Dimethyl Sulfoxide
Apexbio Technology LLC Afatinib (BIBW2992) 439081-18-2 10mM (in 1mL DMSO)
Afatinib (BIBW2992 CAS 439081-18-2) is an irreversible inhibitor targeting receptor tyrosine kinases in the ErbB protein family specifically EGFR (ErbB1) and HER2 (ErbB2) By covalently binding to their kinase domains it suppresses downstream ErbB signaling showing demonstrated inhibition with IC50 values of 0 5 nM for EGFR and 14 nM for HER2 Afatinib blocks EGF-induced phosphorylation and cellular proliferation in multiple EGFR- or HER2-expressing lines including A431 NIH-3T3-HER2 NCI-N87 and BT-474 Research applications include tumor xenograft studies and transgenic lung cancer models evaluating EGFR-dependent oncogenic processes and therapeutic responses
Apexbio Technology LLC Alfacalcidol 41294-56-8 10mM (in 1mL DMSO)
Alfacalcidol is a vitamin D analog functioning as an inhibitor of bone resorption through modulation of calcium homeostasis By binding specifically to vitamin D receptors (VDR) located in calcium-regulating tissues such as intestine bone kidney and parathyroid glands Alfacalcidol contributes to mineral metabolism and bone turnover regulation Preclinical studies using ovariectomized animal models demonstrate that Alfacalcidol at pharmacological doses not inducing hypercalcemia suppresses osteoclast-mediated bone resorption while preserving calcium balance in plasma and urine Due to these properties Alfacalcidol is frequently utilized in biomedical research to investigate mechanisms involved in osteoporosis progression and potential therapeutic interventions addressing calcium and bone metabolism disorders
Apexbio Technology LLC Everolimus (RAD001) 159351-69-6 10mM (in 1mL DMSO)
Everolimus (RAD001) is an orally bioavailable small-molecule inhibitor targeting mammalian target of rapamycin (mTOR) an integral serine/threonine kinase regulating cell proliferation metabolism and survival within the PI3K/Akt pathway Everolimus binds intracellularly to the immunophilin FKBP12 the resulting complex subsequently interacts directly with mTOR inhibiting its kinase activity thereby reducing downstream phosphorylation of S6 kinase 1 (S6K1) and the eukaryotic initiation factor 4E-binding protein (4EBP) Functionally Everolimus exerts immunosuppressive properties used clinically to prevent organ transplant rejection and demonstrates antitumor activity against several malignancies including renal cell carcinoma and basal cell carcinoma Commonly utilized in cancer research Everolimus inhibits mTOR with IC50 values reported in the low nanomolar range ( 1 3 nM)
Apexbio Technology LLC Salubrinal 405060-95-9 10mM (in 1mL DMSO)
Salubrinal is a cell-permeable inhibitor of eukaryotic translation initiation factor 2 alpha (eIF2 ) dephosphorylation exhibiting an IC50 of approximately 15 M It prevents phosphatase complexes from removing phosphate groups from eIF2 thus maintaining its phosphorylated state and modulating protein synthesis during cellular stress responses Salubrinal is utilized experimentally in vitro to investigate apoptotic mechanisms related to endoplasmic reticulum (ER) stress For instance it provides cytoprotection against ER stress-induced apoptosis triggered by protein glycosylation inhibitors or ER-Golgi trafficking inhibitors In vivo murine models employ salubrinal to explore cellular processes underlying oxidative stress and nephrotoxicity induced by chemotherapeutic treatments through modulation of ER stress-associated apoptosis signaling pathways Currently no clinical trials involving salubrinal have been reported
Apexbio Technology LLC Eptifibatide 188627-80-7 10mM (in 1mL DMSO)
Eptifibatide is a cyclic heptapeptide belonging to the glycoprotein IIb/IIIa inhibitor category functioning as an antagonist of platelet adhesion by reversibly binding to the platelet glycoprotein IIb/IIIa receptor This receptor located on platelet surfaces mediates platelet aggregation through binding fibrinogen and von Willebrand factor processes essential in thrombus formation By blocking the GP IIb/IIIa receptor binding site Eptifibatide inhibits fibrinogen-dependent platelet cross-linking reducing platelet aggregation In biomedical research Eptifibatide serves as a pharmacological tool to investigate platelet function thrombosis mechanisms and related cardiovascular diseases in preclinical and clinical models
Apexbio Technology LLC U-73122 112648-68-7 10mM (in 1mL DMSO)
U-73122 (CAS 112648-68-7) is a phospholipase C (PLC) inhibitor utilized in biomedical research By selectively targeting PLC an enzyme responsible for hydrolyzing phosphatidylinositol 4 5-bisphosphate into intracellular messengers diacylglycerol and inositol-triphosphate U-73122 attenuates downstream signaling events such as protein kinase C activation and intracellular calcium release In vitro U-73122 inhibits recombinant human PLC- 2 with an IC50 of approximately 6 M while minimally affecting PLC- 1 3 and 4 isoforms In animal models U-73122 demonstrates anti-inflammatory properties reducing carrageenan-induced rat paw edema and TPA-induced mouse ear edema
Apexbio Technology LLC Vardenafil 224785-90-4 10mM (in 1mL DMSO)
Vardenafil (CAS 224785-90-4) is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) It inhibits PDE5 enzyme activity with an IC50 of approximately 0 7 nM in vitro Compared with other PDE isoforms (PDE1-4 and PDE6) vardenafil demonstrates superior selectivity toward PDE5 though moderate inhibition of PDE6 (IC50 11 nM) is observed Vardenafil enhances cGMP accumulation in human corpus cavernosum and significantly potentiates nitric oxide (SNP)- acetylcholine- and electrical field stimulation-induced relaxation in human trabecular smooth muscle Its vasodilatory effects render it suitable for research in erectile function and related vascular physiology
Apexbio Technology LLC SRT1720 HCl 1001645-58-4 10mM (in 1mL DMSO)
SRT1720 HCl is a small molecule activator of SIRT1 exerting more potent activation than resveratrol It functions through a SIRT1- and PGC-1 -dependent mechanism modulating mitochondrial oxidative metabolism and insulin sensitivity The compound has demonstrated activity in regulating cell growth and apoptosis in multiple myeloma (MM) cells without notably affecting normal cell viability Its antitumor properties relate to activation of caspase-8 caspase-9 caspase-3 and PARP enhancement of reactive oxygen species generation induction of ATM/CHK2 signaling suppression of NF- B signaling and reduction of VEGF-induced migration SRT1720 is utilized in biomedical research to investigate metabolic pathways tumor biology and potential sensitization effects to chemotherapy agents
Apexbio Technology LLC Dorsomorphin 2HCl 1219168-18-9 10mM (in 1mL DMSO)
Dorsomorphin 2HCl (CAS 1219168-18-9) is a small-molecule inhibitor targeting BMP signaling through selective blockade of BMP type I receptors ALK2 ALK3 and ALK6 It prevents phosphorylation of downstream effectors SMAD1/5/8 with an IC50 of approximately 0 47 mM Originally identified by zebrafish phenotypic screening as a disruptor of embryonic dorsoventral patterning Dorsomorphin has been employed to dissect BMP-regulated pathways in iron homeostasis significantly affecting hepcidin expression and iron metabolism in vitro and in vivo It is widely utilized in mechanistic studies of BMP function and signaling regulation
Apexbio Technology LLC AST-1306 897383-62-9 10mM (in 1mL DMSO)
AST-1306 (CAS 897383-62-9) is an inhibitor of epidermal growth factor receptor (EGFR) and HER2 receptor tyrosine kinases In biochemical assays AST-1306 inhibits EGFR and HER2 kinase activity with IC50 values of 0 5 nM and 3 nM respectively It also demonstrates inhibitory activity against EGFR mutations such as T790M/L858R reducing receptor phosphorylation and downstream signaling in both cell-free and cellular systems In various animal tumor models including ErbB2-overexpressing and SK-OV-3 xenografts AST-1306 suppresses tumor growth and signaling pathways supporting its use in EGFR- and HER2-related oncology research
Apexbio Technology LLC MLN2238(Synonyms: Ixazomib, MLN-2238, Ninlaro, MLN9708, Ixazomib citrate), 10mM (in 1mL DMSO), CAS: 1072833-77-2.
MLN2238 (CAS number 1072833-77-2) is a dipeptidyl boronic acid derivative designed as a reversible inhibitor of the 5 subunit (chymotrypsin-like activity) of the 20S proteasome with reported IC50 and Ki values of 3 4 nM and 0 93 nM respectively At higher concentrations MLN2238 also targets the proteasome s 1 (caspase-like) and 2 (trypsin-like) subunits In preclinical studies using xenograft and genetically-engineered models of hematologic malignancies MLN2238 exhibited potent antitumor activity promoting apoptosis and suppressing pathways such as NF- B MLN2238 has research applications in oncology particularly against multiple myeloma and lymphoma including in bortezomib-resistant cell lines
Apexbio Technology LLC Q-VD-OPh 1135695-98-5 10mM (in 1mL DMSO)
Q-VD-OPh is a pan-caspase inhibitor targeting caspases including 1 3 8 and 9 with IC50 values ranging from approximately 25 to 400 nM By blocking multiple caspase-mediated apoptotic pathways including caspase-9/3 caspase-8/10 and caspase-12 pathways Q-VD-OPh prevents apoptotic cell death induced by agents such as actinomycin D In research contexts this inhibitor serves as a tool to investigate apoptosis mechanisms across diverse cell types and species including human mouse and rat It is also used to enhance cell viability upon thawing from cryopreservation under standard cryoprotectant conditions
Apexbio Technology LLC MHY1485 326914-06-1 10mM (in 1mL DMSO)
MHY1485 (CAS 326914-06-1) is a potent activator of mammalian target of rapamycin (mTOR) a serine/threonine kinase critical for cellular growth metabolism and survival pathways By activating mTOR signaling MHY1485 inhibits autophagy initiation and disrupts the fusion step between autophagosomes and lysosomes resulting in accumulation of autophagic marker LC3-II and enlarged autophagic structures In cultured rat Ac2F hepatic cells MHY1485 suppresses basal and starvation-induced autophagic flux Additionally MHY1485 treatment promotes ovarian follicular development and increases explant growth in mouse ovarian culture models providing a useful tool in biomedical research of mTOR signaling and reproductive biology
Apexbio Technology LLC PD98059 167869-21-8 10mM (in 1mL DMSO)
PD98059 (CAS 167869-21-8) is a selective reversible inhibitor of MAP kinase kinase (MEK/MAPK/ERK kinase) It specifically targets MEK1 affecting both basal and partially activated forms with a reported IC50 of approximately 10 M Treatment with PD98059 inhibits ERK1/2 phosphorylation in a dose-dependent manner resulting in downregulation of cyclin E/Cdk2 and cyclin D1/Cdk4 complexes In cell-based studies such as human leukemia U937 cell models treatment leads to cell growth arrest at the G1 phase and induction of apoptosis PD98059 is widely employed in research investigating signaling pathways involving ERK activation cell cycle regulation and apoptosis
Apexbio Technology LLC PD184352 (CI-1040) 212631-79-3 10mM (in 1mL DMSO)
PD184352 (CI-1040 CAS 212631-79-3) is a benzhydroxamate derivative that selectively inhibits the MEK1/2 kinases members of the MAP kinase kinase (MAPKK) family It interacts with a hydrophobic pocket adjacent to the Mg-ATP binding region of MEK1/2 triggering conformational shifts that favor the inactive non-phosphorylated state of these enzymes Acting via an ATP- and ERK1/2-independent inhibitory mechanism PD184352 robustly suppresses purified MEK1 enzyme activity (IC50 17 nM) Preclinical research demonstrates efficacy in reducing tumor growth notably in murine xenograft models of colon carcinoma underscoring its utility as a research tool in oncology