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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
3059 Results for "
Modulators
" in MedChemExpress (MCE) Product Catalog:
Products (3059)
3059 Results for "Modulators" in MCE Product Catalog:
Cat. No.: HY-P1764
CAS No.: 149146-12-3
Target:
Dopamine Receptor Caspase NOD-like Receptor (NLR) IGF-1R VEGFR FGFR AMPK ERK p38 MAPK JAK Bcl-2 Family STAT Apoptosis
Research Areas:
Secretoneurin, rat is a 33-amino acid neuropeptide produced by proteolytic processing of chromogranin II, widely distributed in the central and peripheral nervous systems, and its release is calcium-dependent. Secretoneurin, rat modulates the activities of caspase-3, caspase-1, the NLRP3 inflammasome, IGF-1R, VEGFR1, VEGFR2, FGFR3, AMPK, ERK1/2/MAPK, and Jak2/Stat3 pathways. Secretoneurin, rat regulates neuronal apoptosis, synaptic structure, inflammation, neurogenesis, angiogenesis, oxidative stress, cardiomyocyte hypertrophy, dopamine release, and cell migration and proliferation. Secretoneurin, rat is used in studies of global cerebral ischemia, myocardial infarction, stroke, and cardiac hypertrophy .
Cat. No.: HY-W002585R
CAS No.: 19916-73-5
O6-Benzylguanine Standard is the analytical standard of O6-Benzylguanine (HY-W002585). This product is intended for research and analytical applications. O6-Benzylguanine is an orally active, blood-brain barrier-penetrant inhibitor of O 6-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction .
Cat. No.: HY-W004464R
CAS No.: 20980-22-7
Category:
Cat. No.: HY-W004464S
CAS No.: 1309283-31-5
Research Areas:
2-(1-Piperazinyl)pyrimidine-d8 is the deuterated-labeled 2-(1-Piperazinyl)pyrimidine (HY-W004464). 2-(1-Piperazinyl)pyrimidine is an orally effective α2-adrenoceptor antagonist and 5-HT1A receptor agonist. 2-(1-Piperazinyl)pyrimidine is an in vivo metabolite related to buspirone. 2-(1-Piperazinyl)pyrimidine modulates excitatory synaptic transmission in the hippocampus and the release of monoamine transmitters such as norepinephrine and 5-HT by blocking α2-adrenoceptor and activating 5-HT1A Receptor. 2-(1-Piperazinyl)pyrimidine is used in research on psychiatric disorders such as anxiety and depression .
Cat. No.: HY-W015924R
CAS No.: 594-61-6
Cat. No.: HY-W130288
CAS No.: 57536-86-4
Research Areas:
1-(1-Naphthyl)piperazine is a 5-HT receptor modulator that acts as both a 5-HT2A receptor antagonist and 5-HT1A receptor agonist, and binds to human 5-HT6 receptor with a Ki of 120 nM. 1-(1-Naphthyl)piperazine partially inhibits forskolin-stimulated adenylate cyclase activity in calf substantia nigra. 1-(1-Naphthyl)piperazine inhibits UV-induced immunosuppression. 1-(1-Naphthyl)piperazine induces S-phase cell cycle delay, apoptosis and increases ROS levels, leading to inhibit MNT-1 cell proliferation. 1-(1-Naphthyl)piperazine can be used for melanoma research .
Cat. No.: HY-W508552
CAS No.: 139256-06-7
Target:
Research Areas:
7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one is a dual agonist of PPARα and PPARγ, with an EC50 of 23.10 μM for human PPARα and an EC50 of 22.29 μM for human PPARγ. 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one regulates the expression of lipid metabolism-related genes via PPARα, and modulates the expression of genes associated with glucose homeostasis and adipogenesis via PPARγ. 7-Hydroxy-3-(3-methoxyphenyl)-4H-chromen-4-one can be used in the research of type 2 diabetes and metabolic syndrome .
Cat. No.: HY-W599279
CAS No.: 2761170-84-5
Research Areas:
ABS-752 is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 shows no cytotoxicity in primary human hepatocytes. ABS-752 can be used in the research of hepatocellular carcinoma .
Cat. No.: HY-W778990
CAS No.: 478510-94-0
Cat. No.: HY-W998347
CAS No.: 2922884-90-8
Research Areas:
ABS-752 hydrochloride is an orally active prodrug targeting CRBN-modulating molecular glue with selectivity in protein degradation. ABS-752 hydrochloride preferentially degrades GSPT1 and induces cytotoxicity through this degradation, while it also degrades NEK7, SALL4 and CK1α, with weaker degradation potency against CK1α. As a prodrug, ABS-752 hydrochloride requires metabolic activation to ABT-002 to form the active complex; VAP-1 mediates its conversion to an aldehyde intermediate. ABS-752 hydrochloride induces cell death, reduces cell viability, and exhibits antitumor activity, leading to regression and inhibition of tumor growth. ABS-752 hydrochloride shows no cytotoxicity in primary human hepatocytes. ABS-752 hydrochloride can be used in the research of hepatocellular carcinoma .
Cat. No.: HY-121837
CAS No.: 2088234-50-6
Target:
Research Areas:
β2AR-IN-15 is a selective β2-adrenergic receptor (β2AR) antagonist with a Kd of 1.7 μM. β2AR-IN-15 binds to an intracellular β2AR region overlapping the G-protein binding site, enhancing orthosteric inverse agonist binding while negatively modulating binding of orthosteric agonists with EC50 values of 1.9 and 0.48 μM. β2AR-IN-15 shows inhibitory effect on cAMP production and β-arrestin recruitment to activated β2AR. β2AR-IN-15 can be used for the research of cardiovascular and pulmonary diseases .
Synonyms: Hetrombopag (tautomerism); SHR-8735 (tautomerism)
Research Areas:
Rafutrombopag (tautomerism) (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR‐expressing cells, including 32D‐ MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
Cat. No.: HY-13757AS2
CAS No.: 3047060-10-3
Synonyms: ICI 47699-d2; (Z)-Tamoxifen-d2; trans-Tamoxifen-d2
Target:
Research Areas:
GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
Cat. No.: HY-145589
CAS No.: 2600513-51-5
Synonyms: Hetrombopag; SHR-8735
Research Areas:
Rafutrombopag (Hetrombopag) is an orally active nonpeptide thrombopoietin receptor (TPOR/MPL) agonist. Rafutrombopag can chelate iron and alleviate iron overload while promoting haematopoiesis. Rafutrombopag specifically stimulates proliferation and differentiation of human TPOR-expressing cells, including 32D-MPL and human hematopoietic stem cells through stimulation of STAT, PI3K and ERK signalling pathways. Rafutrombopag effectively up-regulates G1-phase-related proteins, including p-RB, Cyclin D1 and CDK4/6, normalizes progression of the cell cycle, and prevents apoptosis by modulating BCL-XL/BAK expression in 32D-MPL cells. Rafutrombopag protects cardiomyocyte survival from oxidative stress damage as an enhancer of stem cells. Rafutrombopag can be used for the study of immune thrombocytopenia and oxidative stress-related cardiovascular disease .
Cat. No.: HY-14744B
CAS No.: 865430-76-8
Synonyms: (S)-Amlodipine hydrochloride; Levoamlodipine hydrochloride
Target:
Research Areas:
Levamlodipine ((S)-Amlodipine; Levoamlodipin) hydrochloride is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine hydrochloride significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine hydrochloride not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine hydrochloride exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine hydrochloride may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine hydrochloride can be used in research related to hypertension and atherosclerosis .
Cat. No.: HY-14977
CAS No.: 840523-39-9
Target:
Research Areas:
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
Cat. No.: HY-163944
CAS No.: 3081311-94-3
Research Areas:
LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer .
Cat. No.: HY-169262
CAS No.: 1001957-60-3
Target:
Research Areas:
PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
Cat. No.: HY-175238
CAS No.: 1309288-83-2
Target:
Research Areas:
KI-DX-014 is a DDX21 inhibitor with high RNA-binding inhibitory activity (IC50 of 3.31 μM). KI-DX-014 targets DDX21’s intrinsically disordered C-terminal domain, inhibits DDX21-structured RNA interaction, modulates DDX21’s RNA-dependent ATPase activity, and disrupts DDX21 biomolecular condensate formation. KI-DX-014 attenuates in vitro P-TEFb release from the 7SK snRNP complex, suppresses P-TEFb-dependent RNA polymerase II CTD phosphorylation, and induces developmental defects in zebrafish embryos. KI-DX-014 acts as a chemical probe for dissecting DDX21 functions in normal physiology and disease states. KI-DX-014 can be used for cancers and neurodegenerative disorders research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
