steroidogenic

RJW100 is a compound that acts as a potent agonist of liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1), exhibiting pEC50 values of 6.6 and 7.5, respectively. Additionally, RJW100 induces robust activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

(Iso)-RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC 50 s of 6.4 and 7.2, respectively.

AC 45594 (4-Heptyloxyphenol) is an agonist of steroidogenic factor 1 (SF-1) ( IC50 : 50-100 nM)

Galeterone (VN 124) is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17, 20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

ML-180 (SR1848) is a potent inverse agonist of the orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) with an IC50 of 3.7 μM.

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

Diethylumbelliferyl phosphate (DEUP) is a potent and selective inhibitor of cholesterol esterase that does not inhibit protein kinase A activity in vitro. It disrupts steroidogenesis by blocking cholesterol transport to mitochondria in steroidogenic cells, with an IC50 of 11.6 μM. This compound may also limit the absorption of dietary cholesterol.

SID 7969543 is a selective SF-1 inhibitor with potential anticancer activity, inhibits SF-1-triggered luciferase expression and can be used for cancer research.

Propylparaben sodium (propyl parahydroxybenzoate) is a naturally occurring antimicrobial preservative found in plants and bacteria. Widely utilized in cosmetics, pharmaceuticals, and foods, this compound impairs antral follicle growth and steroidogenic function by modifying the cell-cycle, apoptosis, and steroidogenesis pathways. Additionally, propylparaben sodium reduces sperm count and motility in rats.

SS-RJW100 is an enantiomer of RJW100, known as a racemic agonist that targets two nuclear receptors: liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). In vitro experiments reveal that SS-RJW100 promotes the recruitment of coregulator protein fragments and enhances the interaction with the transcriptional intermediary factor 2 (Tif2) coactivator specifically for LRH-1. Additionally, SS-RJW100 disrupts the allosteric activation networks of LRH-1, displaying suboptimal thermal stability [1] [2].

BMS-351 is a potent and selective, nonsteroidal CYP17A1 lyase inhibitor with robust selectivity over steroidogenic CYPs 21A2 and 11B1. BMS-351 emerges as an outstanding preclinical candidate to treat CRPC and is likely to minimize the side effects of current therapies due to its exceptional selectivity. BMS-351 is potentially useful for the Treatment of Prostate Cancer.

RR-RJW100, an enantiomer of RJW100, functions as an agonist for both nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). Among its two synthesized enantiomers, RR-RJW100 and SS-RJW100, the former exhibits greater potency as an LRH-1 agonist. This compound plays a crucial role in regulating metabolic homeostasis and is utilized in researching diabetes, liver disease, and inflammatory bowel disease.

18-Hydroxycortisol, a cortisol derivative and steroidogenic intermediate, is an endogenous steroid secreted by the adrenal cortex. It serves as a useful biochemical marker in primary aldosteronism (PA) research [1].

Lys-γ3-MSH(human) TFA, a melanocortin peptide originating from the C-terminal fragment of pro-opiomelanocortin (POMC), enhances the steroidogenic response of rat adrenal glands to adrenocorticotrophin (ACTH). It is a potent stimulator of lipolysis, demonstrating an apparent EC50 of 3.56 nM, by activating hormone-sensitive lipase (HSL) and Perilipin A, leading to lipolysis [1] [2].

[Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an antagonist of arginine-vasopressin (AVP) that effectively reduces plasma aldosterone concentration in rats and is used to study the growth and steroidogenic capacity of the rat adrenal zona glomerulosa [1].

RFRP-3, mouse is a functional analog of avian Gonadotropin-Inhibitory Hormone (GnIH) that binds to GPR147. It reduces progesterone synthesis by inhibiting FSHR and key steroidogenic enzymes (P450scc, 3β-HSD, StAR). RFRP-3, mouse induces apoptosis by increasing p53 and can inhibit the ERK signaling pathway. Additionally, RFRP-3 is applicable in follicle development research.