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.

WR 151327 is an orally active radiation and chemoprotection protector. WR 151327 can suppress expression of HIV. WR 151327 can be used for the researches of infection and cancer.

Daledalin (UK 3557) is an orally active indoline antidepressant targeting noradrenaline and serotonin transporters in the brain. Daledalin enhances central monoaminergic neurotransmission to alleviate depressive symptoms. Daledalin is proming for rasearch of depression, including endogenous and neurotic depression.

Rivanicline (RJR-2403) hydrochloride is a neuronal nicotinic receptor agonist. Rivanicline hydrochloride is highly selective for the rat brain cortex nAChRs (Ki = 26 nM, EC50 of 732 nM) and α4β2 subtype (Ki = 26 nM, EC50 = 16 μM). Rivanicline hydrochloride can significantly restore the learning impairment and cognitive dysfunction. Rivanicline hydrochloride can be used for the study of neurodegenerative diseases (such as schizophrenia or Alzheimer's disease).

TC-2559 free base is a α4β2 nicotinic acetylcholine receptor (nAChR) agonists with an EC50 of 0.18 μM. TC-2559 free base shows much weaker potencies on the group of b4-containing nAChR subtypes, α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. TC-2559 free base can increase the discharge of dopamine cells in the ventral tegmental area (VTA) of rats in vitro, enhancing the excitability and aggressive behavior of VTA dopamine neurons. TC-2559 free base inhibits STAT3 to exert anti-inflammatory properties and relieves mice mechanical allodynia and improve rats cognitive deficits. TC-2559 free base can be used for the study of nerve pain.

(E/Z)-Rivanicline ((E/Z)-RJR-2403, (E/Z)-Metanicotine) is the E/Z mixture of Rivanicline). Rivanicline is a neuronal nicotinic receptor (neuronal nicotinic receptor) agonist that is highly selective for the α4β2 subtype, Ki is 26 nM, which is more than 1000 times more inhibitory than α7 receptor.

IKZF1/3 ligand-1 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC IKZF1/3 Degrader-1. PROTAC IKZF1/3 Degrader-1 is a potent IKZF1/3 PROTAC degrader with neuroprotective activity.

BCL6 ligand-5 (Compound 37) is a BCL6 ligand. BCL6 ligand-5 can be used as a ligand for target protein for PROTAC to develop and design degraders for PROTAC BCL6, such as PROTAC BCL6 Degrader-2. BCL6 ligand-5 can also be used in tumor research.

DEL1187-126-28-16 is a JAK3 inhibitor with IC50s of 10 and 0.97 nM against JAK3 WT in 0 and 60 min. DEL1187-126-28-16 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-28-16 can be used for the study of immune-mediated diseases.

CLT-28643 is an integrin α5β1 inhibitor. CLT-28643 can inhibit the high expression of integrin α5β1 in the bleb at early time-points after surgery and promote wound healing process.

DNDI-6510 (Compound (S)-x38) is a non-covalent SARS-CoV-2 MPro inhibitor with a IC50 of 0.04 μM. DNDI-6510 has a potent antiviral activity across SARS-CoV-2 and its variants as well as a weak efficacy to SARS-CoV-1. DNDI-6510 significantly improves drug exposure in metabolically humanized mice model (8HUM).

TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.