Infection

HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC₅₀s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC₅₀ of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC₅₀ of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity.

Benzoic acid-d is the deuterium labeled Benzoic acid (HY-N0216). Benzoic acid is an aromatic alcohol existing naturally in many plants and is a common additive to food, drinks, cosmetics and other products. It acts as preservatives through inhibiting both bacteria and fungi.

Maximin H4 is an antimicrobial peptide derived from the skin secretions of Chinese red belly toad Bombina maxima. Maximin H4 has activity against Escherichia coli ATCC25922, Staphylococcus aureus ATCC2592, Bacillus pyocyaneus CMCCB1010 and Candida albicans ATCC2002, the MIC values are 12, 6, 12, 6 μg/ml, respectively.

Ganomycin I is a non-competitive dual inhibitor of α-glucosidase and HMG-CoA reductase, with IC₅₀ values of 0.3 μM and 12.3 μM, respectively. Ganomycin I inhibits HIV-1 protease, with an IC₅₀ of 7.5 μg/mL. Ganomycin I also suppresses RANKL-induced osteoclast differentiation and bone resorption by inhibiting the activation of ERK, JNK and p38 MAPK, as well as downregulating the c-Fos/NFATc1 signaling pathway. Ganomycin I exhibits antibacterial activity against Gram-positive bacteria, and shows weak activity against Mycobacterium tuberculosis H37Ra. It can be used in research related to metabolic diseases, bone metabolism and anti-infection.

Guajaphenone A is a benzophenone glycoside antibacterial agent that can be found in the leaves of Psidium guajava L. Guajaphenone A inhibits the growth of Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. Guajaphenone A is applicable to research related to bacterial infections.

IBT21 is an endoplasmic reticulum stress inhibitor that binds to unfolded or misfolded proteins and prevents their aggregation. IBT21 inhibits UPR activation of the ATF6, IRE1 and PERK branches under ER stress, with IC₅₀ values of 0.24 μM, 0.33 μM, and 0.46 μM, respectively. IBT21 protects cells from ER stress-induced death and mutant prion protein (protein toxin)-induced growth inhibition. IBT21 exhibits chemical chaperone activity distinct from UPR modulators, does not affect protein translation, moderately reduces DTT (HY-15917)-induced ER stress, and fails to inhibit the heat shock response. IBT21 is useful for research related to prion diseases.

PRP020 is a potent and specific inhibitor of mycobacterial ATP synthase. PRP020 does not inhibit acidification driven by succinate. PRP020 exihibits MIC₉₅ against M. tuberculosis of 2 μM, and it remains active against most drug-resistant mutant strains. PRP020 is highly safe and can be used in anti-tuberculosis research.

Brevinin-1Ea is an antimicrobial peptide derived from the skin secretions of Rana esculenta.

Thalrugosaminine is a benzylisoquinoline alkaloid isolated from the roots of Thalictrum minus. Thalrugosaminine shows good antibacterial activity with MIC values of 64-128 µg/ml.

TMV-IN-10 (compound 4h) is an arecoline derivative with anti-tobacco mosaic virus (TMV) activity (EC₅₀=146 µg/mL). TMV-IN-10 can be used in research on controlling crop pests and diseases and improving crop yields by acting on the viral coat protein (CP) to cause viral fragmentation.

Droxinavir (SC-55389A free base) is an HIV-1 protease inhibitor. Droxinavir binds to the S2 and S2' subsites of HIV-1 protease, and this interaction is regulated by protease amino acid residue 88, where the N88S mutation confers viral resistance. Droxinavir can be used in studies related to human immunodeficiency virus type 1 infection.

DVR-01 is a HBV inhibitor with EC₅₀ values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. DVR-01 shows antiviral activity against drug-resistant HBV mutants with EC₅₀s of 2.403-3.273 μM. DVR-01 can be used for the research of HBV infection and related diseases.

Trichodimerol (BMS-182123) is a TNF-α promoter inhibitor that inhibits the activity of lipopolysaccharide-induced cytokine secretion. Trichodimerol inhibits lipopolysaccharide-induced TNF-α promoter activity, reduces steady-state TNF-α mRNA expression, and does not alter the stability of TNF-α mRNA. Trichodimerol inhibits lipopolysaccharide-induced TNF-α secretion in murine and human immune cells. Trichodimerol reduces lipopolysaccharide-induced IL-1β secretion by 25%-50% in vitro. Trichodimerol does not alter total protein synthesis or constitutive lysozyme secretion at effective concentrations. Trichodimerol can be used for the research of septic shock.

Moniliformin-¹³C₄ sodium is the ¹³C-labeled Moniliformin sodium (HY-101905). Moniliformin sodium salt is a potent mycotoxin isolate from Fusarium moniliforme.

VNRX-14079 is an antibacterial agent and PBP2 inhibitor, with an IC₅₀ value of 1.7 μM against wild-type Neisseria gonorrhoeae PBP2. VNRX-14079 forms a covalent bond with Ser310 of PBP2, interacts with multiple residues of PBP2 to stabilize the complex, and induces an inward conformational change of the β₃-β₄ loop in chimeric PBP2. VNRX-14079 exhibits antibacterial activity against Ceftriaxone (HY-B0712)-resistant Neisseria gonorrhoeae strains. VNRX-14079 can be used in the research of gonorrhea.

Hydroxydihydrobovolide is a α-β-unsaturatedγ-lactone found in Portulaca oleracea L.. Hydroxydihydrobovolide shows cytotoxicity against cancer cells and shows anti-HIV-1 activity (IC₅₀ = 122.7 μM). Hydroxydihydrobovolide can be used for the researches of neuroblastoma and HIV-1 infection.

Xibornol (Bactacine) has strong antibacterial action against Streptococcus pneumoniae, Streptococcus pyogenes, and Staphyloccus aureus, as well as against Actinomyces israelii and Corynebacterium ulcerans. Xibornol has the potential for using for the antisepsis of the oral cavity and as adjuvant in pharyngeal infections caused by Gram-positive microorganisms.

ent-Heronamide C has antifungal activity and is designed as probe for the mode-of-action analysis of heronamide C.

CP-67015, a quinolone antibiotic, is a potent topoisomerase II inhibitor. CP-67015 is a positive direct-acting mutagen in mammalian cells with both gene and chromosomal level effects.

4-Glycidyloxycarbazole-d₅ is the deuterium labeled 4-Glycidyloxycarbazole (HY-W013429). 4-Glycidyloxycarbazole (compound 8) is an antimicrobial agent that disrupts bacterial biofilm formation.