SGK1-IN-7 is a blood-brain barrier-permeable SGK1 inhibitor with an IC50 of 0.72 μM. SGK1-IN-7 reduces the phosphorylation level of TAU protein at the Ser396 and Ser214 epitopes. SGK1-IN-7 antagonizes the toxicity induced by Okadaic acid. SGK1-IN-7 can be used in the research of Alzheimer's disease.

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers. (Pink: Epigenetic Reader Domain Target protein ligand; Blue: Ligands for E3 Ligase and VHL ligand ; Black: linker).

PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC50 values of 1.2 nM and 6.7 nM, respectively. PARP1/NAMPT-IN-1 can disrupt the homologous recombination repair (HRR) pathway, leading to the accumulation of DNA double-strand breaks (DSBs), inducing cell cycle arrest and apoptosis, and also has antimigratory effects. PARP1/NAMPT-IN-1 exhibits excellent antitumor effects in a breast cancer xenograft model. PARP1/NAMPT-IN-1 can be used for the study of triple-negative breast cancer (TNBC).

Mal-Pip-ValCit-PAB-AZ7550 is a prodrug of EGFR inhibitor. Mal-Pip-ValCit-PAB-AZ7550 selectively binds covalently to albumin via its maleimide moiety. Mal-Pip-ValCit-PAB-AZ7550 exhibits potent in vivo anticancer activity in non-small cell lung cancer xenograft models. Mal-Pip-ValCit-PAB-AZ7550 can be used in research related to non-small cell lung cancer.

LCB-2122 is an adenosine-like nucleoside analogue bearing a C2'-stereogenic all-carbon quaternary center. LCB-2122 can prevent Doxorubicin-induced cardiomyocytes apoptosis with an IC50 of 0.5 μM and prevent Imatinib-induced apoptosis. LCB-2122 can activate AMPK signaling and induce the phosphorylation of AMPK and its downstream substrate, acetyl-CoA carboxylase (ACC). LCB-2122 can reduce Doxorubicin-induced mitochondrial damage. LCB-2122 can be used for the research of heart failure.

NTM-006 is a selective and brain-penetrant adenosine A3 receptor (A3AR) agonist. NTM-006 selectively interacts with adenosine A3AR via π-π stacking with Phe168 and π-alkyl interactions receptor residues. NTM-006 inhibits Acetic acid-induced writhing responses in mice. NTM-006 can be used for the research of chronic neuropathic pain, cancer-related pain, osteoarthritis-associated pain.

IDO1-IN-31 (Compound 17g) is an IDO1 agonist with an IC50 of 77 nM. IDO1-IN-31 can be used for the study of neurological diseases and cancers.

Fumarranol, a Fumagillin analogue, is a selective type 2 methionine aminopeptidase (MetAP2) inhibitor with a human IC50 of 3.2 μM. Fumarranol inhibits proliferation of bovine aortic endothelial cells and inhibits angiogenesis in a mouse matrigel plug model. Fumarranol can be used for the researches of cancer, diabetic retinopathy, age-related macular degeneration.

Flubeneteram is a succinate dehydrogenase inhibitor with an IC50 of 0.0484 μM. Flubeneteram disrupts succinate dehydrogenase activity. Flubeneteram demonstrates protective effects against Rhizoctonia solani and Sphaerotheca fuliginea in preclinical models. Flubeneteram can be used for research related to fungal infections.

CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.

ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity.

cis-3-(Aminomethyl)cyclobutanol hydrochloride is a PROTAC linker that can be used in the synthesis of PROTACs.

C11-BODIPY 505/515 Glucosyl ceramide is a C11-BODIPY 505/515-labeled Glucosyl ceramide that can be used to prepare lipid nanoparticles for drug delivery (Ex/Em = 505/515 nm).

Antioxidant 245 (AO-245) is a hindered phenol antioxidant. Antioxidant 245 can be used in the research of nanocomposites.

9-Deoxyforskolin (compound 2) is a labdane-type diterpenoid, and also a forskolin derivative identified in hairy root cultures of Coleus forskohlii.

5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases.

1954U89 is a potent, lipid-soluble and orally active inhibitor of dihydrofolate reductase (DHFR). 1954U89 exhibits anticancer activity.

1-(2-(But-3-yn-1-yloxy)ethoxy)-6-chlorohexane is a PROTAC linker that can be used in the synthesis of PROTACs.

Org 6582 is a competitive, selective, and long-acting 5-HT (Ki = 89 nM) uptake inhibitor. Org 6582’s inhibitory effect on 5-HT uptake can last for more than 48 hours. Org 6582 can be used for research on depressive disorders.

8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.

5-Hydroxy-6-methoxy (S)-duloxetine maleate is an orally active and brain-penetrant serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with antidepressant and analgesic activities. 5-Hydroxy-6-methoxy (S)-duloxetine maleate is promising for research of psychiatric and neurological disorders such as depression, diabetic neuropathic pain, generalized anxiety disorder, and fibromyalgia.

TKS 159 is a 5-HT4 receptor agonist. TKS 159 can promote gastrointestinal motility. TKS 159 can be used for research on gastrointestinal conditions.

SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.

BVT-74316 is a 5-HT6 receptor antagonist. BVT-74316 can reduce food intake and bodyweight gain in rodent models. BVT-74316 can be used for the research of metabolic disease, such as obesity.

Batoprazine (8-(1-piperazinyl)-2H-1-benzopyran-2-one)) is a 5-HT1A,1B receptor agonist. Batoprazine can replace the behavioral stimulus of eltoprazine in the two-lever operant discrimination test between eltoprazine and deionized water in rats (ED50: 0.20 mg/kg).

GSK-163090 (dihydrochloride) is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK-163090 (dihydrochloride) inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK-163090 (dihydrochloride) has antidepressant and anxiolytic activities.

BMS-505130 (fumarate) is a potent, selective and orally active serotonin transport inhibitor with a Ki for binding to the serotonin transporter of 0.18 nM (Ki for norepinephrine and dopamine transporters of 4.6 and 2.1 μM, respectively). BMS-505130 (fumarate) can be used for the research of neurological disease, such as depression.

KW-5092 (fumarete) is a gastrokinetic agent. KW-5092 (fumarete) can increase intraluminal 5-HT release via the stimulation of cholinergic neurons .

RS-56812 is a partial agonist of the 5-HT3 receptor. RS-56812 significantly enhances the propulsive peristalsis of the colon. RS-56812 indirectly enhances cholinergic neurotransmission and improves the working memory performance of non-human primates. RS-56812 is used in research on diarrhea/colon peristalsis and cognitive disorders (such as Alzheimer's disease).

GR 55562 is a selective 5-HT1B receptor antagonist. GR 55562 can be used for the research of nerve disease.