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.

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

Elacestrant (RAD-1901) is a novel, orally bioavailable small-molecule selective estrogen receptor degrader (SERD).

RBF197 (RBF-197) is a novel highly potent and selective eIF4A inhibitor, inhibits human eIF4A helicase activity with IC50 of 55.2 pM.

ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer.

ARV471 is an orally bioavailable estrogen receptor-targeting (ER-targeting) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer.

KYN-101 (KYN101) is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.

AS1842856 is a potent and cell-permeable Foxo1 inhibitor with an IC50 of 30 nM.

ATF3W-aeg peptide is a selective, peptide inhibitor of activating transcription factor 3 (ATF3) with high affinity (Kd=151 nM), increases CCL4 expression levels in human macrophages.

(E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.

Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis.

Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.

ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces hepatic collagen deposition and expression levels of fibrogenic markers such as α-smooth muscle actin and collagen type I alpha 1 chain in Western diet-fed mice. ODH-08 suppresses the expression of fibrogenic proteins in hepatic stellate cells (HSCs). ODH-08 suppresses the activity of SMAD2 and 3, which are the primary downstream proteins of transforming growth factor β.

MG-002 is a second-generation, orally bioavailable inhibitor of eIF4A, a key RNA helicase involved in the initiation of cap-dependent mRNA translation. By targeting eIF4A, MG-002 effectively disrupts the translation of certain mRNAs, particularly those with complex 5' untranslated regions (UTRs) that are highly dependent on eIF4A activity. This mechanism of action makes MG-002 a promising candidate for targeting cancers and other diseases driven by dysregulated translation.

1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).

HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.

SR2211 (SR-2211) is a potent, selective RORγ inverse agonist (Ki=105 nM, IC50=320 nM) that potently inhibits production of IL-17 in cells.

SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells).

SGC-CBP30 is a potent CREBBP/EP300 inhibitor with IC50 of 21 nM and 38 nM, respectively.

A endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro.

GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia.

RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM.

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.