endometrial

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.

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.

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.

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

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.

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).

Nomegestrol acetate is a widely used progestin-like drug,which is characterized as a full agonist at the progesterone receptor

GRP75-IN-1 hydrochloride (compound 33) is an agent for combating endometrial cancer (EC) by inducing apoptosis. It functions by targeting GRP75 and disrupting its interaction with IP3R, resulting in reduced Ca2+ levels in the mitochondria.

Melengestrol acetate-d3 is a deuterated compound of Melengestrol acetate. Melengestrol acetate has a CAS number of 2919-66-6. 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.

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].

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].

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg kg.

Zilovertamab (UC-961) is a humanized anti-ROR1 monoclonal antibody that cuts off the WNT5A-induced ROR1 signaling pathway and shows anti-proliferative activity in ovarian and endometrial cancer cells. It can be used to study lymphatic cancer.

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.

α-Cortolone, a metabolite of the glucocorticoid cortisol (hydrocortisone), is produced through the action of 20α-hydroxysteroid dehydrogenase (20α-HSD) via a tetrahydrocortisone (THE) intermediate. Studies indicate that urinary levels of α-cortolone are reduced in patients experiencing severe anorexia nervosa and postmenopausal women diagnosed with endometrial adenocarcinoma, in comparison to postmenopausal women without the condition.

Medroxyprogesterone 17-Acetate-d3 is a deuterated compound of Medroxyprogesterone 17-Acetate. Medroxyprogesterone 17-Acetate has a CAS number of 71-58-9. Medroxyprogesterone acetate 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-d3 is a deuterated compound of Megestrol Acetate. Megestrol Acetate has a CAS number of 595-33-5. Megestrol acetate 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.

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].

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.

Dostarlimab (TSR-042) is a programmed cell death protein 1 (PD-1) receptor immune checkpoint inhibitor that blocks interactions with PD-L1 and PD-L2, used in the study of endometrial cancer.

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

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.

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