Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide, with antitumor activity.
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human[1].
Erythromycin aspartate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin aspartate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin aspartate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Diphenylmethanol-d5 is the deuterium labeled Diphenylmethanol[1].
L685818 is a specific immunophilin ligand. L685818 was neuroregenerative and non-neuroprotective in primary brain cultures. L685818 protects dopaminergic neurons from toxic inhibition of MPP+ and 6-OHDA, reduces tyrosine hydroxylase (TH) loss, and promotes neuronal process regeneration. L685818 is also an antifungal reagent for Cryptococcus neoformans[1][2].
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC50 values of 19 ± 6 nM and 56 ± 12 nM, respectively[1].
5-Difluoromethyluridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively [1].
E3 ubiquitin ligase binder-1 (compound 11) is a potent E3 ubiquitin ligase binder. E3 ubiquitin ligase binder-1 is a ligand for E3 Ligase[1].
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1)[1]. GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice[2][3].
Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
4-Chlorocinnamic acid has inhibitory effects on tyrosinase. 4-Chlorocinnamic acid has antibacterial activity. 4-Chlorocinnamic acid also inhibits Colletotrichum gloeosporioides growth[1][2][3].
Butanserin (R 53393) is a potent and selective α1-adrenoceptor antagonist for the study of cardiovascular disease[1].
N-Boc-C1-PEG3-C3-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Monomethylsulochrin is a potent antibacterial metabolite from endophytic fungus Aspergillus fumigatus, isolated from Albizia lucidior leaves (fabaceae). Monomethylsulochrin exhibits anti-Staphylococcus aureus activity with minimum inhibitory concentration (MIC) of 31.25 μg/mL[1].
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate[1].
4-Heptyloxyphenol (p-(heptyloxy)phenol) has antibacterial activity agaisnt P. gingivalis, S. artemidis, Str. sobrinus (MIC: 0.10, 0.21, 0.14 mM)[1].
Azido-PEG1-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities[1].
GW0742 is a high affinity PPAR β/δ agonist with an IC50 of 1 nM for human PPARδ, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.
Kallikrein-IN-2 (compound 1) is a Kallikrein inhibitor[1].
Abetimus (LJP 394 free base) is an immunosuppressant consisting of four double-stranded DNA (dsDNA) oligonucleotides. Abetimus is capable of crosslinking anti-dsDNA antibodies on the surface of B cells, and decreases anti-dsDNA antibodies levels. Abetimus has the potential for research of systemic lupus erythematosus[1].
Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice[1].
Fmoc-Tyr(SO3nP)-OH is a tyrosine derivative[1].
TNIK-IN-4 is a potent TNIK inhibitor with IC50 of 0.61 μM. TNIK-IN-4 has inhibitory activity against typical colorectal cancer cell line HCT116[1].
2H-Pyrido[2',1':3,4]pyrazino[1,2-b]indazole-3-carboxylic acid, 6-(1, 1-Dimethylethyl)-6, 7-Dihydro-10 -(3-methoxypropoxy)-2-oxo-, (6R)- has antibacterial and antiviral activity and can be used to study Hepatitis B virus.
A small molecule 5-HT1A and 5-HT2A receptor antagonist and inhibitor of serotonin and dopamine reuptake, also possess affinity for the α1A- and α1B-adrenergic receptors. Depression Phase 2 Clinical
Avotaciclib (BEY1107) trihydrochloride is a potent and orally active inhibitor of cyclin dependent kinase 1 (CDK1). Avotaciclib trihydrochloride can be used for the research of locally advanced or metastatic pancreatic cancer[1].
DCZ19931 is a potent multi-targeting kinase inhibitor. DCZ19931 has anti-angiogenic effects on ocular neovascularization. DCZ19931 also inhibits ERK1/2-MAPK and p38-MAPK signaling[1].