Dimethyl Sulfoxide
Apexbio Technology LLC GW788388 452342-67-5 10mM (in 1mL DMSO)
GW788388 (CAS 452342-67-5) is a selective inhibitor targeting activin receptor-like kinase 5 (ALK5) the type I receptor for transforming growth factor-beta (TGF- ) It inhibits the kinase activity of ALK5 suppressing TGF- -mediated signaling cascades GW788388 demonstrates potent inhibition of ALK5 autophosphorylation with an IC50 of 18 nM leading to decreased Smad2 phosphorylation It also inhibits TGF- -induced epithelial-mesenchymal transition (EMT) cellular proliferation fibrosis and angiogenesis in various cell models such as NMuMG MDA-MB-231 RCC and U2OS In animal studies GW788388 ameliorates renal fibrosis in diabetic db/db mouse models highlighting its utility in investigating TGF- -driven pathophysiological processes
Medchemexpress LLC Dimethyl sulfoxide | 67-68-5 | MFCD00002089 | 100.0% | 78.13 g/mol | C2H6OS | 10mL
Dimethyl sulfoxide (DMSO) (GMP Like) is the GMP Like class Dimethyl sulfoxide (HY-Y0320C) Dimethyl sulfoxide is an aprotic solvent that can dissolve water-insoluble therapeutic and toxic agents Dimethyl sulfoxide has a strong affinity for water and has the ability to rapidly penetrate or enhance the penetration of other substances through biological membranes Dimethyl sulfoxide also has potential free radical scavenging and anticholinesterase effects and may affect coagulation activity Dimethyl sulfoxide also induces histamine release from mast cells but is thought to have low systemic toxicity[1]
Apexbio Technology LLC Aurora A Inhibitor I 1158838-45-9 10mM (in 1mL DMSO)
Aurora A Inhibitor I (CAS 1158838-45-9) is a selective and potent small-molecule inhibitor of Aurora A kinase exhibiting an IC50 of 3 4 nM Aurora kinases are serine/threonine kinases crucially involved in mitotic progression with Aurora A specifically implicated in centrosome maturation and spindle assembly Aurora A Inhibitor I exerts high specificity significantly favoring Aurora A over Aurora B or cyclin-dependent kinases (CDKs) in vitro Subtle amino acid changes within kinase active sites significantly impact inhibitor potency highlighting residue-dependent selectivity This compound represents a valuable research tool for investigating Aurora A-related signaling pathways and their roles in cell division and oncogenesis
Apexbio Technology LLC Telaprevir (VX-950) 402957-28-2 10mM (in 1mL DMSO)
Telaprevir (VX-950) is an inhibitor that targets the hepatitis C virus (HCV) NS3-4A protease an essential enzyme for HCV replication Structurally derived from the viral NS5A/5B substrate Telaprevir binds to the NS3-4A protease in a covalent reversible manner through a slow-binding and dissociation mechanism thereby interrupting viral polyprotein processing Experimental studies have demonstrated that Telaprevir inhibits genotype 1 (H strain) NS3 protease with a reported inhibition constant (Ki) of approximately 7 nM In HCV replicon cell assays Telaprevir exhibits antiviral activity effectively suppresses viral replication and delays the development of viral resistance showing synergy when combined with interferon-alpha (IFN- ) Telaprevir serves as a research tool for studying antiviral mechanisms and therapeutic combinations in preclinical HCV models
Apexbio Technology LLC Bedaquiline 843663-66-1 10mM (in 1mL DMSO)
Bedaquiline a diarylquinoline antibiotic targets Mycobacterium tuberculosis via dual inhibition of subunits c and within the bacterial F1FO-ATP synthase complex disrupting ATP production It is applied primarily in research addressing multi-drug resistant (MDR) tuberculosis Recent studies have expanded its use into oncology where bedaquiline inhibits mitochondrial respiratory function and reduces glycolytic activity in cancer stem-cell-like populations In vitro experiments employing breast cancer MCF7 cells revealed bedaquiline increased ROS levels and reduced mitochondrial membrane potential Reported IC50 values for growth inhibition range approximately 1-10 M depending on cell lines and experimental conditions
Medchemexpress LLC Dimethyl sulfoxide (GMP like) | 67-68-5 | MFCD00002089 | 100.0% | 78.13 g/mol | C2H6OS | 100mL
Dimethyl sulfoxide (DMSO) (GMP Like) is the GMP Like class Dimethyl sulfoxide (HY-Y0320C) Dimethyl sulfoxide is an aprotic solvent that can dissolve water-insoluble therapeutic and toxic agents Dimethyl sulfoxide has a strong affinity for water and has the ability to rapidly penetrate or enhance the penetration of other substances through biological membranes Dimethyl sulfoxide also has potential free radical scavenging and anticholinesterase effects and may affect coagulation activity Dimethyl sulfoxide also induces histamine release from mast cells but is thought to have low systemic toxicity[1]
Medchemexpress LLC Ly2090314 1Ml Dmso Reconstitut | HY-16294-1ML DMSO RECONST
Ly2090314 1Ml Dmso Reconstitut
Apexbio Technology LLC SU11274 658084-23-2 10mM (in 1mL DMSO)
SU11274 (CAS 658084-23-2) is a selective inhibitor targeting Met kinase exhibiting an IC50 of approximately 10 nM The compound specifically suppresses the autophosphorylation of Met at residues Tyr1234/1235 disrupting receptor activity with minimal effects on other receptor tyrosine kinases such as EGFR and PDGFR or serine/threonine kinases including CDK2 In NIH3T3 cells expressing drug-sensitive or resistant MET mutants and in H1993 human lung cancer cells treatment with SU11274 induces a dose-dependent inhibition of Met phosphorylation and impairs receptor ubiquitination leading to receptor accumulation SU11274 serves as a useful tool for investigating Met signaling pathways in oncology research
Apexbio Technology LLC PF-543 1415562-82-1 10mM (in 1mL DMSO)
PF-543 (CAS 1415562-82-1) is a cell-permeable inhibitor targeting sphingosine kinase 1 (SphK1) an enzyme that phosphorylates sphingosine to sphingosine-1-phosphate (S1P) It displays potent inhibitory activity against SphK1 with an IC50 of 3 6 nM through sphingosine-competitive (non-ATP competitive) binding Treatment of SphK1-overexpressing head and neck cancer (1483) cells led to a ten-fold decrease in S1P levels confirming effective target engagement PF-543 is widely utilized as a research tool in studies investigating SphK1-mediated signaling pathways in cancer biology and immune cell trafficking
Apexbio Technology LLC LY364947 396129-53-6 10mM (in 1mL DMSO)
LY364947 (CAS 396129-53-6) is a selective inhibitor targeting the kinase domain of transforming growth factor- (TGF- ) type I receptor TGF- signaling regulates crucial biological processes such as cell proliferation differentiation and tissue homeostasis In vitro studies demonstrated that LY364947 inhibits the receptor kinase activity with an IC50 of 51 nM effectively suppressing TGF- -dependent luciferase activity in mink lung epithelial cells (p3TP Lux assay) and growth of NIH 3T3 fibroblasts In vivo LY364947 showed protective effects against NMDA-induced retinal degeneration in rats attenuating retinal ganglion cell loss and capillary degradation Thus LY364947 serves as a valuable pharmacological tool in TGF- -related research and associated pathological conditions
Apexbio Technology LLC AT9283 896466-04-9 10mM (in 1mL DMSO)
AT9283 (CAS 896466-04-9) is a synthetic small-molecule inhibitor developed through fragment-based drug design It inhibits Aurora kinases A and B key components of the serine/threonine kinase family involved in regulating cell division processes as well as targets including Janus kinases (JAKs) BCR-ABL kinase (including the T315I mutant) and Flt-3 With a potent IC50 around 3 nM against Aurora kinases AT9283 exhibits antiproliferative and pro-apoptotic activity in leukemia myeloproliferative diseases solid tumors and B-cell lymphoma models It is utilized primarily in cancer biology research to investigate its therapeutic potential targeting aberrant kinase activity