UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).IC50 value: 4.2 uM/3.1 uM (L3MBTL1/L3MBTL3) [1]Target: L3MBTL1/L3MBTL3
Nerol is a constituent of neroli oil. Nerol Nerol triggers mitochondrial dysfunction and induces apoptosis via elevation of Ca2+ and ROS. Antifungal activity[1][2].
m-PEG3-aldehyde is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
ELOVL1-IN-1 is an ELOVL1 inhibitor extracted from patent WO2018107056A1, compound 87. ELOVL1-IN-1 can reduce very long chain fatty acid levels. ELOVL1-IN-1 can be used for the research of adrenoleukodystrophy (ALD)[1].
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo[1].
Hispidulin 4'-O-β-D-glucopyranosid, a natural compound, may serve as a potential COVID-19 main protease inhibitor[1].
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).IC50 value: 26 nM(Ki) [1]Target: α7 nAChR agonistin vitro: Treatment with PNU-282987 resulted in an attenuation of neuroinflammation in the MPTP-lesioned SN. Furthermore, PNU-282987 attenuated MPTP-induced dopaminergic cell loss in the SN and reduced striatal dopamine depletion [3].in vivo: Mice were subjected to 70% partial hepatic I/R for 60 min and pretreated with either vehicle or with PNU-282987, and blood and hepatic tissue samples were collected at 3, 6, and 12 h following reperfusion. pretreatment with PNU-282987 decreased serum transaminase levels and ameliorated liver injury after hepatic I/R. Moreover, pretreatment with PNU-282987 suppressed NF-κB activation, cytokine production (tumor necrosis factor α, interleukin 1β), and HMGB1 expression in liver after hepatic I/R [2]. Mice treated with 2.5 and 10 mg/kg of PNU devoted less time to rearing into open arms. In the HB task, MC mice displayed higher exploratory activity reflected in more head-dips (HD) during the first minute than EE and SE, whereas EE displayed low exploration levels reflected in total HD (5 min) [4].
5'''-O-Feruloyl complanatoside B is isolated from Astragali Semen, the seeds of Astragalus Complanatus. Semen Astragali Complanati (SAC) include fatty acids, amino acids, polysaccharides, flavonoids, triterpene glycosides and trace elements; have been reported to involve in chronic diseases such as cardiovascular diseases, diabetes mellitus and cancers[1][2].
DBCO-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
ND2158 (ND-2158) is a highly potent and selective IRAK4 inhibitor with IC50 of 1.3 nM;ND2158 demonstrates high selectivity against 334 kinases, and >1000-fold over IRAK1.ND2158 blocked TNF production, collagen-induced arthritis, and gout formation in mice, suppressed LPS-induced TNF production, alleviated collagen-induced arthritis, and blocked gout formation in mouse models.IRAK4 inhibition promoted killing of ABC DLBCL lines harboring MYD88 L265P, by down-modulating survival signals, including NF-κB and autocrine IL-6/IL-10 engagement of the JAK-STAT3 pathway.In ABC DLBCL xenograft models, IRAK4 inhibition suppressed tumor growth as a single agent, and in combination with the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib or the Bcl-2 inhibitor ABT-199.
GSK1016790A is a potent transient receptor potential vanilloid 4 (TRPV4) activator.
Pamatolol is a cardioselective beta-adrenoceptor antagonist without sympathomimetic activity.
Trimethylammonium chloride-13C3,d9 is the deuterium and 13C labeled Trimethylammonium chloride[1]. Trimethylammonium chloride is an endogenous metabolite.
sGnRH-A is a salmon gonadotropin-releasing hormone (GnRH) analogue that stimulates growth hormone secretion and can also be used as an inducer of ovulation by artificial insemination[1][2].
Falbikitug is a humanized immunoglobulin G1-kappa, anti-LIF monoclonal antibody. Falbikitug is an antineoplastic[1].
Secnidazole (RP-14539) hemihydrate is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole (hemihydrate), as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole (hemihydrate) has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole (hemihydrate) can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2.- contents[1].
Magainin 2 is an antimicrobial peptide discovered in the skin of Xenopus laevis.
D-Glucose-d1-4 is the deuterium labeled D-Glucose. D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response[1].
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12[1].
Reticuline, isolated from Litsea cubeba, shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3[1].
Lamiide, an orally active iridoid compound, can be found in Bouchea fluminensis leaves. Lamiide exhibits anti-inflammatory and anti-lipoperoxidative activity[1].
Hydroxy ipronidazole (Ipronidazole-OH) is a metabolite of nitroimidazole antibiotics, such as ipronidazole (IPZ). Hydroxy ipronidazole may has similar mutagenic potential as the parent compound[1].
Ceftiofur sodium is an antibiotic of the cephalosporin type (third generation), licensed for use in veterinary medicine.
Tos-Pro-OH is a proline derivative[1].
11α-O-Tigloyl-12β-O-acetyltenacigenin B is an ester derivative of Tenacigenin B (HY-N1168), which is isolated from Garcinia cambogia (MTC). Tenacigenin B modulates the antitumor effects of Aurora-A in lymphoma.
SOD1-Derlin-1 inhibitor-1 (compound 56-20) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-1 inhibits SOD1G93A-Derlin-1 complex with an IC50 value of 7.11 μM. SOD1-Derlin-1 inhibitor-1 can be used for the research of amyotrophic lateral sclerosis[1].
Scillascillone is a lanostane-type triterpenoid, which can be isolated from the whole plants of Scilla scilloides[1].
Urotensin II, teleost fish is a cyclic peptide. It can be isolated from the caudal neurosecretory system of teleost fish[1].
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.