Dimethyl Sulfoxide
Apexbio Technology LLC Nexturastat A 1403783-31-2 10mM (in 1mL DMSO)
Nexturastat A (CAS 1403783-31-2) is a selective small-molecule inhibitor of histone deacetylase 6 (HDAC6) It displays potent inhibitory activity against HDAC6 with an IC50 of 5 2 nM While predominantly targeting HDAC6 Nexturastat A also exhibits moderate inhibitory effects on other HDAC isoforms (HDAC1-5 and 7-11) at low micromolar concentrations In cell-based studies including mouse B16 melanoma cell lines Nexturastat A has shown antiproliferative properties and induction of apoptosis Due to its selective HDAC6 inhibition Nexturastat A is utilized in cancer research focusing on epigenetic regulation and therapeutic development
Apexbio Technology LLC Bosutinib (SKI-606)(Synonyms: SKI-606, Bosulif, SKI606, Bosutinib monohydrate), 10mM (in 1mL DMSO), CAS: 380843-75-4.
Bosutinib (SKI-606 CAS 380843-75-4) is a dual inhibitor targeting c-Src and Abl kinases with IC50 values of approximately 1 2 nM and 1 nM respectively It suppresses phosphorylation of Bcr-Abl Src and Stat5 in chronic myeloid leukemia (CML) cells thereby decreasing proliferation and inducing regression in K562 xenograft tumor models Bosutinib also reduces Src autophosphorylation and inhibits -catenin signaling by blocking its interaction with TCF4 transcription factor consequently downregulating cyclin D1 expression in colorectal cancer cells This mechanism results in decreased cell motility and enhanced -catenin binding to E-cadherin highlighting utility in cancer research
Apexbio Technology LLC BIX 02189 1094614-85-3 10mM (in 1mL DMSO)
BIX 02189 is a selective kinase inhibitor targeting MEK5 a mitogen-activated protein kinase kinase It belongs to the chemical class of dihydroindolone-based kinase inhibitors Mechanistically BIX 02189 binds and inhibits the catalytic activity of MEK5 leading subsequently to suppression of ERK5 phosphorylation without affecting closely related kinases such as MEK1 MEK2 ERK2 or JNK2 In cellular studies using cultured HeLa and HEK293 cells BIX 02189 inhibits transcriptional activity mediated by downstream substrate MEF2C as well as ERK5 phosphorylation Additionally BIX 02189 has demonstrated inhibition of lymphatic endothelial cell sprouting in three-dimensional lymphangiogenesis assays indicating its applicability in angiogenesis and signal transduction research
Apexbio Technology LLC Levosimendan 141505-33-1 10mM (in 1mL DMSO)
Levosimendan (CAS 141505-33-1) is a small molecule calcium sensitizer that exerts its pharmacological action by binding selectively and in a calcium-dependent manner to cardiac troponin C (cTnC) Through this interaction levosimendan facilitates cardiac muscle contraction without significantly increasing intracellular calcium concentrations Research indicates utility in heart failure treatment where improved myocardial contractility is therapeutically desirable Currently levosimendan is evaluated extensively in Phase 4 clinical studies to explore its efficacy and therapeutic profile
Apexbio Technology LLC Dexlansoprazole 138530-94-6 10mM (in 1mL DMSO)
Dexlansoprazole (CAS 138530-94-6) is the dextrorotatory isomer of lansoprazole classified pharmacologically as a proton pump inhibitor (PPI) It exerts its pharmacological effects by selectively inhibiting the gastric H /K -ATPase enzyme system thereby reducing gastric acid secretion Its dual delayed-release formulation facilitates prolonged acid suppression which has been investigated extensively for therapeutic utility in acid-related gastrointestinal disorders including gastroesophageal reflux disease (GERD) erosive esophagitis and associated conditions
Apexbio Technology LLC Influenza Hemagglutinin (HA) Peptide 92000-76-5 10mM (in 1mL DMSO)
Influenza hemagglutinin (HA) peptide (sequence YPYDVPDYA) is commonly utilized in biomedical studies as an epitope tag for protein detection and isolation Derived from the influenza virus hemagglutinin protein HA mediates viral entry into host cells through initial receptor binding (via HA1 subunit) and subsequent membrane fusion (via HA2 subunit) Under acidic intracellular conditions HA undergoes conformational changes enabling membrane destabilization and viral fusion Synthetic HA-derived peptides can mimic this fusogenic mechanism enhancing gene transfer efficiency in vitro through promoting cellular uptake of transfection complexes in various cultured cell lines including K562 HeLa and BNL CL 2 hepatocyte cells Typically employed within transferrin-polylysine-DNA based delivery systems these HA peptides facilitate membrane disruption increasing complex internalization reported IC50 values vary depending on specific cellular systems and experimental conditions
Apexbio Technology LLC MK-1775 955365-80-7 10mM (in 1mL DMSO)
MK-1775 (CAS 955365-80-7) is a selective inhibitor targeting Wee1 kinase a nuclear Ser/Thr kinase involved in regulating entry into mitosis Mechanistically it inhibits Wee1-mediated Tyr15 phosphorylation of cyclin-dependent kinase 1 (CDC2) thus activating CDC2 and disrupting the G2 DNA damage checkpoint MK-1775 exhibits potent inhibition of Wee1 kinase with an in vitro IC50 of 5 2 nM and demonstrates substantial selectivity over related kinases including Myt1 In cell models harboring mutant p53 (e g WiDr) co-treatment with MK-1775 sensitizes tumor cells to DNA-damaging agents such as gemcitabine carboplatin and cisplatin highlighting its utility in cancer research
Apexbio Technology LLC Bromodomain Inhibitor, (+)-JQ1 1268524-70-4 10mM (in 1mL DMSO)
( )-JQ1 is a selective small-molecule inhibitor targeting BET (bromodomain and extraterminal) protein family members particularly BRD4 It competitively binds the acetyl-lysine recognition domain of BRD4 bromodomains 1 and 2 with reported Kd values of approximately 50 nM and 90 nM respectively By selectively inhibiting BET proteins ( )-JQ1 disrupts transcriptional regulatory processes essential in cancer biology rendering it a useful research tool for examining chromatin remodeling and gene expression patterns associated with tumor pathogenesis Additionally ( )-JQ1 specifically targets the testis-specific bromodomain protein BRDT enabling investigations into male reproductive biology by reversibly impairing spermatogenesis
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 Vorapaxar 618385-01-6 10mM (in 1mL DMSO)
Vorapaxar (CAS 618385-01-6) is a selective inhibitor of protease-activated receptor 1 (PAR1) a G-protein coupled receptor activated by thrombin-mediated cleavage on platelet surfaces leading to platelet activation Derived from the natural product himbacine vorapaxar directly binds PAR1 inhibiting platelet aggregation induced by thrombin receptor-activating peptides (IC 25 nM) and thrombin itself (IC 47 nM) In phase III clinical trials in patients daily oral administration reduced the incidence of cardiovascular death or ischemic events highlighting its relevance as an antithrombotic research agent
Apexbio Technology LLC Golvatinib (E7050) 928037-13-2 10mM (in 1mL DMSO)
Golvatinib (E7050 CAS 928037-13-2) is a small-molecule inhibitor targeting the tyrosine kinases c-Met and VEGFR-2 Golvatinib inhibits phosphorylation of c-Met in MKN45 gastric cancer cells and VEGFR-2 in human umbilical vein endothelial cells (HUVECs) with IC50 values of 14 nM and 16 nM respectively Additionally it suppresses proliferation of various tumor cells including MKN45 EBC-1 Hs746T and SNU-5 and inhibits tumor growth in xenograft models via reduction of c-Met and VEGFR-2-mediated pathways Golvatinib is utilized in cancer research to explore targeted antitumor efficacy related to angiogenesis and oncogenic signaling
Apexbio Technology LLC Carfilzomib (PR-171) 868540-17-4 10mM (in 1mL DMSO)
Carfilzomib (PR-171 CAS 868540-17-4) is a derivative of the natural product epoxomicin and functions as an irreversible inhibitor of the chymotrypsin-like activity within the 20S proteasome Proteasomes play a critical role in intracellular protein degradation thus inhibition results in accumulation of polyubiquitinated proteins Through this mechanism Carfilzomib induces cell cycle arrest and apoptosis consequently suppressing tumor cell growth Research applications primarily involve exploration of its antitumor efficacy and mechanisms in oncology models