(4-Fluorophenyl)methanol-d6 is the deuterium labeled (4-Fluorophenyl)methanol[1].
Azepan-2-one-d10 is the deuterium labeled Azepan-2-one[1].
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1[1][2].
KIN1148, a small-molecule IRF3 agonist, is a novel influenza vaccine adjuvant found to enhance flu vaccine efficacy.
Benorylate (Benoral) is the esterification product of paracetamol and acetylsalicylic acid. It has anti-inflammatory, analgesic and antipyretic properties. Benorylate could also inhibit prostaglandin (PG) synthesis.
Mirin is a small-molecule inhibitor of MRN (Mre11, Rad50, and Nbs1) complex.Target: in vitro: Mirin was shown to block Mre11 exonuclease activity and MRN-dependent ATM activation, and to inhibit the ionizing radiation-induced G2/M checkpoint and homologous recombination in mammalian cells. Mirin inhibition of ATM activation is independent of Mre11 nuclease inhibition since the M(HN)RN and M(HL/DV)RN mutant complexes are inhibited equivalently to the wild-type enzyme despite the fact that they are nuclease-deficient. The effects of Mirin have been ascribed to its effects on Mre11 nuclease activity, but as we show here, Mirin is inhibitory of MRN function independent of the nuclease activity of the complex. [2] Addition of the Mre11 inhibitor Mirin to egg extracts and mammalian cells reduces RCC1 association with mitotic chromosomes. HeLa cells expressing Histone H2B-EYFP were treated with Mirin (25 or 50 μM), and mitotic progression was immediately monitored using live cell imaging. Although Mirin-treated cells were able to congress chromosomes to the metaphase plate with similar kinetics as untreated cells, a significant fraction of Mirin-treated cells paused for extended periods of time in a metaphase-like stage without anaphase onset . [1]
Anticancer agent 74 is a moderate anticancer agent. Anticancer agent 74 has lower selectivity and cytotoxicity than doxorubicin to normal cell[1].
4-Aminopyridine-d4 is deuterium labeled 4-Aminopyridine. 4-Aminopyridine is a nonselective K+ channel blocker that binds from the cytoplasmic side of the cell membrane.
BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties[1].
2’-Deoxy-2’-fluoro-N3-(2S)-(2-amino-3-carbonyl] propyl-beta-D-arabinouridine 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].
CPI-905 is a potent and selective EZH2 inhibitor with IC50 value of 39.5 nM.
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca2+-influx blocker[1].
Pirmenol is an orally active antiarrhythmic agent. Pirmenol inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol can be used in the research of cardiovascular disease, such as atrial fibrillation[1][2][4].
SARS-CoV-2-IN-62 (Compound R3b) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-62 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 2.97 μM and 3.82 μM, respectively[1].
p38 MAP Kinase Inhibitor VI (compound c32) is a p38 MAPK inhibitor with an inhibition rate of 24%[1].
M‑1121 is a covalent and orally active inhibitor of the menin-MLL interaction capable of achieving complete and persistent tumor regression[1].
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1 activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility[1].
Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.
AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM[1].
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases[1].
Sophoranol is an alkaloid that can be isolated from S. flavescens, with antiviral activity. Sophoranol has anti-HBV (hepatitis B virus) activity. Sophoranol shows potent antiviral activities against respiratory syncytial virus (RSV) with an IC50 of 10.4 μg/mL[1][2].
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1].
KY-02327 is an orally active, small molecule inhibitor of the Dishevelled (Dvl)-CXXC5 interaction with IC50 of 3.1 uM, a metabolically stabilized KY-02061 analog; KY-02327 is more stable by 2.3-fold and 1.3-fold than KY-02061 in rat liver microsomes and in human hepatocytes, respectively; shows enhanced effect on induction of ALP activity of osteoblast cells compared with KY-02061; activates the Wnt/β-catenin pathway, promotes osteoblast differentiation, and rescues BMD, bone volume, and trabecular bone structures in variectomized (OVX) mouse model.
BML-111, a lipoxin A4 analog, is a lipoxin A4 receptor agonist. BML-111 represses the activity of angiotensin converting enzyme (ACE) and increases the activity of angiotensinconverting enzyme 2 (ACE2). BML-111 has antiangiogenic, antitumor and anti-inflammatory properties[1][2].
Ternatin B4 is an anthocyanin isolated from the flowers of Clitoria ternatea L. (Leguminosae)[1].
ML277(CID53347902) is a novel, potent and selective K(v)7.1 (KCNQ1) potassium channel activator with EC50 of 270 nM.IC50 value: 270 nM (EC50) [1]Target: K(v)7.1 activatorML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity versus KCNQ2 and KCNQ4) as well as against the distantly related hERG potassium channel.
Tizanidine-d4 is the deuterium labeled Tizanidine. Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons[1][2].
ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs. ALK3.IC50 value:Target: ALK1/ALK2ML347 has IC50’s of 46 and 32 nM, respectively, against ALK1 and ALK2; however, the IC50 against ALK3 is 10,800 nM, >300-fold selective over ALK3. ML347 is completely inactive against allthe other kinases tested (with weak activity against ALK6, 9830 nM and KDR (VEGFR2)19,700 nM). ML347 is potent in the BMP4 cell assay (152 nM).
Biotin-PEG2-C6-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.