NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). NB-598 suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. NB-598 reduced basolaterally secreted radioactivity in cholesterol, cholesterol ester, PL and TG. Furthermore, NB-598 suppressed the basolateral secretion of apolipoprotein (apo) B. When microsomes prepared from control Caco-2 cells were incubated with 10 microM NB-598, acyl CoA:cholesterol acyltransferase (ACAT) activity was inhibited slightly.

Didesmethylrocaglamide is a naturally occurring 1H-cyclopenta[b]benzofuran lignans of the rocaglamide type isolated from three Aglaia species (Aglaia duperreana, A. oligophylla and A. spectabilis). Didesmethylrocaglamide inhibited cell growth in a similar concentration range as the well-known anticancer drug vinblastine sulfate. Didesmethylrocaglamide arrested MPNST cells at G2-M, increased the sub-G1 population, induced cleavage of caspases and PARP, and elevated the levels of the DNA-damage response marker γH2A.X, while decreasing the expression of AKT and ERK1/2, consistent with translation inhibition.

BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity[1].

BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer.

DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.

Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with high affinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier.

Remdesivir O-desphosphate acetonide impurity is an impurity of Remdesivir. Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity and is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.

Mefentrifluconazole is a fungicide on cereals.

MC-Gly-Gly-Phe-Gly is a cleavable ADC linker used for antibody-drug conjugates (ADCs).

SR33805 is a potent Ca2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 blocks L-type but not T-type Ca2+ channels. SR33805 can be used for the research of acute or chronic failing hearts.

LUN42518, also known as Phentolamine Analogue 1, is an analogue of phentolamine. Phentolamine is a nonselective alpha-adrenergic antagonist. LUN42518 has CAS#47142-51-8, no formal name For the convenience of scientific communication, we named it as LUN42518 (combined from Inchi key plus CAS#) according to Hodoodo Chemical Nomenclature.

MW-2474 is an inhibitor of the Lysine Acetyltransferase, KAT6A, as Potent Senescence-​Inducing Anti-​Cancer Agent.

DCBA is a metabolite of insect repellent N-N-diethyl-meta-toluamide (DEET). The concentration of DCBA in urine can assess exposure to DEET.

EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC50=0.31, and 0.82 μM, respectively) and low cytotoxicity (SI>100) in HeLa cells.

Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50=650 nM). Thailanstatin A exerts effects via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the spliceosome and shows low-nM to sub-nM IC50s against multiple cancer cell lines. Thailanstatin A, a payload for ADCs, is conjugated to the lysines on trastuzumab yielding “linker-less” ADC.

KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.

NCGC00092410 is a potent, selective, and nonsugar glucocerebrosidase (GC), with an IC50 of 31 nM. NCGC00092410 shows no activity against the related hydrolases at concentrations up to 77 μM. NCGC00092410 is a GC chaperone and increases the activity and lysosomal localization of glucocerebrosidase in mutant cell lines. NCGC00092410 can be used for the research of Gaucher disease.

DENV-IN-2 is a potent dengue viral replication extracted from patent WO2018215315A1, compound 6AB, has an EC50 of 0.016 nM. DENV-IN-2 shows high potent activity against all four serotypes of the Dengue virus with EC50s ranging from 0.013 to 0.029 nM.

Rineterkib, also known as LTT-462 or ERK-IN-1, is a RAF and ERK1/2 inhibitor which has demonstrated preclinical activity in multiple MAPK activated cancer cells and xenograft models. LTT462 binds to and inhibits ERK, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in numerous tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival.

LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.

CR4056 (CR 4056, CR-4056) is a novel, orally active imidazoline-2 receptor (I2R) ligand with binding IC50 of 596 nM, also selectively inhibits the enzymatic activity of MAO-A with IC50 of 202.7 nM; increases norepinephrine (NE) tissue levels both in the rat cerebral cortex and lumbar spinal cord, shows ED50 of 5.8 mg/kg in CFA rat model of inflammatory pain; shows high effectivity against bortezomib-induced painful neuropathy in rats.

Sulfatinib (HMPL-012) is a potent, multi-targeted tyrosine kinase inhibitor of VEGFR-1/2/3, FGFR1, CSF1R with IC50 of 2/24/1 nM, 15 nM, 4 nM, respectively.

Golgicide A is a potent, highly specific, reversible inhibitor of the cis-Golgi ArfGEF GBF1, inhibits the effect of shiga toxin on protein synthesis with IC50 of 3.3 uM.

JUN76288, also known WEE1-IN-3, is a potent WEE1 kinase inhibitors useful in treatment of cancer and other proliferative diseases. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature

β-Lactamase-IN-2 is a beta-lactamase inhibitor, extracted from patent WO 2019075084 A1, compound 1. β-Lactamase-IN-2 has anti-microbial and anti-bacterial effects.

Epinastine(WAL801) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain).

CC-90001 is a potent, selective and orally active inhibitor of c-Jun N-terminal kinase (JNK). CC-90001 shows 12.9-fold selectivity for JNK1 over JNK2 in a cell-based model. CC-90001 can be used for the research of idiopathic pulmonary fibrosis.

HG106 is a potent SLC7A11 inhibitor and enhances ROS generation, ER stress, and ultimately growth arrest specifically in KRAS-mutant lung adenocarcinoma (LUAD).

YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer.