Endocrinology/Hormones

<p>Akuammicine, as an indole alkaloid from Catharanthus roseus, can be used in cancer cell eradication.</p>

<p>RLA-5331: iron activator with anti-androgen properties; inhibits mCRPC cell proliferation.</p>

<p>AKR1Cs-IN-1 (Compound 29) is an effective and broad-spectrum inhibitor of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). It achieves subtype inhibition by simultaneously binding to the SP2 and SP3 pockets, thereby blocking metabolic pathways related to drug resistance. In enzyme assays, AKR1Cs-IN-1 exhibits significant inhibitory activity with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM for AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. The compound shows excellent resensitizing effects in doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, effectively enhancing the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on breast cancer resistance.</p>

<p>Osteostatin, derived from parathyroid hormone-related protein (PTHrP) 107-111, has demonstrated properties conducive to bone repair in animal models presenting</p>

<p>ER degrader 5: potent ER degrader, anti-cancer, for breast cancer research.</p>

<p>Dipropyl phthalate is a weak androgen receptor inhibitor, and can be used in biochemical experiments and drug synthesis.</p>

<p>PRL 2915 is a potent antagonist of the human somatostatin subtype 2 receptor (hsst 2), exhibiting a binding affinity (K_i) of 12 nM [1].</p>

<p>A unique collection of xnum potassium channel blockers and agonists for high throughput and high content screening;</p>

<p>CNP, from natriuretic family, first in pigs, now in other species, processes into CNP-22/CNP-53, similar to ANP/BNP, with varying potencies.</p>

<p>A unique collection of xnum compounds targeting histaminergic receptor and melatonin receptor for high throughput screening (HTS) and high content screening (HCS</p>

<p>PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group.</p>

<p>Tetrahydro Aldosterone is a steroidal compound that inhibits the adrenal angiotensin II receptor, with an IC50 of 10 μM.</p>

<p>PRO20 is a specific and competitive antagonist of the (pro)renin receptor (PRR). It inhibits the calcium influx induced by Proproin with an IC50 value of 81 nmol/L. By blocking the binding of Prorenin to PRR, PRO20 inhibits the activation of the renin-angiotensin system (RAS), reducing the production of angiotensin II (Ang II) and exerting antihypertensive effects. PRO20 holds promise for research in antihypertensive agents.</p>

<p>Potent GPR171 agonist (EC50 = 1.6 nM). ProSAAS-derived peptide. Regulates body weight in mice and promotes the outgrowth of neurites in Neuro2A cells.</p>

<p>ERα degrader10 is a potent, selective, orally active estrogen receptor α (ERα) degrader. It demonstrates strong ERα binding affinity (IC50 of 24.0 nM) and degradation capability (EC50 of 5.3 nM). This compound degrades ERα through a proteasome-mediated pathway and is utilized in breast cancer research.</p>

<p>UT receptor ligand acts mainly as silent antagonist with slight agonist effects; blocks U-II in rat aorta, pIC50 = 7.46, &amp; inhibits plasma leakage in mice.</p>

<p>EX-A5386 (Glucocorticoid receptor modulator-1) is a potent glucocorticoid receptor modulator, IC50/EC50&lt;100nM.</p>

<p>Imidaprilate, an active TA-6366 metabolite, is a potent ACE inhibitor with an IC50 of 2.6 nM, researched for hypertension.</p>

<p>[Sar1, Ile8]-Angiotensin II(3TFA) is a peptide that has multiple effects on vascular smooth muscle.</p>

<p>AKR1C3-IN-10 (compound 5r), a selective inhibitor of AKR1C3 with an IC50 of 51 nM, demonstrates efficacy in a prostate cancer xenograft model [1].</p>