endometrial

PF-02413873 is a competitive antagonist of nonsteroidal progesterone receptor with a Ki of 2.6 nM. PF-02413873 can be used in studies about the treatment of gynecological conditions such as endometriosis.

Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist that acts on D2 (Ki: 0.56 nM), D3 (Ki: 0.43 nM), and 5-HT2A (Ki: 0.6 nM) receptors, and also binds Alpha-1A adrenergic receptors. It can induce apoptosis, inhibit cancer cell proliferation, and is used to study psychiatric disorders, cancer, and inflammation.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Medroxyprogesterone Acetate (Farlutin) is a synthetic progestin that is derived from 17-hydroxyprogesterone. It is a long-acting contraceptive that is effective both orally or by intramuscular injection and has also been used to treat breast and endometrial neoplasms.

Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Ulipristal acetate (CDB-2914) is an orally bioavailable selective progesterone receptor modulator with anti-progesterone activity. It binds to the progesterone receptor (PR), inhibiting PR-mediated gene expression and interfering with progesterone activity in the reproductive system, potentially suppressing the growth of uterine leiomyomatosis. Additionally, ulipristal can be used as emergency contraception by inhibiting or delaying ovulation and affecting endometrial tissue.

Etonogestrel (Implanon) is a steroidal progestin used as hormonal contraceptives.

EC359 is a potent and selective inhibitor of leukemia inhibitory factor receptor (LIFR), a potent inhibitor with anticancer activity, blocks LIF LIFR interaction, and can be used in the study of leukemia and endometrial cancer.

Gestonorone Capronate  is a progesterone used to treat benign prostatic hyperplasia and endometrial cancer.

Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.

4'-Hydroxytamoxifen TFA, a salt form of a metabolite of Tamoxifen, demonstrates higher affinity for ER compared to Tamoxifen itself. This compound induces non-apoptotic cytotoxicity in human endometrial adenocarcinoma cells.

Trimegestone, a highly effective oral progestogen, is used for endometrial protection, all doses inducing secretory endometrial transformation.

GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.

17-Epiestriol is a metabolite of estrone .1It is formed from estroneviaa 16α-hydroxy estrone intermediate by reduction of the C-17 ketone. 17-Epiestriol binds to estrogen receptor α (ERα) and ERβ with relative binding affinities of 29 and 80 compared with 17β-estradiol .2 1.Brinton, L.A., Trabert, B., Anderson, G.L., et al.Serum estrogens and estrogen metabolites and endometrial cancer risk among postmenopausal womenCancer Epidemiol. Biomarkers Prev.25(7)1081-1089(2016) 2.Kuiper, G.G.J.M., Lemmen, J.G., Carlsson, B., et al.Interaction of estrogenic chemicals and phytoestrogens with estrogen receptor βEndocrinology139(10)4252-4263(1998)

ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. It inhibits DNA relaxation with an IC50 of 2 μM, compared to 120 μM for Etoposide. ARN-21934 exhibits favorable in vivo pharmacokinetic properties and shows promise in anticancer research, displaying affinity for topoIIα with an IC50 of 2 μM and for topoIIβ with an IC50 of 120 μM. It demonstrates activity against human cancer cell lines including melanoma (A375: 12.6 μM, G-361: 8.1 μM), breast (MCF7: 15.8 μM), endometrial (HeLa: 38.2 μM), lung (A549: 17.1 μM), and prostate (DU145: 11.5 μM) cancer cells. Following a single intraperitoneal injection of 10 mg kg, ARN-21934 achieves a peak plasma concentration of 0.68 μg mL in 15 minutes, with a half-life of 149 minutes, and remains detectable in plasma and the brain for up to 360 minutes. [1] Jose Antonio Ortega, et al. Novel, Potent, and Druglike Tetrahydroquinazoline Inhibitor That Is Highly Selective for Human Topoisomerase II α over β. J Med Chem. 2020 Nov 12;63(21):12873-12886.

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK ATM Chk1 2 pathway, leading to inactivation of the Cd

Cridanimod can increase progesterone receptor (PR) expression, with potential antineoplastic adjuvant activity. Cridanimod is able to induce the expression of PR in endometrial cancer. In combination with a progestin, cancer cells could be eradicated thro

ENMD-1068 hydrochloride, a selective protease-activated receptor 2 (PAR2) antagonist, inhibits TGF-β1 Smad signaling, thereby reducing hepatic stellate cell activation and collagen expression. It also suppresses the proliferation of endometrial cells and triggers apoptosis in epithelial lesion cells. This compound is utilized in researching endometriosis and liver fibrosis [1] [2].

Steroid sulfatase-IN-2 is an active inhibitor of steroid sulfatase (STS), demonstrating an IC50 value of 109.5 nM. Its potential application lies in hormone-dependent cancer research, specifically estrogen-dependent breast and endometrial cancer [1].

Melengestrol acetate is a derivative of progesterone and acts as a corticosteroid hormone. Melengestrol acetate promotes endometrial proliferation delay of menstrual activity and pregnancy maintenance.

Zoptarelin doxorubicin, also known as AEZS-108, is an LHRH agonist. Zoptarelin doxorubicin is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Zoptarelin doxorubicin binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates into DNA and inhibits the topoisomerase II activity, which may result in the inhibition of tumor cell DNA replication and tumor cell proliferation

AEZS-112, also known as ZEN012, is an orally active small mol. anti-cancer drug which inhibits the polymn. of tubulin at low micromolar concns. AEZS 112 dose-dependently increased non-vital hypodiploid cells and the cytotoxic effect was least pronounced in G2 phase of the cell cycle, indicating cell death during mitosis, as detd. by FACS anal. AEZS 112 showed anti-tumor activity in human ovarian and endometrial cancer cell lines at low micromolar concns., which could not be abrogated by caspase inhibition and is therefore a good candidate for in vivo studies in these tumors.

Estradiol (β-Estradiol) hemihydrate, a key female sex hormone and steroid, plays a significant role in up-regulating neural markers in human endometrial stem cells (hEnSCs) and facilitating their neural differentiation. It is also utilized in research focused on cancers, neurodegenerative diseases, and neural tissue engineering.

Imlunestrant tosylate (LY-3484356) is a potent, orally active selective estrogen receptor degrader (SERD) with purely antagonistic properties, effectively inhibiting estrogen receptor (ER)-dependent gene transcription and cell growth. This compound is applicable in research on ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) [1] [2].