X15695 is a potent, selective and orally active estrogen receptor alpha (ERα) degrader, destabilizes ERα and stabilizes p53, inhibits ER+ breast cancer cell growth.

SMIP34 (Small Molecule Inhibitor of PELP1 34) is a first-in-class, small molecule inhibitor of estrogen receptor (ER) coregulator PELP1, binds to (Kd=37.4 uM) and reduces PELP1 oncogenic functions.

SLU-PP-915 is a potent pan-ERR (Estrogen-related receptor) nuclear receptor agonist with EC50 of 414/435/378 nM for ERRα/ERRβ/ERRγ, respectively.

CIDD-0149897 is a potent, selective, brain permeable estrogen receptor beta (ERβ) agonist, 40-fold selective over ERα.

VPC-70619 (VPC70619) is a selective small-molecule inhibitor of N-Myc transcription in NMYC transcription inhibition assays.

NSC13728 hydrochloride is a specific small molecule stabilizer of the Max homodimer inhibiting Myc function, also inhibits Myc-Max heterodimerization.

NSC13728 is a specific small molecule stabilizer of the Max homodimer inhibiting Myc function, also inhibits Myc-Max heterodimerization.

MYRA-B (NSC45641) is a small molecule that induces Myc-dependent apoptosis without affecting Myc transactivation or Myc/Max DNA binding.

KSI-3716 is a small molecule c-MYC inhibitor that blocks c-MYC/MAX binding to target gene promoters, inhibits c-MYC mediated transcriptional activity at concentrations as low as 1 uM.

Isopomiferin is a prenylated isoflavonoid, collapses the tumor checkpoint module (TCM) and suppresses both MYCN and TEAD4 in MYCN-amplified NBL cells.

D089 is a selective small molecule stabilizer of the MYC G4-quadruplex, not only inhibits MYC expression in myeloma cell lines, but also selectively induces G1 arrest in MYC-driven cancer cell lines containing the MYC-G4 sequence.

GDU-952 is a novel small molecule aryl hydrocarbon receptor (AhR) agonist, activates and induces nuclear translocation of AhR.

UT-215 (UT215) is a small-molecule selective androgen receptor (AR) irreversible covalent antagonist, covalently and selectively bind to C406 and C327 in the AF-1 region of AR.

UT-105 is a small-molecule, irreversible, selective androgen receptor (AR) degrader (SARD) and irreversible inhibitor, binds to AR N-terminal domain (NTD) and inhibits both the AR and AR splice variants (AR-SVs).

SC428 (SC-428) is a small molecule androgen receptor (AR) signaling inhibitor, directly binds to the AR N-terminal domain (NTD) and exhibits pan-AR inhibitory effect.

M17-B15 is a potent, specific small molecule inhibitor of androgen receptor (AR) targeting the dimer interface pocket (DIP), inhibits AR transcriptional inhibition with IC50 of 0.03 uM.

JJ-450 is a novel analogue of IMTPPE and direct and specific inhibitor of androgen receptor (AR) transcriptional activity, blocks AR recruitment to androgen-responsive elements and suppresses AR target gene expression.

Faznolutamide is a potent, selective androgen receptor (AR) antagonist.

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expre

Promegestone (R-5020), a progestin, is a potent progesterone receptor (PR) agonist. Promegestone has the potential for endocrine regulation and cancer research.

VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104 decreased the levels of palmitoylated TEAD3 and TEAD4 and increased the levels of unpalmitoylated TEAD3 and TEAD4 in the human mesothelioma cell line NCI-H2373.VT104 exhibited inhibitory activity in more mesothelioma cell lines than the TEAD1-selective inhibitor VT103.VT104 (oral administration of 10 and 3 mg/kg) has very strong antitumor efficacy in the human mesothelioma NCI-H226 CDX model, with no effect on body weight gain.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

Tacalcitol is a synthetic vitamin D3 analog. This compound has been shown to regulate calcium levels and induce nerve growth factor production in epidermal keratinocytes. Additionally, Tacalcitol has been noted to promotes normal bone development by regul

Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist. Inecalcitol can induce cell apoptosis and has potent anticancer activities[3.

Elacestrant dihydrochloride (RAD1901 dihydrochloride) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

MB-07811 (VK-2809) is an orally bioavailable, liver-targeted prodrug of MB07344, which is a thyroid hormone receptor-beta agonist (TRβ) agonist, efficiently converted to MB07344 by liver microsomes in vivo.

PX-478 is an inhibitor of HIF-1a with an IC50 of 20-30μM enhances radiosensitivity of prostate carcinoma cells.

Bevurogant is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.

EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

LSZ102 is a potent, orally bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer.