CH2COOH-PEG3-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer[1].
3-O-Methylgalangin (Galangin 3-methyl ether) is a natural flavonoid compound from the rhizome of Alpinia officinarum (AO) with antibacterial activities, which also inhibits pancreatic lipase[1][2].
Boc-Val-Gly-Arg-βNA is a colorimetric substrate for plasminogen activator[1].
Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1[1].
GSK'872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM.
Gageotetrin C is an antimicrobial peptide derived from the marine bacterium Bacillus subtilis. Gageotetrin C is more active against fungi (MIC value is 0.02-0.04 μM) [1].
Tetrazine-Ph-NHS ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
JG26 is an ADAM17 inhibitor, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM for ADAM8, ADAM17, ADAM10 and MMP-12, respectively[1].
N-(Trimethylamine−boranecarbonyl)proline methyl ester is a proline derivative[1].
Amprolium hydrochloride is a coccidiostat used in poultry, is a thiamine analogue and blocks the thiamine transporter of Eimeria species by blocking thiamine uptake it prevents carbohydrate synthesis.
CP-447697 is a lipophilic C5a receptor antagonist with an IC50 value of 31 nM. CP-447697 can be used for the research of inflammation[1].
GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction[1].
7-Prenyljacareubin is a natural xanthone found in Garcinia gardneriana[1].
AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
m-PEG8-thiol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
2'-Fluorothymidine (2'-Fluoro-2'-deoxythymidine), a bioisostere of both thymidine (TdR) and methyluridine, is a putative highly selective substrate for thymidine kinase type 2 (TK2)[1].
Neuchromenin is a microbial melabolite that can be isolated from the culture broth of Eupenicillium javanicum var. meloforme PFll81. Neuchromenin induces neurite outgrowth of PC12 cells[1].
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells[1].
RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property[1].
Rubitecan (RFS 2000), a camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells[1][2][3].
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases[1].
Mephenoxalone inhibits neuron transmission and can relax skeletal muscles by inhibiting the reflex arc[1].
Trimethoprim 3-oxide is the urinary metabolite of trimethoprim.
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV)[1].
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
S07-2001 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 value of 2.08 μM. S07-2001 enhances the activity of Doxorubicin against cancer cells. S07-2001 has potential as a chemotherapeutic potentiator for cancer drug resistance[1].
A novel lysosomotropic REV-ERB ligand that has a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy; relieves REV-ERB-mediated transcriptional repression, significantly increases autophagy-associated protein p62 in treated cells; disrupts lysosomal function, blocks the autophagy process at the late stage, and reduces cancer cell viability; a novel dual autophagy/REV-ERB inhibitor more cytotoxic than chloroquine.
Vildagliptin carboxylic acid metabolite (M20.7) TFA is a potent P450 enzyme activity inhibitor[1].
CH3OCO-D-CHA-Gly-Arg-pNA acetate is a chromogenic substrate for factor Xa[1][2].