JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
Maleylsulfathiazole is an N4-dibasic acid-substituted sulfonamides[1].
DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 exerts a strong antiproliferative effect on the human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression[1].
ALW-II-49-7 (DDR2-IN-1) is a potent, selective DDR2 inhibitor with IC50 of 18.6 nM, also shows ability to inhibit DDR1 and Ephrin-family kinases (IC50=40 nM for EphB2); displays excellent overall kinase selectivity against a panel of over 350 kinases; decreases DDR2 phosphorylation but has little effect on the proliferation of DDR2 mutated cancer cell lines.
Claficapavir (A1752) is a specific nucleocapsid protein (NC) inhibitor with an IC50 around 1 μM. Claficapavir strongly binds the HIV-1 NC (Kd=20 nM) thereby inhibiting the chaperone properties of NC and leading to good antiviral activity against the HIV-1[1].
Isolupalbigenin is an inhibitor of NO. Isolupalbigenin has anti-proliferative activity on HL-60 cells with an IC50 of 5.1 μM[1].
Cyclo(D-Ala-L-Pro) is a cyclodipeptide[1].
μ-Conotoxin KIIIA is an analgesic μ-conotoxin that can be isolated from Conus kinoshitai. μ-Conotoxin KIIIA blocks mammalian neuronal voltage-gated sodium channels (VGSCs) (Nav1.2).μ-Conotoxin KIIIA can be used for research of pain[1][2].
Streptomycin sulfate is an aminoglycoside antibiotic, that inhibits protein synthesis.
Biotin-PEG6-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
AMPK activator 8 (Compound 2) is an AMP-activated protein kinase (AMPK) activator with EC50s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes[1].
N1-Ethoxymethyl pseudouridine 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].
Zinquin is a fluorescent sensor and used to observe reactive Zn2+.
dUTP trisodium is used for PCR.
DS86760016 is a novel selective bacterial leucyl-tRNA synthetase (LeuRS) inhibitor with IC50 of 0.38 uM (Escherichia coli, LeuRS); inhibits Pseudomonas aeruginosa and Acinetobacter baumannii with IC50 of 0.62 and 0.16 uM, respectively; shows active against MDR Gram-negative bacteria (MIC 0.25-2 ug/mL) with an improved pharmacokinetic profile compared with GSK2251052; also shows lower mutant prevention concentrations against P. aeruginosa compared to GSK2251052.
PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
LGD-3303 is a selective androgen receptor modulator (SARM).
Cnidioside B is a glycoside compound, which can be isolated from Leptothyrsa sprucei, C. monnieri and the ripe fruit of Cnidium monieri[1][2][3].
SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.IC50 value: 0.2/0.5 nM [1]Target: D3 receptor antagonistSB269,652 potently (low nanomolar range) abolished specific binding of [(3)H]nemanopride and [(3)H]spiperone to Chinese hamster ovary-transfected D(3) receptors when radioligands were used at 0.2 and 0.5 nM, respectively. However, even at high concentrations (5 μM), SB269,652 only submaximally inhibited the specific binding of these radioligands when they were employed at 10-fold higher concentrations. By analogy, although SB269,652 potently blocked D(3) receptor-mediated activation of Gα(i3) and phosphorylation of extracellular-signal-regulated kinase (ERK)1/2, when concentrations of dopamine were increased by 10-fold, from 1 μM to 10 μM, SB269,652 only submaximally inhibited dopamine-induced stimulation of Gα(i3) [1].
Dusigitumab (MEDI 573) is a human IgG2λ monoclonal antibody that specifically targets IGF2 and IGF1[1].
8-Azanebularine, a compound with hydrogen in place of the C6 amino group, inhibits the ADAR2 reaction at high concentrations (IC50=15 mM). 8-Azanebularine is incorporated into an RNA structure recognized by human ADAR2 results in high-affinity binding (KD=2 nM). 8-Azanebularine can be used for the research of ADAR-catalyzed RNA-editing reaction[1].
DBCO-PEG4 acetic-EVCit-PAB is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Helioxanthin derivative 5-4-2 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV activity with EC50 of 0.08 uM in HepG2.2.15 cells.IC50 value: 0.08 uM (EC50) [1][2]Target: Anti-HBVHelioxanthin derivative 5-4-2 had potent anti-HBV activities in HepG2.2.15 cells, with the EC50s of 1 and 0.08 microM, respectively. The lamivudine-resistant HBV, L526M/M550V double mutant strain, was also sensitive to helioxanthin and 5-4-2. This class of compounds not only inhibited HBV DNA, but also decreased HBV mRNA and HBV protein expression. The EC50 of HBV DNA inhibition was consistent with the EC50 of HBV 3.5 Kb transcript inhibition, which was 1 and 0.09 microM for helioxanthin and 5-4-2 respectively.
STING agonist-16 (1a) is a specific stimulator of interferon genes (STING) agonist. STING agonist-16 (1a) can be used as a potential antiviral and antitumor tool[1].
2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
Boc-NH-PEG7-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1].
Eltrombopag is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.
Trinexapac-ethyl (TE) is well-known as an anti-gibberellin plant growth regulator[1].
2′-Deoxy-5-methoxyuridine is a uridine analogue. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].