Alterlactone is an antimicrobial. Alterlactone shows broad antimicrobial activity against bacterial and fungal. Alterlactone has strong radical scavenging activity[1].
m-PEG10-alcohol (Decaethylene glycol monomethyl ether) is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. m-PEG10-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DFHBI is a small molecule that resembles the chromophore of green fluorescent protein (GFP). Spinach and DFHBI are essentially nonfluorescent when unbound, whereas the Spinach-DFHBI complex is brightly fluorescent both in vitro and in living cells.
Anisocoumarin H is a coumarin that exhibits antifungal activity. Anisocoumarin H shows the activities against Microsporum gypseum, Trichophyton rubrum and Trichophyton mentagrophytes with MICs of 62.5 µg/mL[1].
CHIR-99021 trihydrochloride is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; > 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases.
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases[1][2].
Diethylene glycol bis(p-toluenesulfonate) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
UBP301 is a potent and selective antagonist of kainate receptor with IC50 and KD of 164 μM and 5.94 μM, respectively. UBP301 has ∼30-fold selectivity of kainate receptor over AMPA receptor. UBP301 is the derivative of willardiine[1].
Propargyl-PEG10-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PD 113413 is formed by subsequent hydrolysis of the diketopiperazine quinapril analog. PD 113413 is a potent angiotensin-converting enzyme inhibitor. PD 113413 can be used for research of hypertension and congestive heart failure[1].
Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
1,2-Dierucoyl-sn-glycero-3-phosphocholine (DEPC) is the composition of liposome membrane. 1,2-Dierucoyl-sn-glycero-3-phosphocholine is used for the preparation of liposomes and studying the properties of lipid bilayers. The GO (glucose oxidase) in the 1,2-Dierucoyl-sn-glycero-3-phosphocholine liposome shows the high activity[1][2].
Cereblon inhibitor 2 (compound 8) is a Cereblon inhibitor useful in solid tumor research, especially breast cancer[1].
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells[1].
2'-Deoxy-L-adenosine is an orally active synthon for modified oligodeoxyribonucleotides. 2'-Deoxy-L-adenosine is a potent, specific and selective inhibitor of the replication of hepatitis B virus (HBV) as well as the closely related duck and woodchuck hepatitis viruses (WHV)[1].
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-drug resistant tumor cells[1].
Naltrexone-d4 is deuterium labeled Naltrexone.
Galantide is a reversible and non-specific galanin receptor antagonist.
Thymidine-d2 is the deuterium labeled Thymidine. Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication[1
Cornoside is a phenolic glycoside and has inhibitory effect on rat lens aldose reductase (AR) with an IC50 of 150 μM[1].
Sirt2-IN-6 (compound 24a) potent and selective inhibitor of SIRT2, with an IC50 of 0.815 μM. Sirt2-IN-6 can be used for the research of cancer[1].
MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.IC50 value: 1.65 μM (EC50, for hGPR109a), 1.08 μM (EC50, for mGPR109a) [1]Target: GPR109ain vitro: MK-0354 demonstrated clear and statistically significant partial agonism in the cAMP assays for both the mouse and human receptors with efficacy approximately 60-70% of that of either nicotinic acid or β-hydroxy butyrate, a putative physiologically relevant ligand for hGPR109a, in the same assay platform. In addition, MK-0354 showed no activation of GPR109b in the cAMP assay at any concentration up to 100 μM. Following these interesting observations, we then prepared a number of other 5,5-fused pyrazoles analogous to those that showed receptor activity in our earlier studies. MK-0354 appeared to be somewhat unique among the members of the pyrazole tetrazole series in having reasonable receptor activity.[1]in vivo: MK-0354 retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism, but did not induce vasodilation at the maximum feasible dose. Moreover, preadministration of MK-0354 blocked the flushing effect induced by nicotinic acid but not that induced by PGD2. This profile made MK-0354 a suitable candidate for further study for the treatment of dyslipidemia.[1] MK-0354 is a GPR109A partial agonist that activates the antilipolytic pathway in adipocytes. The single-dose and multiple-dose pharmacokinetics and pharmacodynamics, as well as tolerability, of MK-0354 were examined in two Phase I studies conducted in healthy male volunteers. The lipid efficacy of MK-0354 was assessed in a Phase II study conducted in male and female patients with dyslipidemia.[2]
2,5-Furandimethanol is obtained from 5-Hydroxymethylfurfural. 5-hydroxymethylfurfural, as a building block, is considered an important intermediate due to its rich chemistry and potential availability from carbohydrates such as fructose, glucose, sucrose, cellulose and inulin[1][2].
Ancitabine is an antileukemia drug[1].
Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia[1].
N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methylalanine is an alanine derivative[1].
Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.
(Tyr1)-pTH (1-34) (human) is a biologically active peptide.
Thalidomide-5-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-COOH can be connected to the ligand for protein by a linker to form PROTACs[1].