Dimethyl Sulfoxide
Apexbio Technology LLC PLX-4720 918505-84-7 10mM (in 1mL DMSO)
PLX-4720 (CAS 918505-84-7) is a selective inhibitor of the oncogenic kinase B-RafV600E a frequently observed activating mutation in cancer Structurally derived from a 7-azaindole scaffold PLX-4720 inhibits B-RafV600E with an IC50 of 13 nM exhibiting marked selectivity in comparison to wild-type B-Raf (IC50 160 nM) and other kinases such as FRK CSK SRC FAK FGFR and Aurora A (IC50 1000 nM) PLX-4720 decreases ERK phosphorylation in B-RafV600E-containing cells induces growth arrest and apoptosis in B-RafV600E melanoma lines and delays tumor progression in xenograft models harboring this mutation It represents a valuable tool in cancer research targeting B-Raf signaling pathways
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 LCL161 1005342-46-0 10mM (in 1mL DMSO)
LCL161 (CAS 1005342-46-0) is a small-molecule antagonist targeting inhibitor of apoptosis (IAP) proteins specifically designed as a mimetic of the endogenous second mitochondria-derived activator of caspase (SMAC) LCL161 binds to and inhibits XIAP and cIAP1/2 proteins frequently overexpressed in malignant cells It demonstrates antiproliferative activity in vitro against selected hepatocellular carcinoma cell lines (Hep3B PLC5) and hematologic cancer models (ALL) with IC50 values in the micromolar range In in vivo tumor xenograft studies oral administration of LCL161 has led to significant growth delays across various malignancies including osteosarcoma and glioblastoma Its combination with AAVP-delivered TNF- results in synergistic antitumor effects indicating its utility in oncology research
Apexbio Technology LLC Ondansetron hydrochloride dihydrate 103639-04-9 10mM (in 1mL DMSO)
Ondansetron hydrochloride dihydrate (CAS 103639-04-9) is a small molecule antagonist targeting the serotonin (5-HT3) receptor a ligand-gated ion channel prominent in the central and peripheral nervous systems Through blockade of 5-HT3 receptor signaling ondansetron inhibits serotonin-induced emetic responses Due to this mechanism it is widely utilized in biomedical research investigating serotonin-related signaling pathways and nausea mechanisms particularly in contexts involving chemotherapy-induced emesis
Apexbio Technology LLC UNC1999(Synonyms: UNC-1999, UNC 1999, EZH2 inhibitor UNC1999, EZH2-IN-UNC1999, EZH2-IN3), 10mM (in 1mL DMSO), CAS: 1431612-23-5.
UNC1999 (CAS 1431612-23-5) is a small molecule inhibitor targeting EZH2 and EZH1 enzymes responsible for methylating lysine 27 on histone H3 (H3K27me3) a modification associated with transcriptional suppression It inhibits EZH2 and EZH1 with IC50 values of 2 nM and 45 nM respectively binding at the enzyme s SAM cofactor binding site but not competing with histone substrate UNC1999 reduces cellular H3K27me3 levels (IC50 124 nM) and inhibits proliferation of DLBCL cells harboring EZH2 Y641N mutation (EC50 633 nM) It exhibits oral bioavailability in mouse studies supporting its utility as a research probe for investigating EZH-mediated epigenetic regulation
Apexbio Technology LLC PF-04217903(Synonyms: PF04217903, PF 04217903, PF-4217903, PF4217903, MET inhibitor PF-04217903), 10mM (in 1mL DMSO), CAS: 956905-27-4.
PF-04217903 (CAS 956905-27-4) is a selective ATP-competitive inhibitor targeting the receptor tyrosine kinase c-Met with a reported Ki value of 4 8 nM Aberrant activation or amplification of c-Met signaling contributes significantly to tumor cell proliferation angiogenesis and metastasis PF-04217903 exhibits high selectivity for c-Met over numerous other kinases and inhibits various c-Met mutants including R988C V1092I H1094R and T1010I In cellular studies using lines such as GTL-16 and H1993 PF-04217903 inhibits proliferation and induces apoptosis In vivo it effectively reduces c-Met phosphorylation and tumor growth suggesting potential as a research tool for investigating c-Met-related oncogenic pathways
Apexbio Technology LLC Mesoridazine(Synonyms: Serentil, Mesoridazine besylate, TPS-23), 10mM (in 1mL DMSO), CAS: 5588-33-0.
Mesoridazine (CAS 5588-33-0) is a dopaminergic antagonist primarily targeting dopamine D2 receptors (K d 19 nM) As an active metabolite of the atypical antipsychotic thioridazine mesoridazine demonstrates marked inhibitory effects on both pre- and postsynaptic dopamine receptors impacting dopamine and acetylcholine neurotransmission Furthermore mesoridazine engages histamine H1 (K d 1 8 nM) muscarinic acetylcholine (K d 69 nM) 1-adrenergic (K d 2 nM) and 2-adrenergic (K d 1600 nM) receptors Its receptor profile makes mesoridazine valuable for neuroscience research into antipsychotic mechanisms and neurotransmitter regulation
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 Etonogestrel(Synonyms: 3-Ketodesogestrel, Implanon, Nexplanon, ORG-3236, 11-Methylenelevonorgestrel), 10mM (in 1mL DMSO), CAS: 54048-10-1.
Etonogestrel (CAS 54048-10-1) is a synthetic steroidal molecule derived as the biologically active metabolite of the progestin desogestrel Structurally it belongs to the 19-nortestosterone class and acts primarily through potent binding and agonist activity at progesterone receptors Through this receptor binding it modulates various physiological processes including ovulation suppression cervical mucus viscosity enhancement and endometrial alteration Etonogestrel serves as a widely researched hormonal contraceptive with applications in reproductive biology studies endocrinological research and pharmaceutical development
Apexbio Technology LLC Peramivir(Synonyms: Rapivab, BCX-1812, RWJ-270201, Peramiflu), 10mM (in 1mL DMSO), CAS: 330600-85-6.
Peramivir (CAS 330600-85-6) is a neuraminidase inhibitor under investigation for antiviral activity against influenza virus Structurally peramivir functions as a transition-state analogue inhibitor selectively targeting viral neuraminidase to obstruct enzymatic cleavage required for virion release from infected host cells By this action peramivir effectively impedes viral propagation It has undergone clinical evaluation in research contexts notably receiving emergency use authorization for hospitalized patients during the 2009 H1N1 influenza pandemic
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 SGI-1776 free base 1025065-69-3 10mM (in 1mL DMSO)
SGI-1776 free base (CAS 1025065-69-3) is an ATP-competitive inhibitor targeting Pim kinases a serine/threonine protein kinase family implicated in regulating cellular survival pathways It selectively inhibits all three isoforms Pim-1 Pim-2 and Pim-3 leading to decreased phosphorylation of downstream substrates involved in cell cycle regulation and apoptosis such as p21Cip1/WAF1 and Bad Cellular studies indicate that SGI-1776 induces G1 cell cycle arrest promotes apoptosis and overcomes chemoresistance mediated by multidrug resistance protein 1 (MDR1) in taxane-resistant prostate cancer cells
Apexbio Technology LLC SGC-CBP30 1613695-14-9 10mM (in 1mL DMSO)
SGC-CBP30 (CAS 1613695-14-9) is a selective small-molecule inhibitor targeting the bromodomains of CREB-binding protein (CREBBP) and E1A-binding protein p300 (EP300) exhibiting IC50 values of 21 nM and 38 nM respectively Both EP300 and CREBBP function as transcriptional coactivators involved in diverse regulatory processes including cell proliferation differentiation and transcription factor activation Through its inhibitory action SGC-CBP30 is utilized widely in biomedical research to investigate the molecular roles of CREBBP/EP300 as well as in studies examining related signaling pathways in tumor biology and cellular regulation
Apexbio Technology LLC Thioridazine HCl 130-61-0 10mM (in 1mL DMSO)
Thioridazine HCl is a pharmacological inhibitor targeting dopamine receptor subtypes D2 and D4 as well as a calcium channel blocker It modulates dopaminergic neurotransmission by interfering with receptor-mediated signaling and reduces intracellular calcium influx via calcium channel inhibition (IC50 approximately 1 0 M) Thioridazine is frequently utilized in research contexts involving dopaminergic signaling pathways calcium-related cellular processes and investigations of pharmacological sensitivity shifts following prolonged receptor modulation Specifically it is employed experimentally to examine receptor-mediated cardiovascular responses such as hypotension and to assess alterations in dopamine receptor responsiveness induced by chronic exposure regimens