Dimethyl Sulfoxide
Apexbio Technology LLC Trichostatin A (TSA) 58880-19-6 10mM (in 1mL DMSO)
Trichostatin A (TSA CAS 58880-19-6) is a histone deacetylase (HDAC) inhibitor and antifungal antibiotic isolated from microbial sources TSA acts by reversibly inhibiting HDAC enzymes in a noncompetitive manner leading to increased acetylation of histones particularly histone H4 In mammalian cell cultures TSA treatment results in G1 and G2 phase arrest induction of differentiation and reversion of transformed cellular phenotypes In human breast cancer cell lines TSA inhibits proliferation (IC50 124 4 120 4 nM) and induces hyperacetylation of histone proteins highlighting its utility as a tool compound for investigating epigenetic regulation and oncology-related mechanisms
Apexbio Technology LLC HATU 148893-10-1 10mM (in 1mL DMSO)
HATU (1-[Bis(dimethylamino)methylene]-1H-1 2 3-triazolo[4 5-b]pyridinium 3-oxid hexafluorophosphate) is a peptide coupling reagent routinely employed for amide-bond formation in peptide synthesis and other biomolecular applications In solution HATU converts carboxylic acids into active ester intermediates (OAt esters) facilitating subsequent nucleophilic attack from amines or alcohols This reaction typically proceeds in presence of basic additives such as N N-Diisopropylethylamine (DIPEA) under anhydrous conditions in solvents like dimethylformamide (DMF) Its utility extends to synthesizing peptides and modifying biomolecules through ester or amide linkage formation widely applied in biomedical research and pharmaceutical laboratories
Apexbio Technology LLC (-)-Blebbistatin 856925-71-8 10mM (in 1mL DMSO)
(-)-Blebbistatin is a cell-permeable small molecule inhibitor targeting non-muscle myosin II (NM II) an actin-dependent motor protein involved in cell adhesion migration and differentiation It selectively binds the myosin-ADP-phosphate complex slowing phosphate release and thereby suppressing Mg-ATPase and contractile activities mediated by actomyosin interactions It exhibits inhibitory potency in various model systems (IC50 0 5 5 0 M) with minimal effects on myosin isoforms I V X and reduced activity toward smooth muscle myosin II (IC50 80 M) Its reversible modulation of NM II renders it useful in research on cytoskeletal dynamics cell mechanics and related pathophysiological conditions
Apexbio Technology LLC Org 27569 868273-06-7 10mM (in 1mL DMSO)
Org 27569 (CAS 868273-06-7) is an allosteric modulator targeting the cannabinoid CB1 receptor It enhances the binding of the agonist CP55940 to purified CB1 receptors while simultaneously inhibiting receptor functionality In electrically-stimulated mouse vas deferens assays Org 27569 reduced WIN55212-induced contractions exhibiting a pEC50 of 8 24 0 12 and a maximal response (Emax) of approximately 45 4% Binding studies suggest its interaction at a putative allosteric site on CB1 receptors reflected by parameters such as a pKB of 5 67 0 23 and a Log of 1 14 0 17 Org 27569 serves as a tool compound for studying CB1 receptor allosteric modulation
Apexbio Technology LLC Entinostat (MS-275,SNDX-275) 209783-80-2 10mM (in 1mL DMSO)
Entinostat (MS-275 SNDX-275 CAS 209783-80-2) is an orally bioavailable small molecule inhibitor targeting histone deacetylases (HDACs) a family of enzymes involved in transcriptional regulation by modifying histone acetylation Specifically entinostat exhibits inhibitory activity against class I HDAC enzymes HDAC1 HDAC3 and HDAC8 with reported IC50 values of 0 368 M 0 501 M and 63 4 M respectively In preclinical investigations entinostat demonstrates anti-proliferative effects in diverse human tumor cell lines including breast colon lung multiple myeloma ovarian pancreatic prostate cancers and leukemia Due to these properties entinostat is widely utilized in oncology research
Apexbio Technology LLC Riluzole 1744-22-5 10mM (in 1mL DMSO)
Riluzole (CAS 1744-22-5) is a small molecule modulator of glutamatergic neurotransmission exhibiting multiple mechanisms of neuroprotection Its action primarily involves inhibition of voltage-gated sodium channels modulation of high-voltage-activated calcium and potassium channels and interference with protein kinase C activity collectively mitigating neuronal excitotoxicity In cultured rat cortical neurons riluzole inhibits inward sodium currents with an IC50 of 51 M At submicromolar to micromolar concentrations riluzole enhances sodium-dependent glutamate uptake mediated by the GLAST GLT1 and EAAC1 transporters Owing to these properties riluzole is commonly utilized in neuroscience research on excitotoxicity neurodegeneration and related pathologies
Apexbio Technology LLC Methazolamide 554-57-4 10mM (in 1mL DMSO)
Methazolamide (CAS 554-57-4) is a sulfonamide-derived inhibitor of carbonic anhydrase (CA) selectively targeting isoforms CAII and CAIV with IC50 values of 8 1 nM and 80 3 nM respectively By suppressing CA activity methazolamide reduces bicarbonate ion production thus decreasing fluid secretion and intraocular pressure consequently it has clinical use in glaucoma management Recent studies indicate this compound also exhibits insulin-sensitizing properties distinct from other CA inhibitors notably reducing hepatic glucose output suggesting potential applications in diabetes research and metabolic disorders
Apexbio Technology LLC Olmesartan 144689-24-7 10mM (in 1mL DMSO)
Olmesartan (CAS 144689-24-7) is a small molecule angiotensin II receptor antagonist primarily acting by selectively blocking the binding of angiotensin II to AT1 receptors This mechanism interrupts angiotensin II-mediated vasoconstriction and aldosterone secretion resulting in antihypertensive effects In biomedical research Olmesartan serves as a valuable tool for examining hypertensive disease models elucidating angiotensin II signaling pathways and exploring therapeutic strategies targeting cardiovascular regulation
Apexbio Technology LLC PD318088 391210-00-7 10mM (in 1mL DMSO)
PD318088 (CAS 391210-00-7) is an allosteric non-ATP competitive inhibitor of MEK1/2 kinase activity Structurally related to PD184352 it interacts adjacent to the ATP-binding site of MEK1 in proximity to residues Ile216 Phe209 Arg189 and Asp190 stabilizing a ternary complex involving MEK1/2 and MgATP This binding moderately increases the dissociation constant (Kd) for the MEK dimerization state from 75 nM to 140 nM PD318088 is mainly utilized as a molecular tool in protein kinase signaling research particularly in pathways involving MEK1/2
Apexbio Technology LLC Latrepirdine 97657-92-6 10mM (in 1mL DMSO)
Latrepirdine (CAS 97657-92-6) is an orally bioavailable small molecule investigated for its neuroprotective properties in preclinical studies of neurodegenerative diseases including Alzheimer s and Huntington s diseases Although its precise mechanism remains under investigation latrepirdine has demonstrated the ability to inhibit neuronal cell death pathways in animal disease models Moreover preliminary evidence indicates potential cognitive enhancement in normal physiological conditions Latrepirdine serves as a relevant tool compound to study neuronal survival mechanisms and cognitive function regulation
Apexbio Technology LLC Valganciclovir HCl 175865-59-5 10mM (in 1mL DMSO)
Valganciclovir hydrochloride is an antiviral prodrug that undergoes rapid enzymatic conversion to the active metabolite ganciclovir after oral administration Ganciclovir inhibits viral replication by selectively targeting viral DNA polymerase thereby interfering with viral DNA synthesis and slowing cytomegalovirus (CMV) proliferation Valganciclovir is commonly utilized in laboratory studies to evaluate antiviral activity against CMV and related herpesviruses and to investigate its therapeutic potential in CMV-associated infections including retinitis and organ transplant-associated CMV infections In vitro studies report an IC50 value for valganciclovir-derived ganciclovir ranging approximately from 0 2 to 2 8 M depending on experimental cell type and viral strain
Apexbio Technology LLC CP-724714 537705-08-1 10mM (in 1mL DMSO)
CP-724714 (CAS 537705-08-1) is a small molecule inhibitor selectively targeting erbB2 (Her2) and EGFR kinases with notable potency against erbB2 kinase (IC50 10 3 nM) and considerably lower activity toward EGFR kinase (IC50 6 400 2 100 nM) In cellular assays CP-724714 induces G1 cell-cycle arrest and decreases erbB2 phosphorylation in Her2-overexpressing BT-474 breast cancer cells In animal xenograft models (BT-474 MDA-MB-453) it reduces erbB2 receptor phosphorylation and downstream signaling resulting in tumor growth inhibition and apoptosis induction CP-724714 advanced into phase I clinical trials for Her2-driven breast cancer research
Apexbio Technology LLC Bindarit 130641-38-2 10mM (in 1mL DMSO)
Bindarit (CAS 130641-38-2) also known as AF-2838 is a synthetic small-molecule inhibitor targeting the CC chemokines MCP-1 (CCL2) MCP-2 (CCL8) and MCP-3 (CCL7) By suppressing the transcription and production of MCP proteins Bindarit reduces monocyte chemoattraction and inflammation In vitro data indicate that Bindarit inhibits LPS-induced MCP-1 synthesis in monocytes with an IC50 around 172 M and selectively decreases MCP expression without impacting unrelated cytokines such as IL-6 or IL-8 Animal studies demonstrate its potential to reduce inflammatory cell infiltration vascular smooth muscle cell proliferation and neointimal hyperplasia in rodent injury models highlighting its value for inflammation and cardiovascular disease research
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
Apexbio Technology LLC Tie2 kinase inhibitor 948557-43-5 10mM (in 1mL DMSO)
Tie2 kinase inhibitor (CAS 948557-43-5) is a selective and reversible small-molecule inhibitor targeting the Tie2 receptor tyrosine kinase a critical modulator of endothelial cell survival angiogenesis and vascular integrity By inhibiting Tie2 autophosphorylation this compound disrupts subsequent signaling pathways involved in endothelial maturation and tumor-associated angiogenesis In vitro studies demonstrate potent inhibition of Tie2 kinase activity (IC50 0 25 M) with substantial selectivity over other kinases including p38 In vivo treatment reduces angiogenesis and tumor progression in murine xenograft tumor models This inhibitor is thus relevant for research examining angiogenic mechanisms and cancer progression