PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer.

Pegcantratinib (CT327) is a potent and selective TRKA antagonist with activity against TRKB and TRKC. Pegcantratinib can be used for research of CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, such as psoriasis and concomitant pruritus.

PD 168368 derivative-1 (Compound 16) is a derivative of PD 168368, with Ki values of 0.46 and 3.7 nM for the subtypes of bombesin receptor (BB₁ and BB₂). PD 168368 derivative-1 can be used for the study of various diseases, such as cancer, depression, and eating disorders.

Palmitoyl glutathione is a palmitoylated peptide derivative and a liver-targeted liposome-forming agent. Palmitoyl glutathione can form liposome-like vesicles with cholesterol, which can encapsulate water-soluble solutes and remain stable in fresh Rattus norvegicus (rat) plasma at 37°C. Palmitoyl glutathione can be used in studies related to acetaminophen-induced liver necrosis.

OPC 8490 is a stimulant. OPC 8490 has a positive inotropic effect. OPC 8490 can be used for research on heart failure.

Omega-3 acid ethyl esters (P-OM3) is a omega-3 polyunsaturated fatty acid. Omega-3 acid ethyl esters can be used for the researches of severe hypertriglyceridemia and cardiovascular diseases.

NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD).

NSC 660028 is a DNA topoisomerase II (DNA topoisomerase II) inhibitor with an ID50 of 50 μM. NSC 660028 inhibits DNA topoisomerase II and induces protein-linked DNA breaks. NSC 660028 can be used for cancer research.

NPSR1 modulator-1 is a NPSR1 modulator.

Niravoline (RU51599) is an arginine vasopressin (AVP) release inhibitor and a selective kappa opioid receptor agonist. Niravoline has a pure water diuresis effect without associated electrolyte excretion. Niravoline can reduce brain oedema following transient forebrain ischaemia in rats.

NHWL071065 is a IKZF1/IKZF3 degrader. NHWL071065 selectively degrades IKZF1 and IKZF3 in lymphoma cells via the ubiquitin-proteasome pathway. NHWL071065 inhibits the proliferation of lymphoma cells. NHWL071065 downregulates proteins involved in cytoskeleton assembly, cell adhesion and immune regulation in cells, while upregulating proteins related to the type I IFN signaling pathway. NHWL071065 can be used in the research of lymphoma.

NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer.

Neutrophil elastase-IN-7 (Compound 12) is an effective inhibitor of neutrophil elastase (HNE), with an IC50 value of 0.54 μM. Neutrophil elastase-IN-7 also exhibits significant inhibitory activity against various coagulation proteins, with the IC50 values for thrombin, FXa, FXIa, and FXIIIa being 8.2, 12.7, 1.2, and 5.7 μM, respectively. Neutrophil elastase-IN-7 can be used for research on inflammation, innate immune responses, and tissue remodeling.

ND-654 is a highly selective acetyl-CoA carboxylase (ACC) inhibitor (IC50: ACC1=3 nM, ACC2=8 nM). ND-654 reduces hepatic lipogenesis, decreases neutrophil recruitment and promotes anti-inflammatory M2 macrophage polarization. ND-654 is promising for research of nonalcoholic steatohepatitis and hepatocellular carcinoma.

N2-Succinyl-L-ornithine is a nucleoside metabolite.

N,N-Dimethyl psychosine is a derivative of Psychosine. N,N-Dimethyl psychosine can be used as an internal standard compound to quantify Psychosine in alkaline-treated lipid extracts.

MT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma.

MRS2339 is a ribose-modified nucleotide and a nucleotidase-resistant P2 receptor agonist. MRS2339 activates P2X4R in cardiomyocytes. MRS2339 induces ionic currents via cardiomyocyte P2X receptors, reduces cardiomyocyte cross-sectional area and heart weight/body weight ratio, lacks vasodilatory activity, and extends the lifespan of mice with cardiomyopathy. MRS2339 can be used in research related to heart failure and cardiomyopathy.

MLS-2384 free base is a dual JAK/Src kinase inhibitor. MLS-2384 free base downregulates STAT3 downstream proteins c-Myc and Mcl-1. MLS-2384 free base induces Apoptosis. MLS-2384 free base exhibits anticancer activity against prostate cancer, breast cancer, skin cancer, ovarian cancer, lung cancer, and liver cancer.

MK-0489 is an orally active, highly effective, and selective MC4R agonist. MK-0489 exhibits a strong binding affinity (IC50 = 13 nM) and functional agonist activity (EC50 = 4.6 nM) at human MC4R. MK-0489 shows functional activity of 22 nM (EC50) on mouse MC4R and 1.7 μM (EC50) on mouse MC3R. MK-0489 can be used for the study of obesity.

MINA53-IN-1 is a selective MINA53 inhibitor with an IC50 of 1.5 μM. MINA53-IN-1 induces DNA damage, cell cycle arrest and apoptosis in tumor cells. MINA53-IN-1 can be used for cancer research.

MG16 is a prodrug of 10-Methoxycamptothecin. MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer.

MDL 19205 is a cardiotonic agent with inotropic effect. MDL 19205 can be used for the research of cardiovascular disease, such as heart failure.

Lycorine methiodide (N-Methyllycorine iodide) is a derivative of Lycorine. Lycorine methiodide exhibits no significant in vitro antitumor activity against A549, OE21, Hs683, U373, SKMEL, and B16F10 cell lines, with all IC50 values greater than 10 μM.

LC-61 is a potent antileishmanial agent with an IC50 of 0.076 µM against intracellular L. infantum.

KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases.

KRP-203 monophosphate is a monophosphate of KRP-203. KRP-203 is an orally active sphingosine-1-phosphate receptor (S1PR) modulator that blocks the signal required by T cells to egress from lymph nodes and other lymphoid organs.

JRN73958 is a PI3K/Akt, MAPK, and NF-κB inhibitor. JRN73958 decreases LPS/IFNγ-induced PI3K/Akt, MAPK, and NF-κB activity. JRN73958 can be used for the research of leukemia.

JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease.

Immunosuppressant-2 (Example 21) is an orally active immunosuppressant. Immunosuppressant-2 significantly reduces the number of circulating lymphocytes. Immunosuppressant-2 can be used for research on various autoimmune diseases and organ transplant rejection.