Dimethyl Sulfoxide
Apexbio Technology LLC MK-5172 1350514-68-9 10mM (in 1mL DMSO)
MK-5172 is a selective inhibitor targeting the hepatitis C virus (HCV) NS3/4A protease an enzyme essential for viral replication The HCV virus genome encodes this protease which cleaves polyprotein precursors enabling functional viral proteins formation during replication MK-5172 inhibits protease activity across multiple HCV genotypes demonstrating IC50 values in enzymatic assays at low nanomolar concentrations In cell-based replicon systems MK-5172 exhibits IC50 values of 2 nM (genotype 1a) 0 5 nM (genotype 1b) 8 nM (genotype 2a) and 13 nM (genotype 3) MK-5172 is utilized in antiviral studies examining various genotype infections viral resistant variants and the dynamics of viral load reductions in experimental chronic infections
Apexbio Technology LLC LDN193189 Hydrochloride 1062368-62-0 10mM (in 1mL DMSO)
LDN193189 Hydrochloride is a selective pharmacological inhibitor targeting BMP type I receptor kinases specifically activin receptor-like kinase 2 (ALK2) and ALK3 The compound acts by blocking receptor-mediated activation of Smad-dependent signaling pathways (Smad1/5/8 phosphorylation) as well as mitigating associated non-Smad signaling including phosphorylation of Akt and p38 Commonly utilized in biomedical research involving cellular differentiation epithelial barrier integrity and heterotopic ossification LDN193189 has shown the capacity to modulate BMP-induced phenotypic changes in various cell lines such as C2C12 myoblasts and bronchial epithelial cells and to influence related in vivo processes
Apexbio Technology LLC LY2874455(Synonyms: LY-2874455, LY 2874455, FGFR inhibitor LY2874455, Fibroblast growth factor receptor inhibitor LY2874455), 10mM (in 1mL DMSO), CAS: 1254473-64-7.
LY2874455 (CAS 1254473-64-7) is a small molecule inhibitor targeting fibroblast growth factor receptors (FGFRs) proteins functioning through ligand-induced receptor dimerization and tyrosine kinase activation By blocking FGFR phosphorylation and downstream signaling pathways LY2874455 inhibits proliferation and migration in FGFR-dependent cancer cell models LY2874455 shows inhibition of FGFR phosphorylation in FGFR1- FGFR2- and FGFR3-expressing cancer cell lines and xenografts demonstrating antitumor efficacy across various FGFR-driven tumor types It serves as a valuable tool molecule in oncology research investigating FGFR-mediated cancers
Apexbio Technology LLC Sitaxentan sodium(Synonyms: TBC11251, Sitaxsentan sodium, Thelin, Sitaxentan sodium hydrate, Sitaxentan sodium salt), 10mM (in 1mL DMSO), CAS: 210421-74-2.
Sitaxentan sodium (CAS 210421-74-2) is a small molecule compound functioning as an orally bioavailable and highly selective antagonist for endothelin receptor subtype A (ETA) By specifically inhibiting ETA receptor signaling sitaxentan sodium interferes with endothelin-1 mediated vasoconstriction and cellular proliferation pathways In biomedical research contexts it serves as a valuable tool for investigating endothelin-related physiological and pathological processes with particular relevance to studies on vascular disorders and pulmonary arterial hypertension
Apexbio Technology LLC Bikinin(Synonyms: Bikinin, GSK3 Inhibitor VII, Glycogen Synthase Kinase-3 Inhibitor VII, GSK-3 Inhibitor VII), 10mM (in 1mL DMSO), CAS: 188011-69-0.
Bikinin (CAS 188011-69-0) is a small molecule inhibitor targeting glycogen synthase kinase 3 (GSK3)-like kinases particularly BIN2 thereby activating brassinosteroid (BR) signaling pathways downstream of the BRI1 receptor BR signaling regulates plant developmental processes including stem elongation vascular cell differentiation leaf expansion and stress responses Treatment with Bikinin can phenotypically rescue BR-insensitive mutants in Arabidopsis by restoring BR-dependent gene expression Additionally Bikinin usage promotes xylem cell differentiation in Nicotiana benthamiana leaf disk culture suggesting utility across different biological models
Apexbio Technology LLC Idarubicin HCl 57852-57-0 10mM (in 1mL DMSO)
Idarubicin hydrochloride an anthracycline derivative structurally related to daunorubicin acts primarily by inhibiting DNA topoisomerase II It exerts cytotoxic effects through stabilization of DNA-topoisomerase II intercalation complexes inducing DNA strand breaks and apoptosis Idarubicin can be enzymatically activated intracellularly via NADPH-cytochrome C reductase enhancing DNA damage Experimentally it is commonly utilized in leukemia research particularly acute myeloid leukemia (AML) assessing cellular response to DNA damage apoptosis induction and mechanisms underlying drug resistance Idarubicin exhibits IC50 values typically ranging from low nanomolar to micromolar concentrations depending on cell line and assay conditions
Apexbio Technology LLC Aprepitant 170729-80-3 10mM (in 1mL DMSO)
Aprepitant (MK-0869) is a highly selective antagonist of the neurokinin-1 (NK-1) receptor functioning by competitively inhibiting substance P (SP) an undecapeptide belonging to the tachykinin family from activating NK-1 receptors Its binding affinity for human NK-1 receptors is indicated by a dissociation constant (Kd) of approximately 86 pM In cellular models overexpressing NK-1 receptors including glioma (GAMG) neuroblastoma (SKN-BE2 IC50 19 6 M IMR-32 IC50 27 7 M KELLY IC50 30 4 M) retinoblastoma (Y-79 IC50 23 M WERI-Rb-1 IC50 31 2 M) pancreatic cancer (PA-TU-8902 IC50 27 4 M CAPAN-1 IC50 22 7 M) and colon cancer (SW-403 IC50 30 5 M) aprepitant application has been reported to inhibit tumor cell proliferation in vitro
Apexbio Technology LLC AM095 1345614-59-6 10mM (in 1mL DMSO)
AM095 (CAS 1345614-59-6) is an orally bioavailable antagonist targeting the lysophosphatidic acid receptor 1 (LPA1) It selectively inhibits recombinant human and mouse LPA1 receptors with IC50 values of 0 98 M and 0 73 M respectively In cell-based assays AM095 suppresses LPA1-mediated chemotaxis in mouse LPA1/CHO and human melanoma A2058 cells (IC50 values 0 78 M and 0 23 M respectively) In vivo studies demonstrate its ability to prevent LPA-triggered histamine release reduce collagen and protein accumulation and limit inflammatory cell infiltration in mouse pulmonary models AM095 serves as a valuable tool for investigating LPA1-associated pathologies
Apexbio Technology LLC EMD638683 1181770-72-8 10mM (in 1mL DMSO)
EMD638683 (CAS 1181770-72-8) is a selective inhibitor of serum- and glucocorticoid-inducible kinases (SGKs) including isoforms SGK1 SGK2 and SGK3 SGK1 regulates key cellular processes such as ion transport survival proliferation and responses to steroid hormones EMD638683 shows inhibitory activity against SGK1 SGK2 and SGK3 (IC50 3 M) significantly reducing SGK-dependent phosphorylation of NDRG1 in vitro It demonstrates limited off-target interactions inhibiting only MSK1 and PRK2 at 1 M while sparing numerous other kinases In cell models EMD638683 influences mitochondrial polarization and caspase activity exhibiting antitumor effects in colorectal tumor cells and antihypertensive activity in vivo
Apexbio Technology LLC CAL-101 (Idelalisib, GS-1101) 870281-82-6 10mM (in 1mL DMSO)
CAL-101 (Idelalisib GS-1101 CAS 870281-82-6) is a selective inhibitor targeting the p110 isoform of phosphatidylinositol 3-kinase (PI3K) an enzyme involved in signaling pathways critical for proliferation and survival of malignant B cells By inhibiting PI3K p110 CAL-101 reduces PI3K-mediated phosphorylation of Akt and other downstream factors leading to enhanced PARP cleavage and caspase activation ultimately inducing apoptosis in malignant B cells CAL-101 has been demonstrated to counteract survival signals initiated by molecules such as CD40 ligand (CD40L) TNF- and fibronectin This agent is valuable in investigating B-cell malignancies
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 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