Amphotericin X1 is an 13-O-methyl derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, C.parapsilosis 937A, Cryptococcus neoformans 451, Aspergillus niger 57A and A.fumigatus with MIC values of 1 μg/mL, 8 μg/mL, 1 μg/mL, 2 μg/mL and 2 μg/mL, respectively[1].
(R)-3-(Benzylthio)-2-((tert-butoxycarbonyl)amino)propanoic acid is a cysteine derivative[1].
hnps-PLA-IN-1 (compound 5aa), a indole-3-acetamide, is a hnps-PLA2 inhibitor (IC50=0.124 μM)[1].
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanoma cells[1].
(S)-Osanetant is the S-enantiomer of Osanetant. Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia[1].
GB-2a is a bioflavonoids that can be isolated from Rheedia gardneriana. GB-2a has significant analgesic activity in mice with 58.9% inhibition[1].
c-Myc inhibitor 9 (compound 332) is a c-Myc inhibitor with an logEC50 of ≥6. c-Myc inhibitor 9 inhibits tumor growth in nude mouse models. c-Myc inhibitor 9 can be used for cancer research[1].
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.Target: beta-lactamaseImipenem with Relebactam is active against Escherichia coli, Klebsiella pneumoniae, and Enterobacter spp., including K. pneumoniae carbapenemase (KPC)-producing isolates. The combination of Imipenem with Relebactam demonstrated activity against KPC-producing Enterobacteriaceae and multidrug-resistant P. aeruginosa. The imipenem MIC50 and MIC90 values for the ESBL-producing isolates were 0.25 and 0.5 μg/ml, respectively; with the addition of Relebactam, the corresponding values were 0.25 and 0.25 μg/ml. Five isolates harbored blaKPC. For these 5 isolates, the imipenem MICs ranged from 0.5 to >32 μg/ml. With the addition of Relebactam, the MICs decreased to 0.12 to 0.5 μg/ml.[1] Relebactam inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. β-Lactamase inhibitors (BLIs) have played an important role in combatting β-lactam resistance in Gram-negative bacteria, but their effectiveness has diminished with the evolution of diverse and deleterious varieties of β-lactamases.[2]
CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer[1].
cis-Methylisoeugenol (compound 10) can be isolated from the MeOH extract of R. fasciculatum[1].
LL-37, Human is a 37-residue, amphipathic, cathelicidin-derived antimicrobial peptide, which exhibits a broad spectrum of antimicrobial activity[1]. LL-37, Human could help protect the cornea from infection and modulates wound healing[2].
N6,N6-Dimethyladenosine is a modified ribonucleoside previously found in rRNA, and also exhibits in mycobacterium bovis Bacille Calmette-Guérin tRNA[1].
2-Hydroxybutyric acid (α-Hydroxybutyric acid ) is converted from 2-Aminobutyric acid, with 2-oxobutyric acid as an intermediate metabolite[1].
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells[1][2][3].
Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers[1][2].
Oligomycin D (Rutamycin A) is an antibiotic. Oligomycin D can be derived from a strain of S. rutgersensis. Oligomycin D also is a potent inhibitors of K-Ras PM localization. Oligomycin D can be used for the research of various cancers[1].
(+)-Nortrachelogenin (Wikstromol), a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity[1].
γ-Glutamylornithine is the urine excreta of patients with HHH syndrome (hyperuricemia, hyperaminemia, and hypercitrullinuria) and rotary atrophy associated with hyperuricemia. Increased levels of endogenous ornithine increase levels of γ-Glutamylornithine in the urine[1].
IONIS-FB-LRx is a specific antisense oligonucleotide (ASO) targeting complement factor B (CFB). IONIS-FB-LRx effectively reduces circulating levels of CFB. IONIS-FB-LRx can be used for geographic atrophy (GA) research[1][2].
4,5-O-Dicaffeoyl quinic acid methyl ester (compound 4), a dicaffeoylquinic acid, has potent antiviral activity against respiratory syncytial virus (RSV) with an IC50 of 0.63 μg/mL and a CC50 of 118.68 μg/mL.
Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals[1].
16-Azidohexadecanoic acid, a synthetic fatty acid, can be used as a modification marker for nucleotides and a molecular probe for fatty acid metabolism[1][2].
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study[1][2][3].
rCRAMP (rat) is the rat cathelin-related antimicrobial peptide. rCRAMP (rat) contributes to the antibacterial activity in rat brain peptide/protein extracts. rCRAMP (rat) is a potential key player in the innate immune system of rat CNS[1][2].
Cipropride (S enantiomer) is the S enantiomer of cipropride; cipropride is an antiemetic drug.
1-Hexanol, a primary alcohol, is a surfactant that can be employed in industrial processes to enhance interfacial properties[1]. 1-Hexanol uncouples mitochondrial respiration by a non-protonophoric mechanism[2].
Mibefradil is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels displaying IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.
Tectorigenin 7-O-Xylosyl Glucoside is a glycosidic isoflavone isolated from Pueraria thomsonii flower[1].
Ophiobolin C inhibits CCR5 binding to the envelop protein gp120 and CD4, which is responsible for mediating the entry of HIV-1 into cells[1]. Ophiobolin C is also cytotoxic to chronic lymphocytic leukemia cells[2].