Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer.

LNS8801 is an orally active agonist of the G protein-coupled estrogen receptor (GPER). By activating GPER, LNS8801 mediates downstream signaling pathways, such as promoting the production of cyclic adenosine monophosphate (cAMP) and activating the cAMP response element-binding protein (CREB) signaling, thereby exerting anti-tumor activities including inhibiting tumor cell proliferation, inducing cell differentiation, and enhancing tumor immunogenicity. LNS8801 can be used in the research of various cancers (e.g., melanoma, pancreatic cancer, colorectal cancer, lung cancer, etc.) and relevant studies exploring the roles of GPER in normal physiological and pathological processes.

Hexolame is an estrogen receptors agonist with dual anticoagulant and estrogenic properties. Hexolame binds to estrogen receptors to induce anticoagulant effects by modulating clotting factors or platelet activity. Hexolame is promising for research of prostatic cancer and prevention of thrombosis.

GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research.

Estrone acetate (Hogival) is an estrogen derivative and an estrogen receptor (ER) activator. It promotes mammary gland development, stimulates pituitary prolactin secretion, and induces the proliferation and activation of lactotrophs (e.g., by reducing prolactin storage granule size while increasing rough endoplasmic reticulum and Golgi apparatus volume density). Estrone acetate holds potential for endocrine research, particularly in studying estrogen's effects on pituitary function, prolactin regulation, and mammary tumor models.

2,3,4-Trihydroxybenzophenone is a hydroxylated benzophenone UV filter with estrogenic activity. 2,3,4-Trihydroxybenzophenone is a quorum sensing inhibitor and an EC 1.14.18.1 (tyrosinase) inhibitor. 2,3,4-Trihydroxybenzophenone is also a human urinary metabolite, a rat metabolite and a drug metabolite.

(E/Z)-Panomifene (hydrochloride) is an orally active tamoxifen (TMX), thereby suppressing tumor growth both in vitro and in vivo.

(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity.

NSC308848 is a potent apoptosis inducer in a Myc-dependent manner. NSC308848 inhibits Myc transactivation and interferes with the DNA-binding activity of Myc family proteins.

KL4-219A is a selective covalent oncogenic transcription factor MYC degrader. KL4-219A potently and durably degrades MYC in cancer cells. KL4-219A binds covalently to MYC at C203, leading to the destabilization of MYC and subsequent proteasome-dependent degradation. KL4-219A is promising for research of cancers driven by MYC overexpression.

Cotylenin A is a type of phenanthraquinone compound that works alongside vitamin K2 to induce the differentiation of monocytes and halt their growth, while also inhibiting the expression of c-Myc and inducing the expression of cyclin G2 in human leukemia HL-60 cells. Cotylenin A can be used in studies on acute myeloid leukemia.

(-)-CMLD010509 ((-)-SDS-1-021) is an isomer of CMLD010509 (SDS-1-021). DOTAGA-FAP-2286-ALB is a selective fibroblast activation protein (FAP) inhibitor with an IC50 value of 67.5 nM. DOTAGA-FAP-2286-ALB enhances tumor retention via albumin interaction, prolonging blood circulation and improving radiometal complex stability (e.g., with 111In and 225Ac). DOTAGA-FAP-2286-ALB is promising for research of radionuclide therapy (TRT) of FAP-positive solid tumors.

Verproside, a catalpol derivative iridoid glycoside isolated from the genus Pseudolysimachion, represses TNF-α -induced MUC5AC expression by inhibiting NF-κB activation via the IKK/IκB signaling cascade. Verproside has potent anti-inflammatory, antioxidant, antinociceptive and anti-asthmatic activities. Verproside has the potential for the study of chronic obstructive pulmonary disease (COPD).

MJ210 is a modulator of the NF-κB and MAPK pathways with oral activity and the ability to penetrate the blood-brain barrier, and it exhibits neuroprotective activity. In vitro, 5 μM of MJ210 can increase the survival rate of SH-SY5Y cells treated with Rotenone to 81.9% and reduce the level of ROS, etc. In vivo, 5 mg/kg of MJ210 can improve the motor impairment in a rat model of Parkinson's disease. MJ210 can be used in the research of neurological diseases, such as Parkinson's disease.

MAY0132 is a potent and selective EPAC2 inhibitor with an IC50 of 0.4 μM. MAY0132 significantly inhibits replication of HMPV, AdV and RSV, reduces viral infection-induced cytokine/chemokine production, and inhibits NF-κB activation. MAY0132 has antiviral activity and can be used in the study of respiratory virus infection.

DBMB is an inhibitor of spleen tyrosine kinase (Syk), capable of significantly inhibiting the activity of Syk kinase. DBMB exhibits anti-inflammatory activity by suppressing the signaling of NF-κB, which in turn reduces the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB can be utilized in research on inflammatory diseases.

BS-153 is a novel synthetic oxazolidinone agent with anti-inflammatory activities by blocking the activation of the NF-κB/PKCθ pathway. BS-153 inhibits the expression levels of iNOS and COX-2 and pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) on LPS-stimulated RAW264.7 cells.

Bengamide B is an inhibitor for NF-κB with an IC50 of 85 nM. Bengamide B inhibits LPS-induced expression of TNF-α, IL-6 and MCP-1, exhibits anti-inflammatory activity. Bengamide B exhibits antitumor efficacy (IC50 for HCT-116 is 2 nM).

Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis.

(S,R,S)-AHPC-Boc derivative 1 (Compound 80-9; VH032-Boc derivative 1) is a selective proteasomal degrader targeting MALT1, which recruits the E3 ubiquitin ligase CRBN to form a ternary complex with MALT1, leading to ubiquitination and subsequent proteasomal degradation of MALT1. (S,R,S)-AHPC-Boc derivative 1 inhibits the NF-κB signaling pathway by disrupting the CBM complex, demonstrating potential for inducing apoptosis in ABC-DLBCL cells. (S,R,S)-AHPC-Boc derivative 1 is promising for research of MALT1-dependent cancers, such as diffuse large B-cell lymphoma (DLBCL).

RWJ-58643 hydrochloride is a β-trypsin inhibitor that inhibits allergic inflammation. RWJ-58643 hydrochloride (1 g) significantly reduces nasal allergy symptoms, eosinophil infiltration, and IL-5 levels at low doses. RWJ-58643 hydrochloride causes late eosinophilia and elevated IL-5 levels at high doses (300 mg and 600 mg). RWJ-58643 hydrochloride modulates allergic reactions by inhibiting the release of β-trypsin from mast cells.

L-Isoleucyl-L-valine (Ile-Val) is a dipeptide that induces the bovine trypsinogen-trypsin transition.

Benzamidine is a reversible competitive trypsin inhibitor with a Ki of 19 μM. Benzamidine shows inhibitory activity against homogeneous boar sperm acrosin with a Ki of 4 μM.

Plodicitinib is a Janus tyrosine kinase 3/TEC family kinase inhibitor with anti-inflammatory activity.

Yakuchinone B is an Acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitor with hypocholesterolemic activity, which is found in the seeds of Zingiberaceae. Yakuchinone B inhibits rat hepatic ACAT with an IC50 value of 20.6 μM. Yakuchinone B is promising for research of hypercholesterolemia and atherosclerosis.

Epicochlioquinone A can inhibit rat liver microsomal ACAT with IC50 of 1.7 μM, inhibit plasma lecithin cholesterol acyltransferase (LCAT) with IC50 of 15.8 μM, and inhibit cholesterol absorption in rats by 50% at 75 mg/kg.

Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras.

ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD).

BAY 74-4113 is a DGAT1 inhibitor (IC50: 72 nM). BAY 74-4113 can be used in obesity research.

ALT-007 is an orally effective serine palmitoyltransferase (SPT) inhibitor. SPT is the rate-limiting enzyme for the de novo synthesis of ceramide. In a mouse model of age-related sarcopenia, ALT-007 can effectively restore the muscle mass and function impaired by aging. ALT-007 may enhance protein homeostasis in Caenorhabditis elegans and mouse models of aging and age-related diseases and play the role of a ceramide inhibitor.