Socrodeucitinib (Compound Example 58) is an orally active and selective tyrosine kinase 2 (TYK2) inhibitor with an IC50 value of 1.41 nM. Socrodeucitinib exerts anti-inflammatory activity by inhibiting TYK2-mediated cytokine signaling pathways and reducing the secretion of inflammatory factors. Socrodeucitinib is promising for research of autoimmune diseases such as psoriasis and inflammatory diseases.

ISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.

E0199 is a novel potent dual-target KV7/NaV modulator that activates the KV7 channel (KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels) while simultaneously blocks the NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. E0199 shows a potent analgesic effect without affecting heart and skeletal muscle ion channels critically in a chronic constriction injury (CCI) mouse model. E0199 can be used for Neuropathic pain (NP) research.

ZSA-215 is a potent and orally active STING agonist with an EC50 of 3.3 μM. ZSA-215 enhances STING signaling through promoting the phosphorylation of STING and interferon regulatory factor 3 (IRF3) and secretion of IFN-β. ZSA-215 inhibits tumor regression and long-term survival of mice in MC38 colon cancer model. ZSA-215 can be used to the study of colon cancerr.

Eprazole trisulfide dimer is a trisulfide dimer of Ilaprazole), an orally active proton pump inhibitor that irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Eprazole trisulfide dimer can be utilized in research on gastric ulcers.

TBS6b is a potent and selective ACKR3 molecular glue degrader. TBS6b degrades ACKR3 via the ubiquitin-proteasome pathway. TBS6b inhibits hepatocellular carcinoma cell proliferation, migration, and invasion. TBS6b is relevant to hepatocellular carcinoma (HCC) research.

Y-36912 is an orally active, highly selective and affinity 5-HT4 receptor agonist (Ki = 1.5 nM). Y-36912 can accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 can be used for research on gastrointestinal conditions.

DDS5 is a CD28 inhibitor with a kd of 175.57 µM. DDS5 significantly inhibits CD28-CD80 interaction (IC50: 332 µM). DDS5 can be used for research of immune-mediated diseases, including inflammatory bowel disease and rheumatoid arthritis.

MK-7337 is an α-synuclein PET ligand. MK-7337 labeled with 11C can be used as a PET tracer for neurodegenerative disorders like Parkinson’s disease imagination.

Azacyclohexane-C-piperazine-C(OCH3)2 is a PROTAC linker that can be used to synthesize PROTAC LRRK2 Degrader-4. PROTAC LRRK2 Degrader-4 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.

Azacyclohexane-O-cyclohexane-C-(OCH3)2 is a PROTAC linker that can be used to synthesize PROTAC LRRK2 Degrader-3. PROTAC LRRK2 Degrader-3 is a potent LRRK2 PROTAC degrader with anti-neuroinflammatory activity.

PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research.

LAB687 (Compound 2a) is a Microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.9  nM for the secretion of apoB from HepG2 cells. LAB687 is also a Smoothened (Smo) antagonist with IC50s of 2.48 and 3.42 μM for mouse and human Smo receptor, respectively. LAB687 can lower the level of triglycerides and LDL cholesterol and inhibits the Hedgehog signaling pathway.

BRL 35135 is a potent and selective β3-adrenergic receptor agonist. BRL 35135 can dose dependently increase energy expenditure, reduce weight, and only reduce fat without reducing muscle protein. BRL 35135 can significantly improve glucose tolerance and insulin sensitivity. BRL 35135 can be used to study metabolic conditions such as obesity and diabetes.

Bromomonilicin is a selective fungal cell membrane inhibitor. Bromomonilicin exerts antifungal activity by disrupting fungal cell membrane integrity. Bromomonilicin is promising for research of plant pathogenic fungal infections (e.g., Monilinia fructicola-induced brown rot) and superficial mycoses (e.g., dermatophyte infections).

KW-4490 is a selective phosphodiesterase 4 (PDE4) inhibitor. KW-4490 can be used for the researches of inflammation and immunology, such as asthma.

SKLB-11A is a selective, orally active and allosteric SIRT3 (sirtuin 3) agonist with a Kd value of 4.7 μM. SKLB-11A is highly selective for other members of the SIRT family. SKLB-11A activates autophagy-related signaling pathways, prevents mitochondrial dysfunction, improves cardiac function in Doxorubicin)-induced cardiotoxicity and myocardial ischemia/reperfusion models.

CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.

PQ32 is an antitumor agent that targets c-MYC Pu27 and KRAS G-quadruplexes. PQ32 inhibits tumor cell proliferation, arrests the cell cycle at the G2 phase, and induces apoptosis. PQ32 inhibits the expression of c-MYC and KRAS genes. PQ32 can inhibit tumor growth in mice and is used in the study of lymphoma, breast cancer, lung cancer, hepatocellular carcinoma, colorectal cancer, and other cancers.

SB 247083 is a selective, competitive and orally active endothelin-A receptor antagonist with a Ki of 0.41 nM. SB 247083 shows a Ki of 467 nM to endothelin-B receptor. SB 247083 shows a Kb of 3.5 nM for ET-1-induced contraction of rat aorta. SB 247083 can be used for the research of cardiovascular disease.

TH10184 is a NUDT5 inhibitor. TH10184 can be conjugated with VH032 and linker to synthesize PROTAC NUDT5 degrader DDD2

TH10184-octanedioic acid is a conjugate of the NUDT5 ligand and the linker. TH10184-octanedioic acid can be used for synthesizing PROTAC NUDT5 degrader DDD2

IITZ-02 is a lysosomotropic Autophagy inhibitor. IITZ-02 enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally inducing the inhibition of autophagy. IITZ-02 abolishes mitochondrial membrane potential and induces apoptosis through the mitochondria-mediated pathway. IITZ-02 has a potent antitumor activity in MDA-MB-231 xenograft mouse models. IITZ-02 can be used for cancers research.

CGS-30440 is a potent and orally active dual inhibitor of neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE). CGS-30440 exhibit antihypertensive and natriuretic effects. CGS-30440 also shows protective effect for chronic renal failure. CGS-30440 can be used for the research of cardiovascular disease, such as hypertension.

mTOR inhibitor-28 (SM-3) is a potent mTOR inhibitor. mTOR inhibitor-28 inhibits A549, H292, and H460 cells with IC50s of 72.74, 67.66, and 43.24 μM, respectively.

ML247 is a non-inhibitory and selective small molecule chaperone of acid alpha glucosidase. ML247 can be used for the research of metabolic disease, such as Pompe disease.

ent-Epanorin is an enantiomer of Epanorin ent-Epanorin has more potent antibacterial and antiparasitic activity against Bacillus subtilis (ATCC 6633), Staphylococcus aureus (ATCC 25923) and Giardiaduodenalis 713 compared to Epanorin.

SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer.

Ocipumaltib (Example 2) is an inhibitor of mucosa associated lymphoid tissue protein 1 (MALT1). Ocipumaltib is an antitumor agent. Ocipumaltib can be studied in research for cancer, infection, neurological and hematological diseases.

BU08028 is a dual-functional agonist that targets both the μ-opioid peptide receptor (MOP) and the neuropeptide FQ receptor (NOP). BU08028 activates the inhibitory G protein (Giα), thereby inhibiting the activity of adenylate cyclase (AC), resulting in a decrease in intracellular second messenger cyclic adenosine monophosphate (cAMP) levels, and suppressing the generation and transmission of pain signals. BU08028 can take effect within 30 minutes in mouse models of neuropathic pain and inflammatory pain, and its analgesic effect can last for up to 24 hours. BU08028 has excellent safety, no addiction, respiratory depression, or side effects. BU08028 can be used for pain research.