve neurodegeneration caused by aging, offering potential avenues for research in neurological disorders .
Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitory activity against both wild-type and mutated target enzymes.
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .
VU0415374 is a positive allosteric modulator that modulates mGlu4 receptor activity. VU0415374 could help achieve precise light control of physiological responses. VU0415374 has high selectivity and can be used to further study the role of mGlu4 in co-expression of other mGlu receptor systems. The improved properties of VU0415374 make it an important candidate for studying mGlu4 with high precision in space and time .
URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout .
Fluorescent DOTAP (NBD-DOTAP) is a cationic lipid which can be used for nucleic acid and protein delivery. Fluorescent DOTAP is labeled with a fluorophore NBD (maximum excitation/emission wavelength ∼463/536 nm). Fluorescent DOTAP can be used for gene delivery systems, drug delivery, as well as cell imaging and nanocarrier tracking. Fluorescent DOTAP is an ideal candidate for both biological and pharmaceutical formulation (e.g. co-delivery of vaccines) research .
β-Amyrin shows effectively counteract amyloid β (Aβ)-induced impairment of long-term potentiation (LTP). β-Amyrin is a promising candidate for Alzheimer's disease (AD) research. β-Amyrin exhibits anti-inflammatory effects, protective activity against pulmonary fibrosis, and notable antibacterial capabilities. β-Amyrin is an orally active natural triterpenoid compound .
EIDD-2749 (4'-Fluorouridine) is an orally active RdRp inhibitor. EIDD-2749 effectively blocks the replication of RSV and SARS-CoV-2. EIDD-2749 also exhibits activity against HCV and lymphocytic choriomeningitis virus (LCMV). EIDD-2749 is a promising oral therapeutic candidate for COVID-19 and is also suitable for research on other RNA viruses .
Cariprazine-d8-1 (RGH-188-d8-1) is the deuterium labeled Cariprazine (HY-14763). Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Emoquine-1 is an orally active and potent antimalarial drug. Emoquine-1 is efficient against multidrug-resistant Plasmodium parasites, including the Artemisinin-resistant quiescent stage. Emoquine-1 is active against proliferative P. falciparum with IC50 values of 20-55 nM. Emoquine-1 is a candidate to fight Plasmodium parasites resistant to artemisinin-based combination therapies (ACTs) with a capacity to eliminate persistent parasites .
PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .
KSK-104 has potent antibacterial activity against Mycobacterium tuberculosis (MIC=0.78 μM). The role of KSK-104 is mainly involved in the synthesis and recovery pathways of pyridoxal 5'-phosphate (PLP), PLP-dependent enzymes and oxidative stress networks. KSK-104, as a candidate molecule for novel anti-tuberculosis drugs, can be used to develop research against drug-resistant mycobacterium tuberculosis .
β-Amyrin shows effectively counteract amyloid β (Aβ)-induced impairment of long-term potentiation (LTP). β-Amyrin is a promising candidate for Alzheimer's disease (AD) research. β-Amyrin exhibits anti-inflammatory effects, protective activity against pulmonary fibrosis, and notable antibacterial capabilities. β-Amyrin is an orally active natural triterpenoid compound .
The Tubulysin family of secondary metabolites was originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizers and anti-microtubule toxins (anti-microtubule toxins), with effective IC50 concentrations against multidrug-resistant cancer cell lines. In the picomole range. Tubulysins are ideal candidates for incorporation into small active molecule conjugate (SMDC) delivery systems and are commonly used in ADC synthesis as ADC cytotoxins (ADC Cytotoxin) .
Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
Zgwatinib (SOMG-833) is a potent, selective, and ATP-competitive c-MET inhibitor, with an IC50 of 0.93 nM against c-MET, over 10,000-fold more potent compared with 19 tyrosine kinases (including c-MET family members and highly homologous kinases). Zgwatinib potently inhibits c-MET-driven cell proliferation. Zgwatinib as a potential candidate agent for c-MET-driven human cancers research .
Tropolone is a seven-membered non-benzenoid aromatic compound, which is the precursor of many Azulene derivatives. Tropolone is a potent mushroom tyrosinase inhibitor with an IC50 value of 0.4 μM. Its inhibitory effect can be achieved by dialysis or excess CU 2+ Reversa. Tropolone exhibits broad anti-viral and anti-fungal activity and is synergistic upon co-treatment with nucleos(t)ide analog drugs. Tropolone is a promising candidate for research in osteosarcoma .
MU1409 is an inhibitor of MRE11 nuclease with an IC50 of 12.1 μM. Additionally, MU1409 also inhibits FEN1 and EXO1, with IC50 values of 24.2 and 176.4 μM, respectively. MU1409 affects DNA repair in cells, preventing the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for research on BRCA2 mutation-induced cancers .
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
Antibacterial agent 119 (Compound 21 g) is an antibacterial candidate against Methicillin (HY-121544)-resistant Staphylococcus aureus (MICs less than 1 μg/mL against tested strains). Antibacterial agent 119 induces ROS production. Antibacterial agent 119 also acts on the bacterial cell membrane to cause membrane breakage. Antibacterial agent 119 exhibits potent antibacterial activity with low cytotoxicity, rapid bactericidal ability, and good in vivo antibacterial activity .
Verubulin (hydrochloride) (Standard) is the analytical standard of Verubulin (hydrochloride). This product is intended for research and analytical applications. Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer .
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
Ziyuglycoside I (Standard) is the analytical standard of Ziyuglycoside I. This product is intended for research and analytical applications. Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
PDE5-IN-6c is a potent and selective phosphodiesterase 5A1 (PDE5A1) inhibitor with the potential to inhibit Alzheimer's disease (AD). PDE5-IN-6c exhibits an excellent in vitro IC50 (0.056 nM), demonstrating its potent inhibitory activity. PDE5-IN-6c has improved water solubility, making it a more attractive drug candidate .
TAT-NEP1-40 acetate is a therapeutic candidate for axonal regeneration and functional recovery after stroke. TAT-NEP1-40 acetate can protect PC12 cells against oxygen and glucose deprivation (OGD) and promote neurite outgrowth. TAT-NEP1-40 acetate protects the brain against ischemia/reperfusion injury through inhibition of neuronal apoptosis. TAT-NEP1-40 acetate can be efficiently delivered into the rat brains .
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .
ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer .
3β,15α-Dihydroxy-7,11,23-trioxo-lanost-8-dien-26-oic acid is a triterpene compound that can be found in Ganoderma lucidum, and it inhibits nitric oxide (NO) production in BV-2 microglial cells induced by lipopolysaccharide (LPS, HY-D1056), with an IC50 of 6.50 μM, making it a potential candidate for anti-inflammatory research .
APA-H-MPO hydrochloride is an inhibitor of PCAF bromodomain/Tat-AcK50 interaction with potential for anti-HIV/AIDS. APA-H-MPO hydrochloride can effectively inhibit the binding of PCAF bromodomain to Tat-AcK50. APA-H-MPO hydrochloride showed low cytotoxicity in preliminary cell studies. APA-H-MPO hydrochloride is considered a potential candidate for a promising inhibitory strategy targeting the host cell protein PCAF BRD to block HIV replication .
CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer .
αGalCer-RBD is a self-adjuvanting lipoprotein conjugate. αGalCer-RBD induces potent immunity against SARS-CoV-2 and its variants of concern. αGalCer-RBD conjugate induces RBD-specific, cytokine-producing T cell development. αGalCer-RBD has great potential to be an effective COVID-19 vaccine candidate. α-Galactosylceramide (αGalCer) is a potent invariant natural killer T cell (iNKT) agonist . RBD: receptor-binding domain
UK-1745 is a cardiotonic agent with vasodilating and antiarrhythmic properties. It increases intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes by inhibiting phosphodiesterase III, thereby enhancing myocardial contractility. Additionally, UK-1745 exhibits β-adrenergic receptor blocking activity, which helps reduce the oxygen consumption of the heart and prevent calcium overload. These characteristics make UK-1745 a promising candidate for research in congestive heart failure .
Flaviviruses-IN-1 is an inhibitor of several viruses belonging to the Flaviviridae family, with activity to inhibit viral infection. Flaviviruses-IN-1 is able to specifically inhibit multiple viruses of the Flaviviridae family. The mechanism of action of Flaviviruses-IN-1 is related to the modulation of the host cell immune response to viral infection. Flaviviruses-IN-1 was identified as a potential candidate compound in a high-throughput screening. Flaviviruses-IN-1 provides a new strategy for inhibiting infections caused by the Flaviviridae family .
PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active .
RC-33 hydrochloride is a selective and metabolically stable σ receptor agonist with activity in enhancing nerve growth factor (NGF)-induced neurite outgrowth. Both enantiomers of RC-33 hydrochloride bind to the σ receptor with similar affinity and show almost equal effectiveness as σ receptor agonists. The R-configured enantiomer of RC-33 hydrochloride shows higher liver metabolic stability in the presence of NADPH. RC-33 hydrochloride was selected as the best candidate for further in vivo studies in animal models of amyotrophic lateral sclerosis .
Caprospinol (SP-233) is a steroid compound candidate based on the structure of 22R-hydroxycholesterol. It has multiple mechanisms of neuroprotection, including binding to β-amyloid protein (Aβ(42)), interacting with the mitochondrial respiratory chain, clearing Aβ(42) monomers, and acting as a σ-1 receptor ligand. It can cross the blood-brain barrier in vivo and restore cognitive impairment, and has the potential to inhibit Alzheimer's disease.
Cucurbit[7]uril is a cyclic organic molecule consisting of seven glycoluril units linked by methylene bridges. It has a rigid barrel-like structure with two identical inlets at both ends to selectively encapsulate guest molecules of appropriate size, shape, and polarity. Cucurbit[7]uril is known for its high binding affinity for a variety of organic and inorganic guests, including drugs, amino acids, peptides, and metal ions. This property makes them promising candidates for various applications in areas such as drug delivery, catalysis, and sensing.
Aidioxa has the ability to improve delayed gastric emptying in rats. It can partially improve delayed gastric emptying caused by clonidine or restraint stress. The allyltoin part of Aidioxa restores gastric emptying activity by antagonizing α-2 adrenergic receptors. Its aluminum hydroxide part is involved in restoring gastric compliance. Aidioxa can improve both delayed gastric emptying and impaired gastric compliance, both of which play an important role in functional dyspepsia (FD). Aidioxa is a candidate agent for inhibiting FD.
YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focal adhesion kinase (FAK) and Src. YF-452 is a potential antiangiogenic agent candidate for cancer research .
Hexetidine (NSC-17764) is an orally active antibacterial and antifungal agent with broad antibacterial and antifungal activity. Hexetidine combined with IPBC potentiates strong fungal growth inhibition properties. Hexetidine at concentrations greater than 0.1% can cause oral ulceration. Additionally, Hexetidine improves its plaque inhibiting activities combined with zinc and has been confirmed the effectiveness on purulent wound along with ultrasound. Hexetidine is a promising candidate for research in fungus-related diseases and soft tissue purulent-inflammatory
Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
(Rac)-AB-423 (DVR-23) is an anti-HBV candidate compound with promising anti-HBV activity. (Rac)-AB-423 showed no induction of CYP1A2, CYP3A4, or CYP2B6 enzyme activity at high concentrations. (Rac)-AB-423 exhibited desirable pharmacokinetic properties, enabling good systemic exposure and high oral bioavailability. (Rac)-AB-423 achieved more than 2 log viral load reduction in the hydrodynamic injection (HDI) HBV mouse model .
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
L-Methionine-DL-sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-DL-sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-DL-sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS) .
VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research .
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) .
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)) is a quorum-sensing molecule of Vibrio vulnificus that specifically interacts with RIG-I, inhibiting RIG-I polyubiquitination, suppressing IRF-3 activation, and reducing type I interferon production. Cyclo(Phe-Pro) enhances susceptibility to HCV and influenza virus and also alleviates plant aluminum toxicity stress. The mechanism of Cyclo(Phe-Pro) involves the regulation of host immune signaling pathways, bacterial virulence gene expression, and plant antioxidant systems, making it a promising candidate for research in viral infections, bacterial virulence regulation, and agricultural stress resistance .
BTPTT-4F (Y6) is a non-fullerene acceptor-donor-acceptor (A-D-A) type small molecular acceptor (SMA) characterized by its flexible alkyl chains and centrally fused ring structure. Featuring a ladder-type electron-deficient core, BTPTT-4F can be effectively blended with PM6, showcasing significant potential for enhancing the performance of organic photovoltaic applications. Its tailored optical properties and adjustable electronic energy levels contribute to improved thermal and photochemical stability, making it a promising candidate for next-generation high-performance organic solar cells.
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
Isoquercetin (Standard) is the analytical standard of Isoquercetin. This product is intended for research and analytical applications. Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
TPS1-IN-1 (Compound O1) is a highly potent and broad-spectrum TPS1 inhibitor. TPS1-IN-1 with IC50s of 14.73 μM for MoTPS1 (TPS1 of M oryzae) and 59.99 μM for BcTPS1 (TPS1 of B cinerea), respectively. TPS1-IN-1 exerts a broad-spectrum fungicidal effect by interfering with spore germination, appressorium formation, and turgor pressure accumulation of fungi. TPS1-IN-1 has good safety and has the potential to be a novel fungicide candidate compound .
Apoptosis inducer 34 (Compound 4) is a small molecule compound that induces apoptosis by directly activating the intrinsic apoptotic pathway. Apoptosis inducer 34 promotes Apaf-1 oligomerization to form mature apoptosomes, thereby activating caspase-9 and caspase-3. It significantly activates the apoptotic pathway in Jurkat cells by enhancing the cytochrome c-dependent apoptotic signaling pathway, inducing PARP cleavage and chromosomal DNA fragmentation. Furthermore, Apoptosis inducer 34 exhibits low toxicity to normal cells, demonstrating potential for selective targeting of cancer cells. Apoptosis inducer 34 is a promising candidate for studying cancer related to apoptotic pathways .
Rolofylline (Standard) is the analytical standard of Rolofylline. This product is intended for research and analytical applications. Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450) .
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
AY-4 (Compound AY-4) is an efficient PROTAC degrader targeting FTH1 (Kd = 3.17 nM). AY-4 effectively upregulates the levels of ferrous (Fe 2+) and ferric (Fe 3+) ions in cells. AY-4 is a potential anticancer candidate compound that regulates iron homeostasis through ferritin degradation and enhances the efficacy of existing drugs. AY-4 can effectively reduce the level of FTH1 in breast cancer cells (Pink: FTH1 ligand AY-2 (HY-174871); Blue: E3 ligand Pomalidomide (HY-10984); Black: Linker, Pomalidomide-PEG3-acid (HY-174872)) .
Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
ODE-Bn-PMEG is an antiviral compound with strong inhibitory activity against HPV-11, -16, and -18. ODE-Bn-PMEG effectively reduced transient amplification of viral DNA in transfected cells at concentrations well below its cytotoxic levels. ODE-Bn-PMEG showed increased uptake in human foreskin fibroblasts and was able to be efficiently converted to the active antiviral metabolite PMEG diphosphate in vitro. The P-chiral enantiomer of ODE-Bn-PMEG showed comparable antiviral activity, indicating its potential application against multiple HPV types. ODE-Bn-PMEG is a promising candidate for local inhibition of HPV-16, HPV-18, and other high-risk types .
Chalcones A-N-5 is a trihydroxy chalcone derivative compound. Chalcones A-N-5 doesn’t show cytotoxicity at the concentration lower than 100 µM (with IC50 > 1 mM), but has a significant effect on promoting cell proliferation. Chalcones A-N-5 potentially promotes neuronal cell growth in the damaged brain tissue. Chalcones A-N-5 also inhibits ferroptosis induced by RSL or erastin and reduces the lipid peroxidation levels induced by Aβ1-42 protein aggregation. Chalcones A-N-5 is a promising molecular skeleton candidate for further development of lead compound for in vivo test to research AD .
KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties .
Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the treatment of chronic liver disease .
Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD .
Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .
Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor .
Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .
XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases.
Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
BMVC4 is a G-quadruplex (G4) stabilizer of the human telomeric sequence d[AG3(T2AG3)3]. Screening by circular dichroism (CD) spectroscopy revealed that BMVC4 is more suitable as the core molecule of G4 stabilizers than BMVC. The results showed that BMVC4-12C and BMVC4-8C3O are better candidates for G4 stabilizers and are worthy of further study. A simple and rapid screening method based on Cu2+-induced G4 unfolding can be used to find better G4 stabilizers for potential anticancer applications. CD results showed that the trivalent cations of 9-substituted BMVC derivatives are more suitable as G4 stabilizers than the divalent cations of BMVC. In addition, by monitoring the disappearance of the 291 nm CD band of human telomeres after Cu2+ addition, it was found that the core molecule of G4 stabilizer BMVC4 has better stability.
With the aging population and increasing competitive pressures, neurodegenerative diseases of the central nervous system (CNS) have become a serious medical challenge in modern society, including Parkinson's disease, Alzheimer's disease, brain tumors, and multiple sclerosis.
The CNS MPO (Multi-Parameter Optimization) score is a widely recognized algorithm in medicinal chemistry. Developed by Pfizer, this method is based on an analysis of approved CNS drugs and their interior CNS drug candidates, establishing the CNS MPO rules. It incorporates six key physicochemical properties (ClogP, ClogD, MW, TPSA, HBD, and pKa) to prospectively optimize CNS drug attributes—such as high blood-brain barrier (BBB) permeability, low P-gp efflux liability, low metabolic clearance, and high safety—thereby improving the clinical success rate of CNS drug candidates.
The CNS MPO compound library is a collection of compounds with CNS MPO scores greater than 5, specifically designed for CNS drug discovery.
“BioDesign” approach incorporates key structural features of known pharmacologically relevant natural products (e.g. alkaloids and other secondary metabolites) into synthetically feasible medicinal chemistry scaffolds. In order to identify the privileged pharmacophores, ring systems and linkers, we have carried out statistical analysis of structural features of natural products, marketed drugs, and drug candidates.
Saturated, fused ring, spiro, and bridged systems with a tendency towards multiple chiral centers are highly privileged among natural products and marketed drugs yet these structures are very poorly represented in commercial libraries. This library addressed this market need by incorporating these privileged elements into the design of novel synthetic molecules with high molecular framework diversity, multiple stereogenic centers (≥2), and degree of saturation (Fsp3 > 0.5).
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 4,474 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
PYR14-TFSI is a room temperature ionic liquid (RTIL) with a wide electrochemical window (5.5V) and a high viscosity, making it a useful candidate for electrochemical energy applications .
Fluorescent DOTAP (NBD-DOTAP) is a cationic lipid which can be used for nucleic acid and protein delivery. Fluorescent DOTAP is labeled with a fluorophore NBD (maximum excitation/emission wavelength ∼463/536 nm). Fluorescent DOTAP can be used for gene delivery systems, drug delivery, as well as cell imaging and nanocarrier tracking. Fluorescent DOTAP is an ideal candidate for both biological and pharmaceutical formulation (e.g. co-delivery of vaccines) research .
Cucurbit[7]uril is a cyclic organic molecule consisting of seven glycoluril units linked by methylene bridges. It has a rigid barrel-like structure with two identical inlets at both ends to selectively encapsulate guest molecules of appropriate size, shape, and polarity. Cucurbit[7]uril is known for its high binding affinity for a variety of organic and inorganic guests, including drugs, amino acids, peptides, and metal ions. This property makes them promising candidates for various applications in areas such as drug delivery, catalysis, and sensing.
Dodecanedioyl dichloride, Dodecanedioyl dichloride is commonly used in organic synthesis as a general building block for the preparation of various polymers and plastics, including nylon 12 and polyester resins, it can be used to introduce acid chloride groups into other organic molecules, which can then be further reaction to form more complex compounds, moreover, it has been used in medicinal chemistry as a starting material for the synthesis of various drugs and drug candidates.
M2e, human TFA, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A. M2e, human TFA is a valid and versatile vaccine candidate to protect against any strain of human influenza A .
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer .
Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)) is a quorum-sensing molecule of Vibrio vulnificus that specifically interacts with RIG-I, inhibiting RIG-I polyubiquitination, suppressing IRF-3 activation, and reducing type I interferon production. Cyclo(Phe-Pro) enhances susceptibility to HCV and influenza virus and also alleviates plant aluminum toxicity stress. The mechanism of Cyclo(Phe-Pro) involves the regulation of host immune signaling pathways, bacterial virulence gene expression, and plant antioxidant systems, making it a promising candidate for research in viral infections, bacterial virulence regulation, and agricultural stress resistance .
H3B10-27(13/17αF) is an excellent scaffold for further developing reagent candidates and an important tool for understanding the physiological functions of the neuropeptide G protein-coupled receptor RXFP3, and it's very stable in serum .
CH401 peptide is a HER2-derived antigen peptide. After being bound to the artificial viral capsid by a self-assembled β-cyclic peptide, CH401 peptide is encapsulated in a lipid bilayer containing the lipid adjuvant α-GalCer, and can be studied as a self-adjuvant anti-breast cancer vaccine candidate .
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
HPV16-E711-20 epitope is a well-known HLA-A *0201-restricted human cytotoxic T lymphocyte (CTL) epitope of the HPV16 E7 protein that shows high-affinity binding to HLA-A2 in vitro. HPV16 CTL epitopes may be good candidates for the development of an effective peptide-based antitumor vaccine .
TAT-NEP1-40 acetate is a therapeutic candidate for axonal regeneration and functional recovery after stroke. TAT-NEP1-40 acetate can protect PC12 cells against oxygen and glucose deprivation (OGD) and promote neurite outgrowth. TAT-NEP1-40 acetate protects the brain against ischemia/reperfusion injury through inhibition of neuronal apoptosis. TAT-NEP1-40 acetate can be efficiently delivered into the rat brains .
CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser 216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer .
Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent .
Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents .
Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .
Sophoridine is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
Rehmannic acid (lantadene A) is a compound isolated from Lantana camara. Rehmannic acid shows considerable in vitro antioxidant, free radical scavenging capacity activities in a dose dependant manner. Rehmannic acid is a promising candidate for use as an antioxidant and hepatoprotective agent .
Phyllalbine is an alkaloid compound found in the roots of Convolvulus subhirsutus, exhibiting both central and peripheral sympathomimetic effects, making it a promising candidate for neurological disease research .
Cinnabarin is an antibiotic which can be extracted from Polystiotus cinnabarinus, P. versicolo and Trametes cinnabarinus. Cinnabarin exhibits antibacterial activity against Gram-positive bacteria as well as antiviral activity, making it a potential candidate for infectious disease research .
Tracheloside (Standard) is the analytical standard of Tracheloside. This product is intended for research and analytical applications. Tracheloside is an antiestrogenic lignin. Tracheloside promotes keratinocyte proliferation through ERK1/2 stimulation. Tracheloside is a good candidate to promote wound healing .
Dihydrokaempferol (Standard) is the analytical standard of Dihydrokaempferol. This product is intended for research and analytical applications. Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents .
Erythrodiol (Standard) is the analytical standard of Erythrodiol. This product is intended for research and analytical applications. Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis .
d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
Sophoridine (Standard) is the analytical standard of Sophoridine. This product is intended for research and analytical applications. Sophoridine is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
5-Methyl-2-thiophenecarboxaldehyde (Standard) is the analytical standard of 5-Methyl-2-thiophenecarboxaldehyde. This product is intended for research and analytical applications. 5-Methyl-2-thiophenecarboxaldehyde acts as a candidate to microscopic third order non-linear optical (NLO) material[1].
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
N-Formylfortimicin A (SF-1854) is an aminoglycoside antibiotic with broad-spectrum antibacterial activity. It primarily acts on bacterial ribosomes to inhibit protein synthesis and exhibits notable inhibitory effects against various Gram-positive and Gram-negative bacteria (e.g., E. coli with a MIC of 12.5-50 μg/mL), making it a potential candidate for research on bacterial infection-related diseases .
N-Acetyl-D-mannosamine (ManNAc) is an oral active sialic acid precursor that can prevent hypertension by increasing sialylation of IgG, making it a promising candidate for cardiovascular disease research. Additionally, N-Acetyl-D-mannosamine can activate hypocretin (HCRT) gene expression in orexin neurons and improve neurodegeneration caused by aging, offering potential avenues for research in neurological disorders .
β-Amyrin shows effectively counteract amyloid β (Aβ)-induced impairment of long-term potentiation (LTP). β-Amyrin is a promising candidate for Alzheimer's disease (AD) research. β-Amyrin exhibits anti-inflammatory effects, protective activity against pulmonary fibrosis, and notable antibacterial capabilities. β-Amyrin is an orally active natural triterpenoid compound .
β-Amyrin shows effectively counteract amyloid β (Aβ)-induced impairment of long-term potentiation (LTP). β-Amyrin is a promising candidate for Alzheimer's disease (AD) research. β-Amyrin exhibits anti-inflammatory effects, protective activity against pulmonary fibrosis, and notable antibacterial capabilities. β-Amyrin is an orally active natural triterpenoid compound .
Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
Tropolone is a seven-membered non-benzenoid aromatic compound, which is the precursor of many Azulene derivatives. Tropolone is a potent mushroom tyrosinase inhibitor with an IC50 value of 0.4 μM. Its inhibitory effect can be achieved by dialysis or excess CU 2+ Reversa. Tropolone exhibits broad anti-viral and anti-fungal activity and is synergistic upon co-treatment with nucleos(t)ide analog drugs. Tropolone is a promising candidate for research in osteosarcoma .
Ziyuglycoside I (Standard) is the analytical standard of Ziyuglycoside I. This product is intended for research and analytical applications. Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
3β,15α-Dihydroxy-7,11,23-trioxo-lanost-8-dien-26-oic acid is a triterpene compound that can be found in Ganoderma lucidum, and it inhibits nitric oxide (NO) production in BV-2 microglial cells induced by lipopolysaccharide (LPS, HY-D1056), with an IC50 of 6.50 μM, making it a potential candidate for anti-inflammatory research .
Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
Isoquercetin (Standard) is the analytical standard of Isoquercetin. This product is intended for research and analytical applications. Isoquercetin (Quercetin 3-glucoside) is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties. Isoquercetin alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway . Isoquercetin regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Isoquercetin has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies .
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .
Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
The CHRNA1 Protein undergoes a substantial conformational shift upon acetylcholine binding, influencing all subunits and leading to the activation of an ion-conducting channel. Yet, the acetylcholine receptor alpha subunit of CHRNA1 can be non-functional in certain cases, underscoring the need to comprehend the factors governing its functionality and integration into fully operational acetylcholine-gated cation-selective channels. CHRNA1 Protein, Human (His) is the recombinant human-derived CHRNA1 protein, expressed by E. coli , with N-6*His labeled tag.
The CHRNA1 Protein undergoes a substantial conformational shift upon acetylcholine binding, influencing all subunits and leading to the activation of an ion-conducting channel. Yet, the acetylcholine receptor alpha subunit of CHRNA1 can be non-functional in certain cases, underscoring the need to comprehend the factors governing its functionality and integration into fully operational acetylcholine-gated cation-selective channels. CHRNA1 Protein, Human (His-Trx) is the recombinant human-derived CHRNA1 protein, expressed by E. coli , with N-Trx, N-6*His labeled tag.
The CDK15ic protein, functioning as an antiapoptotic kinase, counteracts TRAIL/TNFSF10-induced apoptosis by phosphorylating BIRC5 at 'Thr-34'. This regulatory role crucially inhibits programmed cell death triggered by TRAIL/TNFSF10, highlighting the heterodimer's active contribution to antiapoptotic signaling. CDK15-CCNY Protein, Human (sf9, GST, Flag) is the recombinant human-derived CDK15-CCNY, expressed by Sf9 insect cells , with GST, Flag labeled tag. ,
Pleckstrin Homology-Like Domain Family A Member 2; Beckwith-Wiedemann Syndrome
Chromosomal Region 1 candidate Gene C Protein; Imprinted in Placenta and Liver Protein; Tumor-Suppressing STF cDNA 3 Protein; Tumor-Suppressing Subchromosomal Transferable Fragment
PHLDA2 protein regulates placenta growth, potentially through its PH domain, which competes with other PH domain-containing proteins, hindering their binding to membrane lipids. PHLDA2 Protein, Human (His) is the recombinant human-derived PHLDA2 protein, expressed by E. coli , with C-6*His labeled tag.
The CDK15ic protein, functioning as an antiapoptotic kinase, counteracts TRAIL/TNFSF10-induced apoptosis by phosphorylating BIRC5 at 'Thr-34'. This regulatory role crucially inhibits programmed cell death triggered by TRAIL/TNFSF10, highlighting the heterodimer's active contribution to antiapoptotic signaling. CDK15-CCNY Heterodimer Protein, Human (sf9) is a recombinant protein dimer complex containing human-derived CDK15-CCNY Heterodimer protein, expressed by sf9 insect cells , with tag free.
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Tetradecanedioic acid-d24 is the deuterium labeled Tetradecanedioic acid . Tetradecanedioic acid is an endogenous metabolite and belongs to the class of organic compounds known as long-chain fatty acids. Tetradecanedioic acid can act as a candidate biomarker for organic anion-transporting polypeptide mediated agent-agent interactions .
Cariprazine-d8-1 (RGH-188-d8-1) is the deuterium labeled Cariprazine (HY-14763). Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties . Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease . Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD . Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .
Wolf Hirschhorn syndrome candidate 1 like 1; WHSC1L1; NSD3; pp14328; Histone-lysine N-methyltransferase NSD3; Protein whistle
WB, FC
Human, Mouse, Rat
NSD3 Antibody (YA3074) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3074), targeting NSD3, with a predicted molecular weight of 162 kDa (observed band size: 162 kDa). NSD3 Antibody (YA3074) can be used for WB, FC experiment in human, mouse, rat background.
FLJ23286 antibody; IL5 promoter REII region binding protein antibody; KIAA1090 antibody; MGC176638 antibody; MMSET antibody; MMSET type II antibody; Multiple myeloma SET domain containing protein type III antibody; Multiple myeloma SET domain protein antibody; Multiple myeloma SET domain-containing protein antibody; NSD 2 antibody; FLJ23286 antibody; IL5 promoter REII region binding protein antibody; KIAA1090 antibody; MGC176638 antibody; MMSET antibody; MMSET type II antibody; Multiple myeloma SET domain containing protein type III antibody; Multiple myeloma SET domain protein antibody; Multiple myeloma SET domain-containing protein antibody; NSD 2 antibody; NSD2 antibody; NSD2_HUMAN antibody; Nuclear receptor binding SET domain protein 2 antibody; Nuclear SET domain-containing protein 2 antibody; Probable histone-lysine N-methyltransferase NSD2 antibody; Protein trithorax-5 antibody; REIIBP antibody; Trithorax/ash1 related protein 5 antibody; TRX5 antibody; TRX5 protein antibody; WHS antibody; Whsc1 antibody; Wolf Hirschhorn syndrome candidate 1 antibody; Wolf Hirschhorn syndrome candidate 1 protein antibody; Wolf-Hirschhorn syndrome candidate 1 protein antibody
ASPSCR1; ASPL; RCC17; TUG; UBXD9; UBXN9; Tether containing UBX domain for GLUT4; Alveolar soft part sarcoma chromosomal region candidate gene 1 protein; Alveolar soft part sarcoma locus; Renal papillary cell carcinoma protein 17; UBX domain
WB, ELISA
Mouse
TUG Antibody (YA5093) is a mouse-derived and non-conjugated monoclonal antibody, targeting to TUG. It can be applicated for WB, ELISA assays, in the background of mouse.
HN37 as a potent and chemically stable antiepileptic agent candidate, with an EC50 of 37 nM for KCNQ2 . HN37 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(4-(Bromomethyl)phenyl)(4-(prop-2-yn-1-yloxy)phenyl)methanone is a compound with anticancer activity that can effectively inhibit the growth of tumor cells and shows potential application value in compound development. The compound has also been studied for the improvement of certain neuropathological conditions and as a candidate compound for anti-inflammatory inhibition.
Fluorescent DOTAP (NBD-DOTAP) is a cationic lipid which can be used for nucleic acid and protein delivery. Fluorescent DOTAP is labeled with a fluorophore NBD (maximum excitation/emission wavelength ∼463/536 nm). Fluorescent DOTAP can be used for gene delivery systems, drug delivery, as well as cell imaging and nanocarrier tracking. Fluorescent DOTAP is an ideal candidate for both biological and pharmaceutical formulation (e.g. co-delivery of vaccines) research .
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