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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
3072 Results for "
Modulators
" in MedChemExpress (MCE) Product Catalog:
Products (3072)
3072 Results for "Modulators" in MCE Product Catalog:
Cat. No.: HY-121837
CAS No.: 2088234-50-6
Target:
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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:
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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:
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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
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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
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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
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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
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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 .
Cat. No.: HY-176535
CAS No.: 2648377-08-4
Synonyms: BBC0115
Research Areas:
KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
Cat. No.: HY-180261
CAS No.: 3107761-81-6
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
Cat. No.: HY-180406
CAS No.: 1262495-12-4
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NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal .
Cat. No.: HY-18234
CAS No.: 55123-66-5
Leupeptin is a broad-spectrum protease inhibitor . By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin can be used in research on chronic inflammatory diseases and skin tumorigenesis .
Cat. No.: HY-182707
CAS No.: 2055045-42-4
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Research Areas:
JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .
Cat. No.: HY-183478
CAS No.: 39740-82-4
Target:
Ser/Thr Protease Cathepsin Autophagy SARS-CoV Atg8/LC3 NO Synthase COX p62 Arginase PTEN NF-κB PI3K Akt p38 MAPK ERK Reactive Oxygen Species (ROS)
Research Areas:
Leupeptin hydrochloride is a broad-spectrum protease inhibitor . By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hydrochloride significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hydrochloride inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hydrochloride can be used in research on chronic inflammatory diseases and skin tumorigenesis .
Research Areas:
p-Toluenesulfonamide is a small-molecule anticancer agent and plasticizer. p-Toluenesulfonamide exerts antitumor activity by inducing lysosomal membrane permeabilization, cathepsin B release and lysosome-mediated cell death. p-Toluenesulfonamide modulates cholesterol distribution in lipid rafts of tumor cell membranes and the Akt/mTOR/p70S6K pathway. p-Toluenesulfonamide shows activity against various cancers including hepatocellular carcinoma, non-small cell lung cancer and tongue squamous cell carcinoma; intrapleural injection effectively reduces malignant pleural effusion without causing pleural adhesion. p-Toluenesulfonamide is also the main degradation product of the disinfectant Chloramine-T (HY-B0959) in water. p-Toluenesulfonamide facilitates the localization of fluorescent probes to the endoplasmic reticulum. p-Toluenesulfonamide can be used in cancer-related research .
Cat. No.: HY-B0113S2
CAS No.: 1189891-71-1
Synonyms: Omeprazole sulphone (methoxy-d3)
Cat. No.: HY-B0113S3
CAS No.: 1261395-28-1
Synonyms: H 16868-13C,d3
Cat. No.: HY-B0113S5
CAS No.: 922731-02-0
Synonyms: H 16868-d6
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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
