Dimethyl Sulfoxide
Apexbio Technology LLC N6022(Synonyms: N6022, GSNOR inhibitor N6022, N-6022, N 6022, GSNOR Inhibitor N-6022, CAS 1208315-24-5, GSNORi N6022), 10mM (in 1mL DMSO), CAS: 1208315-24-5.
N6022 (CAS 1208315-24-5) is a selective reversible inhibitor of S-nitrosoglutathione reductase (GSNOR) an enzyme involved in regulating the levels of S-nitrosoglutathione (GSNO) Inhibition of GSNOR leads to elevated GSNO concentrations promoting vasodilatory and anti-inflammatory effects In biochemical assays N6022 exhibits IC50 values of 8 nM (GSNO reduction assay) and 32 nM (HMGSH oxidation assay) with corresponding Ki values of 2 5 nM and 3 1 nM respectively Due to its selectivity profile and potency N6022 has entered clinical evaluation for inflammatory pulmonary conditions
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 MK 0893 870823-12-4 10mM (in 1mL DMSO)
MK 0893 is a small molecule antagonist targeting both the glucagon receptor (GCGR) and insulin-like growth factor-1 receptor (IGF-1R) It competitively and reversibly inhibits glucagon binding to GCGR subsequently reducing receptor-mediated cAMP production In cell-based assays utilizing CHO cells expressing human GCGR MK 0893 showed nanomolar-level inhibitory potency with a receptor binding IC50 around 6 6 nM and a cellular cAMP inhibition IC50 near 15 7 nM Additionally MK 0893 exhibits potent inhibitory activity on IGF-1R demonstrated in IGF-1-driven mouse xenograft tumor models Therefore MK 0893 serves as a relevant pharmacological tool in research related to type 2 diabetes and IGF-1R-mediated oncogenic signaling pathways
Apexbio Technology LLC Doxercalciferol 54573-75-0 10mM (in 1mL DMSO)
Doxercalciferol chemically known as 1 -Hydroxyvitamin D2 is a synthetic analog of vitamin D2 characterized by selective activation of the vitamin D receptor (VDR) Upon metabolic activation Doxercalciferol undergoes hepatic transformation to its biologically active form inducing gene transcription mediated via the VDR signaling pathway Central to its mechanism activated VDR regulates calcium and phosphate homeostasis influencing cellular differentiation proliferation and parathyroid hormone expression In biomedical research Doxercalciferol serves as a tool compound to investigate the molecular pathways regulated by vitamin D receptor activation particularly in renal insufficiency models bone metabolism studies and parathyroid physiology experiments
Apexbio Technology LLC PP 2 (AG 1879) 172889-27-9 10mM (in 1mL DMSO)
PP 2 (AG 1879 CAS 172889-27-9) is a selective inhibitor targeting Src family tyrosine kinases such as Lck and Fyn with reported IC50 values of approximately 4 nM and 5 nM respectively Src family kinases are composed of nine closely related tyrosine kinases including Src Yes Fyn Fgr Yrk Lyn Blk Hck and Lck PP 2 suppresses early T-cell signaling by blocking Lck- and Fyn-mediated tyrosine phosphorylation following anti-CD3 stimulation Research in glioma cell models (U251) has demonstrated PP 2-mediated inhibition of Src-dependent cellular invasion and proliferation at micromolar concentrations PP 2 exhibits moderate inhibitory activity toward EGF-R (IC50 480 nM) and minimal effect on ZAP-70 and JAK2 Thus PP 2 serves as a research tool for studying Src kinase-dependent signaling pathways implicated in cancer and immunological responses
Apexbio Technology LLC CB-5083 1542705-92-9 10mM (in 1mL DMSO)
CB-5083 (CAS 1542705-92-9) is an orally bioavailable small-molecule inhibitor targeting the AAA ATPase p97 (also termed valosin-containing protein VCP) P97 functions in diverse cellular processes related to protein homeostasis including membrane fusion intracellular trafficking and degradation pathways CB-5083 selectively inhibits the second ATPase domain of p97 (IC50 15 4 nM) promoting cytoplasmic protein degradation and triggering apoptosis in cultured cancer cell lines such as A549 and HCT116 In vivo orally administered CB-5083 demonstrates significant reduction of tumor growth in xenograft models The compound is being investigated clinically for treatment of solid tumors and multiple myeloma
Apexbio Technology LLC Linsitinib(Synonyms: OSI-906, ASP7487, IGF-1R inhibitor OSI-906, IGF-1R/IR inhibitor OSI-906, OSI906), 10mM (in 1mL DMSO), CAS: 867160-71-2.
Linsitinib (CAS 867160-71-2) also known as OSI-906 is a small-molecule inhibitor targeting both insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) kinases It exhibits potent inhibitory effects with IC50 values of 75 nM against IR and 35 nM against IGF-1R In vitro studies using the 3T3/hulGF-1R (LISN) cell line demonstrate that Linsitinib inhibits IGF-1R ligand-dependent autophosphorylation and downstream signaling via pERK1/2 pAKT and p-p70S6K It shows antiproliferative activity across multiple cancer cell lines and exhibits dose-dependent tumor growth inhibition in LISN xenograft animal models supporting its utility in oncology research
Apexbio Technology LLC CCT128930 HCl 885499-61-6 (free base) 10mM (in 1mL DMSO)
CCT128930 HCl is a potent selective ATP-competitive inhibitor targeting AKT2 kinase with an IC50 of approximately 6 nM It exhibits higher selectivity for AKT2 compared to related kinases such as PKA and p70S6K Akt protein kinase involved in diverse cellular pathways including metabolism proliferation apoptosis transcription control and cell mobility is frequently deregulated in various tumor types In cancer cell models CCT128930 HCl impairs cellular proliferation and reduces phosphorylation of specific Akt downstream substrates Preclinical studies employing PTEN-deficient glioma cells and breast cancer xenograft models show inhibition of signaling activity and tumor growth Consequently CCT128930 HCl serves as a promising research tool for studying Akt-mediated signaling mechanisms pathway regulation and potential therapeutic responses in cancer biology
Apexbio Technology LLC UNC 0642(Synonyms: UNC0642, UNC-0642, G9a/GLP inhibitor UNC0642, UNC0642 inhibitor, G9a inhibitor UNC0642), 10mM (in 1mL DMSO), CAS: 1481677-78-4.
UNC 0642 (CAS 1481677-78-4) is a selective small-molecule inhibitor targeting lysine methyltransferases G9a and GLP These enzymes catalyze dimethylation of lysine 9 on histone H3 (H3K9) impacting chromatin organization and transcriptional regulation UNC 0642 inhibits G9a enzymatic activity with potent nanomolar affinity (IC50 2 5 nM) in cellular assays It is employed in epigenetic studies investigating G9a/GLP-mediated gene silencing and holds relevance in cancer biology neuroscience and stem cell research
Apexbio Technology LLC Teriflunomide 108605-62-5 10mM (in 1mL DMSO)
Teriflunomide (CAS 108605-62-5) the active metabolite of the antirheumatic agent Leflunomide acts primarily by selectively inhibiting dihydroorotate dehydrogenase (DHODH) a mitochondrial enzyme critical for pyrimidine nucleotide synthesis By restricting pyrimidine production teriflunomide exerts antiproliferative effects on activated lymphocytes resulting in immunosuppressive and anti-inflammatory activity Due to these properties teriflunomide is extensively studied as an oral therapeutic candidate in multiple sclerosis research addressing autoimmune-mediated disorders
Apexbio Technology LLC GSK2656157 1337532-29-2 10mM (in 1mL DMSO)
GSK2656157 (CAS 1337532-29-2) is a highly selective inhibitor of protein kinase R-like endoplasmic reticulum kinase (PERK) demonstrating an IC50 of 0 9 nM In kinase selectivity assays involving 300 kinases GSK2656157 displays marked specificity for PERK In cellular studies using BxPC3 pancreatic cancer cells this compound blocks PERK signaling reducing phosphorylation of downstream targets including eIF2 ATF4 and CHOP and subsequently suppressing protein synthesis In animal models bearing human tumor xenografts including pancreatic (BxPC3 HPAC Capan2) and multiple myeloma (NCI-H929) oral administration of GSK2656157 results in dose-dependent inhibition of tumor growth with notable sensitivity in Capan2 tumors
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 (+)-MK 801(Synonyms: Dizocilpine, Dizocilpine maleate, MK-801, (+)-MK-801, (+)-Dizocilpine), 10mM (in 1mL DMSO), CAS: 70449-94-4.
( )-MK 801 (CAS 70449-94-4) is a potent selective and non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor displaying a Ki of approximately 30 5 nM This small molecule readily crosses the blood-brain barrier and interacts reversibly with specific binding sites on cortical membranes predominantly localized within the hippocampus In vitro assays utilizing rat cortical slice preparations indicate that ( )-MK 801 robustly inhibits NMDA-induced depolarization events and suppresses epileptiform activity mediated by neurotoxic agents Due to these pharmacological properties ( )-MK 801 is utilized experimentally in neuroscience research to study NMDA receptor-mediated events neurotoxicity convulsions and excitatory neurotransmission pathways