MGB4 is a DNA minor groove binder. MGB4 binds to ARE-containing DNA and inhibition of topoisomerase I activity. MGB4 can impacts key cellular pathways, including inhibition oftranslation and alterations in sphingolipid and amino acid metabolism. MGB4 also reduces spermine and spermidine metabolism companied with Doxorubicin). MGB4 can be used for the research of cancer, such as Prostate cancer.

LY 255262 is an antibacterial agent. LY 255262 exhibits potent inhibitory effects against a variety of Gram-positive and Gram-negative bacteria in vitro. LY 255262 has MIC values of 64, 0.25, 0.5, 0.25, 0.25, 1, and 1 μg/mL for Staphylococcus aureus, Streptococcus pneumoniae, Haemophilus influenza, Escherichia coli, Klebsiella, Enterobacter aerogenes, and Serratia, respectively. LY 255262 has a relatively weak inhibitory effect on Pseudomonas (MIC >128 μg/mL). LY 255262 can be used in antibacterial research.

SC-77964 is a potent, selective and orally active matrix metalloprotease (MMP) inhibitor. SC-77964 shows IC50 values < 0.1 nM against MMP-2, MMP-9, and MMP-13. SC-77964 can be used for the research of cancer and inflammation, such as melanoma.

Carpipramine is an antipsychotic agent that belongs to the iminodibenzyl class. Carpipramine is a potent dopamine antagonist which blocks alpha 1- and alpha 2-adrenoceptors. Carpipramine also has antagonist properties with respect to serotonin (5-ΗΤ2) receptors. Carpipramine exhibits antipsychotic and anti-depressant effects. Carpipramine can be used for the research of neurological disease, such as post-traumatic stress disorder (PTSD) and depression.

SGC-NSP2hel-1 (RA-0188293), a chemical probe, is a potent, specific and orally active nsP2 inhibitor. SGC-NSP2hel-1 has broad spectrum activity against multiple alphaviruses of the nsP2 helicase with a CC50 > 250 μM. SGC-NSP2hel-1 (RA-0188293) shows selectivity index > 4000 against human RNA helicases. SGC-NSP2hel-1 reduces virus replication and limited virus-induced pathology by forming a stable complex with nsP2 and ATP in a preclinical small animal model of CHIKV disease.

Taligantinib (Compound Example 70) is an orally active and selective dual inhibitor targeting vascular endothelial growth factor receptor 2 (VEGFR-2) and hepatocyte growth factor receptor (c-Met). Taligantinib suppresses tumor angiogenesis and cell proliferation. Taligantinib is promising for research of solid tumors such as non-small cell lung cancer and hepatocellular carcinoma.

(R,R)-VRT-534 is the (R,R)-enantiomer of VRT-534). VRT-534 (Compound 3) is a chemical chaperone targeting connexin 26 (Cx26). Vrt-534 exhibits dose-responsive binding to recombinant WT Cx26 and mutant Cx26 K188N with EC50s of 19 and 5 μM, respectively. Vrt-534 can be used in research related to hearing impairment.

1,4-Naphthoquinone-NH-C2-NH-Trolox is a brain-penetrant Trolox-vitamin K conjugate with neuroprotective activity. 1,4-Naphthoquinone-NH-C2-NH-Trolox can inhibit oxytosis, ferroptosis, ATP depletion and ROS production. 1,4-Naphthoquinone-NH-C2-NH-Trolox selective suppresses M1 markers expression. 1,4-Naphthoquinone-NH-C2-NH-Trolox can be used for the research of neurological disease, such as Alzheimer’s disease (AD).

cBu-Cit-PAB (Compound 13) is a key intermediate of ADC linker. cBu-Cit-PAB can be used for synthesis of antibody-drug conjugates (ADCs).

UTPU (trisodium) (Compound 19) is a selective P2Y6R agonist with an EC50 of 0.4 μM. UTPU (trisodium) can activate the intracellular calcium signaling pathway mediated by P2Y6. UTPU (trisodium) can be used for the research of inflammation.

Ara-UTP is a sugar-modified nucleotide triphosphate that deceives RNA polymerases and blocks chain extension.

Tub114 is a drug-linker conjugate for ADC. Tub114 is a Tubulysin B analog with a stable hydrophilic linker. Tub114 can be used for synthesis of ADCs.

LD2-3 is a topoisomerase I inhibitor. LD2-3 can be connected to monoclonal antibodies via linkers to form antibody-drug conjugate (ADC) molecules. LD2-3 can be coupled with CEA antibodies to form ADC drugs for the study of CEA overexpressing tumors.

GYKI 12743 is a vasoselective, postsynaptic α-adrenoceptor blocker. GYKI 12743 inhibits but does not completely eliminate the cutaneous microcirculatory blood flow reduction evoked by electrical stimulation of the peripheral stump of the cut saphenous nerve in rats. GYKI 12743 can be used for the study of neurological diseases.

L07-2 (Compound 6) is an active scaffold comprising a stimulator of TLR7/8. L07-2 can be used for synthesis of immune-stimulating antibody conjugates (ISACs) for cancers research.

Ac-BIM-acid bromide is a derivative of Acridine. Ac-BIM-acid bromide significantly inhibits amyloid fibrillation. Ac-BIM-acid bromide modulates the structure of N-terminal region of Saccharomyces cerevisiae Stm1 protein (Stm1_N1-113) and the amyloid morphology of human Aβ42 protein, inhibiting theirs growth. Ac-BIM-acid bromide can be used for Alzheimer’s disease research.

Dioctatin A hydrochloride is a metabolite of Streptomyces and an inhibitor of human dipeptidyl aminopeptidase II. Dioctatin A hydrochloride can inhibit aflatoxin production by Aspergillus parasiticus with an IC50 of 4.0 μM. Dioctatin A hydrochloride can reduce the mRNA levels of aflatoxin biosynthetic genes and the regulatory gene aflR, inhibit conidiation and decrease the mRNA level of the brlA gene, and also promote kojic acid production. In addition, Dioctatin A hydrochloride can inhibit sterigmatocystin production. Dioctatin A hydrochloride has pleiotropic regulatory effects on the production and differentiation of fungal secondary metabolites.

J-104123 is an inhibitor of squalene synthase with monocarboxylic acid structure. J-104123 can lower serum cholesterol level in dog models.

RM-5038 is a thiazolide antivirus agent. RM-5038 can induce innate immunity and reduce HIV replication.

NU1064 (dihydrochloride) is an inhibitor of PARP. NU1064 (dihydrochloride) potentiates the cytotoxicity of DNA-methylating agent (MTIC) in a concentration-dependent manner.

CHIPOpt, a peptide, is an orthosteric CHIP TPR domain inhibitor with a Kd of ∼16 nM. CHIPOpt has anti-aggregation activity and decreases p.tau ubiquitination with little effect on unmodified tau. CHIPOpt can be used for Alzheimer’s disease research.

Primidophos is an ingredient in insecticide and acaricide compositions. Primidophos can be used in research on the prevention and control of insect and acarid pests.

(±)-Dehydroaltenusin, an antibiotic, is a selective eukaryotic DNA polymerase α (pol α) inhibitor with an IC50 of 0.68 μM. (±)-Dehydroaltenusin can be isolated from fungus Alternaria tenuis. (±)-Dehydroaltenusin competitively inhibits the DNA template primer (Ki: 0.23 μM) and non-competitively suppresses the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki: 0.18 μM). (±)-Dehydroaltenusin induces the cancer cell S-phase cycle arrest and apoptosis. (±)-Dehydroaltenusin can be used for cancers like human adenocarcinoma research.

N-Benzyl-N-demethylpronqodine A (Compound 16) is an inhibitor of NAD(P)H:quinine acceptor oxidoreductase 1 (NQO1) with an IC50 of 83.3 nM.

(Rac)-AAA is the racemate of AAA. (Rac)-AAA is an antagonist of 20-HETE receptor. (Rac)-AAA can increase the expression of GPR75 receptor in androgen-insensitive prostate cancer cells. (Rac)-AAA dose-dependently increases p38 phosphorylation. (Rac)-AAA induces a significant decrease in the phosphor-AKT signal in nuclei of cells. (Rac)-AAA mitigates the NF-κB signal in unstimulated cell nuclei. (Rac)-AAA can diminish the membrane associated signal intensity. (Rac)-AAA decreases the FAK phosphorylation induced by 20-HETE.

SCH 34343 is a penem antibiotic. SCH 34343 is highly active against Streptococcus pneumoniae (MIC50 ≤ 0.015 mg/L), viridans streptococci (MIC50 = 0.06 mg/L), streptococci of groups A (MIC50 = 0.03 mg/L), B (MIC50 = 0.06 mg/L), C and G (MIC50 = 0.03 mg/L), and Str. bovis. SCH 34343 can be used for antibacterial research.

DZ-2640 is an oral Carbapenem antibiotic, a prodrug of DU-6681. DU-6681 exhibits antibacterial activity against a broad spectrum of gram-positive and -negative bacteria.

DU-6681 is the active parent compound of DZ-2640. DU-6681 possesses a broad-spectrum and potent in vitro antibacterial activity against the majority of gram-positive and gram-negative bacteria. DU-6681 can be used for antibacterial research.

TPG-20A is a SARS-CoV-2 main protease inhibitor with an IC50 of 27.8 nM. TPG-20A also inhibits MERS-CoV main protease. TPG-20A can be used for the research of infection, such as SARS-CoV-2.

AR-709 is a new type of diaminopyrimidine antibiotic. AR-709 exhibits potent and broad-spectrum antibacterial activity against Streptococcus pneumoniae (MIC = 0.03 mg/L). AR-709 can be used for research on bacterial infections.