Propioxatin A, a secondly metabolite produced in microorganism, and is an enkephalinase B inhibitor[1].
Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL[1].
Qingyanshengenin (NSC 379666; compound 2), a pregnane glycoside, is a C21 steroidal aglycone isolated from the root of Cynanchumot ophyllum (Asclepiadaceae). Qingyanshengenin has anti-cancer activity[1].
PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
2-O-Benzoyl-3-O-t-butyldiphenylsilyl-L-threono lactone is a purine nucleoside analog. 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].
RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphan receptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer[1].
SLV-2436 is a highly potent and ATP-competitive inhibitor of MNK1 and MNK2 with IC50s of 10.8 nM and 5.4 nM, respectively.
AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
Yemuoside YM12 is a nortriterpenoid saponin, that can be found in Stauntonia chinensis Decne[1].
Phosphoramidon, a microbial metabolite, is a specific metalloprotease thermolysin inhibitor with an IC50 of 0.4 μg/mL. Phosphoramidon also inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively[1][2][3].
H-D-Lys(Alloc)-OH is a lysine derivative[1].
S-(-)-N-trans-Feruloyl normetanephrine is a nature product with weak anti-acetylcholinesterase activity. S-(-)-N-trans-Feruloyl normetanephrine can be isolated from the aerial parts of Bassia indica Wight[1].
PA3552-IN-1 (compound 15) is an antibiotic adjuvant that restores sensitivity of MDR P. aeruginosa DK2 strain to Polymyxin B. PA3552-IN-1 can reduce PA3552 expression[1].
Adenosine-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology,
Cimidahurinine can be extracted from the seeds of Perilla frutescens[1].
Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.Target: HCN Channel blockerCilobradine is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of Cilobradine. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM Cilobradine (8 ± 2% inhibition; n = 4).
I-152 is a conjugate containing N-acetyl-cysteine (NAC) and cysteamine (MEA). I-152 activates NRF2 and ATF4 signals. I-152 has anti-proliferative properties[1].
Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity[1].
APJ receptor agonist 4 is a potent and oral active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease[1].
Fructo-oligosaccharide DP9/GF8 belongs to fructooligosaccharides (FOS) with degree of polymerization (DP=9) . Fructo-oligosaccharides (FOS) are composed of 8 fructose units linked by (2→1)-β-glycosidic bonds and having a single D-glucosyl unit at the non-reducing end[1].
ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC50=69 nM). ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively[1][2].
4'',5''-Dehydroisopsoralidin is a β-glucuronidase inhibitor (IC50: 6.3 μM). 4'',5''-Dehydroisopsoralidin has anti-inflammatory and anti-oxidative effects. 4'',5''-Dehydroisopsoralidin can be used in the research of inflammation and cancners[1][2].
N-Hydroxysulfosuccinimide (sodium) is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Boc-D-Ser(tBu)-OH is a serine derivative[1].
(±)-8-Prenylnaringenin, a natural prenylated flavonoid, is a potent phytoestrogen. (±)-8-Prenylnaringenin is an orally active selective estrogen receptor modulator (SERM) (Estrogen Receptor/ERR) that inhibits ERα and ERβ with IC50s of 57 nM and 68 nM, respectively. (±)-8-Prenylnaringenin has anticancer effects, and can be used for osteoporosis research[1][2].
h-NTPDase-IN-2 (compound 3l) is a pan-inhibitor of h-NTPDase, with IC50s of 0.35 μM (h-NTPDase1), 4.81 μM (h-NTPDase2), 37.73 μM (h-NTPDase3), 10.32 μM (h-NTPDase8), respectively[1].
1-[(3,5-Dimethylisoxazol-4-yl)sulfonyl]proline is a proline derivative[1].
8-Nitroguanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Biotin-PEG4-Dde-TAMRA-PEG3-Azide is a cleavable 7 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].