BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure[1].
Triacsin C (WS 1228A), a natural intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, is from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity[1]. Triacsin C is found to be highly effective against rotavirus replication[2].
2’-O-(2-Methoxyethyl) inosine 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].
6-Methylmercaptopurine riboside 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].
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitory activity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively[1].
TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).
A-1155463 is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell.
RDN2150 (Compound 25) is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 covalently binds to the C346 residue of ZAP-70. RDN2150 inhibits the expression of CD25 and CD69, and inhibits CD4+ T cell activation. RDN2150 can be used for research of psoriasis[1].
Alterlactone is an antimicrobial. Alterlactone shows broad antimicrobial activity against bacterial and fungal. Alterlactone has strong radical scavenging activity[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].
Cereblon inhibitor 2 (compound 8) is a Cereblon inhibitor useful in solid tumor research, especially breast cancer[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].
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.
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].
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.
HBC525 is a HBC-like fluorophore and a fluorogenic RNA aptamer (Kd=3.8 nM). HBC525 can be directly used as fusion tags for the imaging and tracking of cellular RNAs of interest. Fluorogenic RNA aptamers have also been used to construct various interesting dynamic RNA nanodevices for cellular target detection and imaging[1][2].
Pam3-Cys-Ala-Gly, a synthetic bacterial lipopeptide, is a potent macrophage and B cell activator[1].
Tos-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC)[1].
Enazadrem is a 5-lipoxygenase inhibitor with antiinflammatory activities.
Boc-NH-PEG1-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(R)-Thalidomide ((R)-(+)-Thalidomide) is the R-enantiomer of Thalidomide. (R)-Thalidomide has sedative properties[1][2].
Tubulysin H is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. Tubulysin H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].