regulation

Adenosine (D-Adenosine) is a natural product, a ribonucleoside consisting of adenine bound to ribose. Adenosine has vasodilatory, antiarrhythmic and analgesic effects.

Taurochenodeoxycholic Acid (12-Deoxycholyltaurine) is one of the main bioactive substances of animals' bile acid.

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).

ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.

Metergoline (Methergoline) is a dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for migraine disorder therapy.

Ecdysone is a major steroid hormone in insects and herbs. Ecdysone triggers mineralocorticoid receptor activation and induces cellular apoptosis. Ecdysone signaling through Ecdysone receptor isoform B1 is required cell autonomously for the muscle death.

Sodium taurocholate is a biologically active compound that can inhibit bile duct injury induced by hepatic artery ligation by upregulating VEGF-A expression. It also exhibits immunomodulatory effects and can be used to induce pancreatitis models.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

AZD9496 maleate is a highly potent and selective antagonist of the estrogen receptor alpha (ERα), exhibiting an IC50 value of 0.28 nM. This compound, AZD9496 maleate, is an orally bioavailable selective estrogen receptor degrader (SERD).

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

D18 is an immune modulator that acts as a dual agonist for TLR7/8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1/PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

3-Deazaneplanocin A HCl is a synthetically derived inhibitor of the histone methyltransferase (EZH2) and S-adenosylhomocysteine hydrolase (SAHH). By regulating epigenetic methylation pathways, 3-deazaneplanocin A induces apoptosis and inhibits tumor cell proliferation, demonstrating significant antitumor activity in various tumor models. 3-deazaneplanocin A HCl can be used in research on epigenetic regulation, tumorigenesis and progression, and stem cell differentiation.

Encorafenib (LGX818) is an oral, highly selective inhibitor of the BRAF V600E mutation with an IC50 of 0.3 nM, exhibiting antitumor activity. Encorafenib can be used for studying tumor signaling pathway regulation and mechanisms of drug resistance.

PLX5622 is an orally active small-molecule CSF1R inhibitor that selectively depletes microglia in the brains of mice and rats. It is commonly used to establish models related to microglia-associated neuroinflammation, neurodegenerative diseases (such as Alzheimer's disease and Parkinson's disease), brain injury, and neuroimmune regulation. This product is also available as a premixed diet version (C2005 PLX5622 in AIN-76A Diet (1200 ppm)), eliminating the need for self-preparation and offering superior stability and reproducibility.

Soquelitinib (CPI-818) is a covalent, irreversible, oral and selective ITK inhibitor that preferentially inhibits Th2 cytokine production over Th1, inhibits in vivo tumor growth in mice, and decreases markers of T-cell exhaustion, resulting in an increase in tumor infiltration and up-regulation of CXCR3, IFNγ, TNFα, and CD107a expression in normal CD8 cells.

Agomelatine (L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2), and Agomelatine (S-20098). L(+)-Tartaric acid also functions as a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native porcine and cloned human 5-HT2C receptors), actively supporting research into melatonergic signaling pathways, receptor-mediated regulation, and novel psychiatric therapeutics by enabling precise modulation of circadian and serotonergic systems in cellular models to improve neuropharmacological understanding and experimental reproducibility across neuroscientific and clinical translational studies.

BAY-784 is a potent gonadotropin-releasing hormone receptor (GnRH-R) antagonist that exhibits strong inhibitory activity with IC50 values of 21 nM for human GnRH-R and 24 nM for rat GnRH-R, BAY-784 is widely applied in endocrine research to study GnRH signaling, reproductive hormone regulation, and therapeutic modulation of hormone-dependent physiological and pathological processes.

INT-777 (S-EMCA) is a potent, selective TGR5 agonist with an EC₅₀ of 0.82 μM. Following subarachnoid hemorrhage in rats, INT-777 inhibits NLRP5-ASC inflammasome-mediated neuroinflammation via the TGR3/cAMP/PKA signaling pathway. INT-777 exhibits multiple effects, including metabolic regulation, anti-inflammatory activity, cholagogue effects, and vascular protection. INT-777 can be used in research on diseases such as metabolic syndrome, non-alcoholic fatty liver disease, inflammatory bowel disease, and pulmonary arterial hypertension.

nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a reversible inhibitor of arginase with anti-leukemic activity, effective in treating endothelial dysfunction, immunosuppression, and metabolism regulation.

β-Apo-13-carotenone, a naturally occurring apocarotenoid, functions as an antagonist of the retinoid X receptor (RXR). β-Apo-13-carotenone inhibits transactivation of RXRα but does not interfere with coactivator binding to the receptor in the manner observed for the known antagonist UVI3003. β-Apo-13-carotenone induces the formation of a transcriptionally silent RXR tetramer. β-Apo-13-carotenone is therefore relevant for mechanistic investigations involving nuclear receptor signaling, transcriptional regulation, and retinoid-associated cellular processes.

Dicirenone (SC26304) inhibits the Mineralocorticoid receptor (MR), aldosterone regulation of the urinary K+:Na+ ratio, and aldosterone binding to renal cytoplasmic and nuclear receptors.

0990CL is an effective heterotrimer Gαi subunit specific inhibitor, which can interact with purified Go± in GDP-bound state, and can block α2AR mediated cAMP regulation. In the cell model, low concentration of 0990CL could partially restore cAMP level, and high concentration of 0990CL (10μM) began to have negative effects on cell viability.

Triparanol (NSC-65345) interferes with posttranslational modification of Hedgehog signaling molecules as well as the sterol sensing domain of its receptor PTCH1, leading to down-regulation of Hedgehog signaling. Triparanol suppresses human tumor growth and is an antilipemic agent with high ophthalmic toxicity.