Benzenesulfonamides
Medchemexpress LLC GSK8612 | 2361659-62-1 | 99.6% | 520.33 | 100 MG
GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1. It is intended for research use only and not for sale to patients. In vitro, GSK8612 inhibits toll-like receptor (TLR)3-induced IRF3 phosphorylation in Ramos cells and type I IFN secretion in primary human mononuclear cells. In THP1 cells, it inhibits the secretion of IFNβ in response to dsDNA and cGAMP, the natural ligand for STING.
- Highly selective and potent tank-binding kinase-1 (TBK1) inhibitor.
- pIC50 of 6.8 for recombinant TBK1.
- Inhibits TLR3-induced IRF3 phosphorylation in Ramos cells.
- Inhibits type I IFN secretion in primary human mononuclear cells.
- Inhibits secretion of IFNβ in response to dsDNA and cGAMP in THP1 cells.
Medchemexpress LLC Rac-osmi-1 | 2748153-92-4 | 96.5% | 5 MG
(Rac)-OSMI-1 is the racemic form of OSMI-1, a cell-permeable small-molecule inhibitor of O-GlcNAc transferase (OGT) used in biochemical and cell-based research to reduce protein O-GlcNAcylation.
- Cell-permeable OGT inhibitor with reported IC50 ≈ 2.7 μM.
- Suitable for cell-based assays and biochemical studies.
- Purity approximately 96.5% (manufacturer-stated).
- Molecular weight 563.64 g/mol; formula C28H25N3O6S2.
- Research-use only; not for clinical or human use.
Medchemexpress LLC Iacs-13909 | 2160546-07-4 | 99.9% | 377.27 | 100 MG
IACS-13909 is a selective, potent, and orally active allosteric SHP2 inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. It demonstrates greater selectivity for SHP2 over other phosphatases, including SHP1. It exhibits antitumor activities and can suppress MAPK pathway signaling in receptor tyrosine kinase (RTK)-dependent cancers.
- Potently suppresses proliferation of wild-type SHP2 and KYSE-520 cells.
- Suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells.
- Suppresses proliferation of both parental and NCI-H1975 CS cells in a dose-dependent manner.
- Potently suppresses tumor growth in NSG mice injected with KYSE-520 cells, achieving 100% tumor growth inhibition.
![Medchemexpress LLC 4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- | 2160546-07-4 | 100.0% | 377.27 | 5 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000364203-logo.png-250.jpg){kind=logo}
Medchemexpress LLC 4-Piperidinamine, 1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl- | 2160546-07-4 | 100.0% | 377.27 | 5 MG
IACS-13909 is a selective, potent, and orally active SHP2 allosteric inhibitor. It exhibits greater selectivity for SHP2 over other phosphatases, including SHP1. This compound demonstrates antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinase (RTK)-dependent cancers.
- Potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells.
- Suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells.
- Inhibits the proliferation of parental cells and NCI-H1975 CS cells in a dose-dependent manner.
- Achieved 100% tumor growth inhibition (TGI) in mice studies.
- Functions as a selective SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM.
Medchemexpress LLC Sildenafil | 139755-83-2 | MFCD00867528 | 99.99% | 474.58 | 100 MG
Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM. It has been shown to potentiate the phosphorylation of ERK1/ERK2, increase the percentage of cells in S phase, and enhance cell proliferation in vitro. In animal models, it significantly increases intracavernosal pressure and has been observed to decrease flap necrosis by increasing the secretion of growth factors.
- Potent phosphodiesterase type 5 (PDE5) inhibitor.
- Increases intracavernosal pressure.
- Potentiates phosphorylation of ERK1/ERK2.
- Increases cell proliferation.
- Decreases flap necrosis by increasing growth factor secretion.
Medchemexpress LLC Sildenafil citrate | 171599-83-0 | C28H38N6O11S | 1 G
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM. It is for research use only.
- Potent phosphodiesterase type 5 (PDE5) inhibitor.
- Potentiates phosphorylation of ERK1/ERK2 in vitro.
- Increases percentage of cells in S phase and enhances cell proliferation in vitro.
- Significantly increases intracavernosal pressure (ICP) in a dog model of erection in vivo.
- Reduces the number of TL+-cells in vivo.
- Decreases flap necrosis in preclinical animal models by increasing secretion of growth factors (FGF and VEGF).
Selleck Chemical LLC OSMI-1-5mg
OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with IC50 of 2.7 μM for full length human OGT (ncOGT).
Apexbio Technology LLC Bosentan Hydrate 157212-55-0 10mM (in 1mL DMSO)
Bosentan Hydrate (CAS 157212-55-0) is a sulfonamide-derived competitive antagonist of endothelin receptors exhibiting preferential affinity toward endothelin A over endothelin B receptors By interfering with endothelin-triggered signaling in endothelial and vascular smooth muscle cells it attenuates vasoconstrictive and bronchoconstrictive responses In vitro studies revealed bosentan inhibited endothelin receptor activity in P388/dx cells (IC50 15 1 1 6 M) and effectively reversed antiangiogenic effects of systemic sclerosis patient sera on dermal microvascular endothelial cells In animal models bosentan administration post-myocardial infarction significantly elevated plasma leptin levels Clinically bosentan is applied extensively in research on pulmonary arterial hypertension showing beneficial outcomes on patients exercise capacity
![Medchemexpress LLC 5-[6-methyl-5-[(1S,2R)-2-propan-2-ylcyclopropyl]pyridazin-3-yl]-1H-pyrimidine-2,4-dione | 2375815-63-5 | 99.9% | 286.33 g/mol | C15H18N4O2 | 5 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000222450.png-250.jpg)
Medchemexpress LLC 5-[6-methyl-5-[(1S,2R)-2-propan-2-ylcyclopropyl]pyridazin-3-yl]-1H-pyrimidine-2,4-dione | 2375815-63-5 | 99.9% | 286.33 g/mol | C15H18N4O2 | 5 MG
CD73-IN-3 is a small-molecule CD73 inhibitor intended for preclinical cancer research and cell-based assays. It is supplied as a high-purity solid and has been characterized in human cell assays for potency and stability.
- Potent CD73 inhibition with IC50 = 7.3 nM in Calu6 human cell assay.
- High purity (99.89%) suitable for research applications.
- Solid, white to off-white physical form for easy handling and storage.
- Stable under recommended storage: powder -20°C (3 years), 4°C (2 years); in solvent -80°C (6 months), -20°C (1 month).
- Molecular formula C15H18N4O2 and molecular weight 286.33 g/mol for formulation planning.
Apexbio Technology LLC Bosentan Hydrate 157212-55-0 200mg
Bosentan Hydrate (CAS 157212-55-0) is a sulfonamide-derived competitive antagonist of endothelin receptors exhibiting preferential affinity toward endothelin A over endothelin B receptors By interfering with endothelin-triggered signaling in endothelial and vascular smooth muscle cells it attenuates vasoconstrictive and bronchoconstrictive responses In vitro studies revealed bosentan inhibited endothelin receptor activity in P388/dx cells (IC50 15 1 1 6 M) and effectively reversed antiangiogenic effects of systemic sclerosis patient sera on dermal microvascular endothelial cells In animal models bosentan administration post-myocardial infarction significantly elevated plasma leptin levels Clinically bosentan is applied extensively in research on pulmonary arterial hypertension showing beneficial outcomes on patients exercise capacity
Apexbio Technology LLC Bosentan Hydrate 157212-55-0 100mg
Bosentan Hydrate (CAS 157212-55-0) is a sulfonamide-derived competitive antagonist of endothelin receptors exhibiting preferential affinity toward endothelin A over endothelin B receptors By interfering with endothelin-triggered signaling in endothelial and vascular smooth muscle cells it attenuates vasoconstrictive and bronchoconstrictive responses In vitro studies revealed bosentan inhibited endothelin receptor activity in P388/dx cells (IC50 15 1 1 6 M) and effectively reversed antiangiogenic effects of systemic sclerosis patient sera on dermal microvascular endothelial cells In animal models bosentan administration post-myocardial infarction significantly elevated plasma leptin levels Clinically bosentan is applied extensively in research on pulmonary arterial hypertension showing beneficial outcomes on patients exercise capacity
Apexbio Technology LLC Bosentan Hydrate 157212-55-0 50mg
Bosentan Hydrate (CAS 157212-55-0) is a sulfonamide-derived competitive antagonist of endothelin receptors exhibiting preferential affinity toward endothelin A over endothelin B receptors By interfering with endothelin-triggered signaling in endothelial and vascular smooth muscle cells it attenuates vasoconstrictive and bronchoconstrictive responses In vitro studies revealed bosentan inhibited endothelin receptor activity in P388/dx cells (IC50 15 1 1 6 M) and effectively reversed antiangiogenic effects of systemic sclerosis patient sera on dermal microvascular endothelial cells In animal models bosentan administration post-myocardial infarction significantly elevated plasma leptin levels Clinically bosentan is applied extensively in research on pulmonary arterial hypertension showing beneficial outcomes on patients exercise capacity
Medchemexpress LLC dTRIM24 | 2170695-14-2 | 99.89% | 1113.30 | 10 MG
dTRIM24 is a selective bifunctional degrader of TRIM24, designed to suppress growth in MOLM-13 cells by recruiting the VHL E3 ubiquitin ligase. This PROTAC-based degrader leads to potent and selective degradation of TRIM24, causing apoptosis and a sustained proliferative defect.
- Potent and selective degradation of TRIM24
- Suppresses growth in MOLM-13 cells
- Induces apoptosis with enhanced PARP cleavage
- Based on PROTAC technology
Apexbio Technology LLC Sulfasalazine 599-79-1 10mM (in 1mL DMSO)
Sulfasalazine (599-79-1) is a small-molecule inhibitor targeting the NF- B signaling pathway and the cystine-glutamate antiporter system (system Xc-) It is designed to suppress NF- B activation and inhibit cystine uptake thereby modulating inflammatory gene expression and intracellular glutathione synthesis Sulfasalazine exerts its biological activity primarily through inhibition of NF- B activation and blockade of system Xc- In in vitro studies sulfasalazine demonstrates growth inhibition and induction of apoptosis in several cancer cell lines including MIA PaCa-2 PANC-1 and glioblastoma cells with reported IC50 values ranging from approximately 0 2 to 0 5 mM depending on cell type and conditions Based on these pharmacological properties sulfasalazine holds research potential in inflammation NF- B signaling oxidative stress modulation and cancer studies
Medchemexpress LLC HY-117383 10mg Medchemexpress, NGI-1 CAS:790702-57-7 Purity:>98%
Medchemexpress, HY-117383 10mg NGI-1 CAS:790702-57-7 NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability. Purity:>98% Medchemexpress has over 10000 novel life-science reagents, reference compounds, APIs and natural compounds for laboratory and scientific use. Other quantity can also be offered.