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Catalog No.
Product Name
Application
Product Information
Citations
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ACE inhibitor
Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.- E Saman, .et al. , Physiol Res, 2025, Dec 31;74(Suppl 2):S231-S244 PMID: 41532630
- Sona Cacanyiova, .et al. , Biol Res, 2023, Oct 25;56(1):55 PMID: 37875978
- Tomas Jasenovec, .et al. , Biomedicines, 2021, Dec 14;9(12):1902 PMID: 34944718
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Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
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Renin inhibitor
Aliskiren is an orally active, synthetic nonpeptide renin inhibitor.- Karibe T, .et al. , Drug Metab Dispos, 2018, May;46(5):667-679 PMID: 29358184
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dual 5alpha-reductase inhibitor
Dutasteride is a dual 5-a reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).- Makoto Ishikawa, .et al. , Sci Rep, 2018, 8: 12851 PMID: 30150786
- Makoto Ishikawa, .et al. , Neuropharmacology, 2016, Dec; 111: 142-159 PMID: 27596950
- Makoto Ishikawa, .et al. , Invest Ophthalmol Vis Sci, 2014, 55(12): 8531-8541 PMID: 25406290
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RNA polymerase inhibitor
Antibiotic; inhibits bacterial RNA polymerase. Prototypical activator of the pregnane X receptor (PXR).- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
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AR inhibitor downregulator
AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.- Qian Liu, .et al. , Nat Commun, 2024, Feb 7;15(1):1148 PMID: 38326303
- Soumitra Ghosh, .et al. , bioRxiv, 2023, Jun 28:2023.06.28.546870 PMID: 37425957
- Qian Liu, .et al. , Research Square, 2023, Mar 10
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Aromatase inhibitor
Fadrozole is a nonsteroidal aromatase inhibitor exhibiting a very potent and selective inhibitory effect of the aromatase enzyme system in vivo and estrogen biosynthesis in vivo.- Steve U. Ayobahan, .et al. , Sci Rep, 2019, 9, Article number: 6599 PMID: 31036921
- Muth-Köhne E, .et al. , Aquat Toxicol, 2016, Jul;176:116-27 PMID: 27130971
- Ma YN, .et al. , Aquat Toxicol, 2016, Oct;179:55-64 PMID: 27571716
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Aromatase inhibitor
Letrozole is an Aromatase inhibitor. CGS 20267 is a new non-steroidal compound which potently inhibits aromatase in vitro (IC50 of 11.5 nM) and in vivo (ED50 of 1?€?3 μg/kg p.o.)- WEI LIU, .et al. , Exp Ther Med, 2015, Oct; 10(4): 1297-1302 PMID: 26622481
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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GPR3 agonist/NOS/ NADPH oxidases inhibitor
Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells. -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
renin inhibitor
Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren, which is a direct renin inhibitor approved for the treatment of essential hypertension. -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
HMG-CoA Reductase inhibitor
Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.
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ACE inhibitor/Beta blocker
Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. -
ACE inhibitor
Cilazapril is a pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure. -
ACE inhibitor
Fosinopril is an angiotensin converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of chronic heart failure. -
GPR40 Inhibitor
GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors. -
CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
LTA4 hydrolase inhibitor
Captopril Disulfide is a reversible and competitive inhibitor of LTA4 hydrolase (IC50=11 M). Captopril has been shown to be an of angiotensin converting enzyme-1 (ACE1), but not ACE2(IC50 = 22 nM). -
ACE inhibitor
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. -
Renin inhibitor
VTP-27999 HCl is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin. -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
5 alpha-reductase inhibitor
Epristeride is a selective and specific uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. -
aromatase inhibitor
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively. -
angiotensin-converting enzyme inhibitor
Lisinopril (MK-521) is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks. -
Aromatase inhibitor
Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM. -
Smurf1 inhibitor
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation. -
ACE inhibitor
Imidaprilate is an active metabolite of TA-6366, acts as a potent angiotensin converting enzyme (ACE) inhibitor, with an IC50 of 2.6 nM, and is used in the research of hypertensive disease. -
ACE inhibitor
H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM. -
RORγt inhibitor
S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production. -
Renin inhibitor
VTP-27999 2,2,2-trifluoroacetate is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases. -
Enkephalin-degrading and ACE inhibitor
Spinorphin is an endogenous factor that exhibits inhibitory effects on enkephalin-degrading enzymes. -
LXRα inhibitor
(20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects. -
RORγt inhibitor
AGN-242428, also known as VTP-43742, is a potent, selective and orally active RORγt inhibitor for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis. -
Androgen Receptor Inhibitor
SC428 is a selective androgen receptor (AR) inhibitor that targets the N-terminal domain, effectively reducing the transactivation of various isoforms including AR-V7, AR-v567es, and full-length AR (AR-FL) along with its LBD mutants. This compound inhibits the nuclear translocation, chromatin binding, and subsequent transcription of AR-regulated genes in response to androgens. Additionally, SC428 demonstrates significant anti-proliferative effects on tumor cells in vitro and promotes apoptosis in vivo, particularly in mice bearing 22RV1 xenografts. Its application in cancer research highlights its potential utility in targeting androgen-dependent tumors. -
ERα Inhibitor
Isocurcumenol is an estrogen receptor alpha (ERα) inhibitor derived from the rhizomes of Curcuma zedoaria. It demonstrates significant anti-tumor activity, exhibiting IC50 values of 99.1 μg/mL in Dalton's lymphoma ascites (DLA) cells and 178.2 μg/mL in KB cells. This compound has potential applications in cancer research, particularly in exploring targeted therapies for hormone-dependent tumors. -
GR/IL-6 Inhibitor
Glucocorticoid receptor/IL-6-IN-1 is a selective dual inhibitor that targets both the glucocorticoid receptor (GR) and the IL-6 signaling pathway, demonstrating IC50 values of 120 nM and 59 nM, respectively. This compound effectively inhibits IL-6-induced phosphorylation of JAK/STAT3, thereby blocking the transcription of inflammatory cytokines. Glucocorticoid receptor/IL-6-IN-1 is a valuable tool for investigating inflammatory diseases, including rheumatoid arthritis and asthma. -
Renin Inhibitor
Aliskiren fumarate is a potent and selective renin inhibitor with an IC50 of 1.5 nM. It is primarily utilized in research related to hypertension and cardiovascular diseases, as well as cancer cachexia. Its mechanism of action involves the inhibition of renin, a key enzyme in the regulation of blood pressure, making it an important tool for studying these conditions. -
Renin Inhibitor
Aliskiren hydrochloride is a potent and selective renin inhibitor, exhibiting an IC50 of 1.5 nM. This compound is widely used in the study of hypertension and cardiovascular diseases, as well as in research related to cancer cachexia. Its ability to modulate renin activity makes it a valuable tool for exploring the pathophysiological mechanisms underlying these conditions. -
HGPRT Inhibitor
8-Azahypoxanthine is a purine analog that functions as an inhibitor of hypoxanthine-guanine phosphoribosyltransferase (HGPRT). This compound demonstrates antitumor activity, making it a valuable tool in cancer research, particularly for studying adenocarcinoma and other tumor types. Its ability to inhibit HGPRT may provide insights into the mechanisms of tumor growth and potential therapeutic strategies. -
GR/IL-6 Inhibitor
Glucocorticoid receptor/IL-6-IN-2 is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and the IL-6 signaling pathway, with IC50 values of 40 nM and 19 nM, respectively. This compound has demonstrated significant potential in inhibiting inflammatory responses, making it a valuable tool for research into inflammatory diseases such as rheumatoid arthritis and asthma. Its unique mechanism of action allows for exploration of therapeutic strategies aimed at modulating immune responses and mitigating chronic inflammation. -
Androgen Receptor Inhibitor
Androgen receptor-IN-7 is a potent inhibitor of the androgen receptor (AR), demonstrating significant anticancer activity against PC-3 (IC50 = 370.37 nM) and LNCaP cell lines through both AR-dependent and AR-independent mechanisms. This compound induces reactive oxygen species (ROS) production in PC-3 cells, highlighting its potential role in oncological studies. Androgen receptor-IN-7 is useful for research focused on prostate cancer and related therapeutic strategies.
