Dimethyl Sulfoxide
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
Apexbio Technology LLC Nutlin-3a chiral 675576-98-4 10mM (in 1mL DMSO)
Nutlin-3a chiral (CAS 675576-98-4) is a small-molecule antagonist targeting mouse double minute 2 (MDM2) which functions as a negative regulator of the tumor suppressor TP53 By binding directly to the TP53-interacting pocket of MDM2 Nutlin-3a blocks the degradation of TP53 stabilizing the protein and activating TP53-dependent pathways Studies in solid tumors and lymphomas indicate that Nutlin-3a induces cell cycle arrest growth inhibition and apoptosis Research has demonstrated antitumor activity in vitro and in vivo highlighting its utility in studying TP53-related cell signaling pathways and its potential in cancer research applications
Gold Biotechnology Inc DMSO, ACS Grade 10 mL
Dimethylsulfoxide (DMSO) is a very polar organic compound that is useful in organic chemistry for solubilizing organic and inorganic compounds. DMSO is also used as a cryoprotectant for cell media, preventing the formation of ice crystals, which would otherwise damage cells. DMSO can be used in PCR reactions to inhibit the self-complementation of DNA or PCR primers and increase amplification, especially for DNA sequences, which have GC rich sequences.
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 TWS119 601514-19-6 10mM (in 1mL DMSO)
TWS119 (CAS 601514-19-6) is a selective inhibitor of glycogen synthase kinase-3 (GSK-3 ) exhibiting an IC50 of approximately 30 nM Originally identified from a library of pyrrolopyrimidine-based compounds TWS119 binds GSK-3 with a Kd value around 126 nM By inhibiting GSK-3 activity TWS119 modulates downstream transcriptional events promoting neuronal differentiation in murine embryonic carcinoma (P19) and mouse embryonic stem cells through mechanisms distinct from classical Wnt signaling Due to this property TWS119 serves as a useful tool for research in neural differentiation and regenerative medicine
Apexbio Technology LLC AM1241(Synonyms: AM-1241, CB2 receptor agonist AM1241, Cannabinoid receptor CB2 agonist AM1241, AM 1241), 10mM (in 1mL DMSO), CAS: 444912-48-5.
AM1241 (CAS number 444912-48-5) is a selective agonist of the cannabinoid receptor type 2 (CB2) a G protein-coupled receptor encoded by the CNR2 gene CB2 receptors modulate inflammation and neuropathic pain pathways outside the central nervous system In vitro studies suggest stereoisomer-dependent activities specifically the S-enantiomer demonstrates higher functional potency toward human and rodent CB2 receptors compared to the R-enantiomer In animal models AM1241 administration reduces neuropathic pain phenotypes including hyperalgesia and allodynia and shows potential for delaying disease progression in an ALS (amyotrophic lateral sclerosis) mouse model Currently AM1241 remains a valuable investigational tool in preclinical pain and neurodegeneration research
Apexbio Technology LLC Dacomitinib (PF299804, PF299) 1110813-31-4 10mM (in 1mL DMSO)
Dacomitinib (PF299804 CAS 1110813-31-4) is an irreversible pan-HER small-molecule inhibitor that targets the epidermal growth factor receptor (EGFR/ErbB-1) ERBB2 (HER2) and ERBB4 (HER4) It acts by covalently binding EGFR family tyrosine kinases inhibiting downstream signaling through phospho-HER family proteins AKT and ERK Dacomitinib shows activity in vitro inducing G0/G1 cell cycle arrest and apoptosis and suppresses proliferation in trastuzumab- or lapatinib-resistant HER2-amplified breast cancer cell lines In vivo studies demonstrate antitumor effects in EGFR-mutant (e g T790M) gefitinib-resistant lung cancer xenografts making it relevant for non-small cell lung cancer research
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 Flutamide 13311-84-7 10mM (in 1mL DMSO)
Flutamide is a synthetic nonsteroidal antiandrogen agent commonly employed in biomedical research and clinical oncology Its pharmacological activity is mediated through competitive antagonism at the androgen receptor (AR) whereby its active metabolite interacts specifically with AR exhibiting a receptor binding affinity at a K sub i /sub value around 55 nM By interfering with androgen signaling pathways flutamide inhibits AR-mediated transcriptional activity resulting in reduced cellular proliferation particularly in androgen-dependent tissues In research contexts this compound is frequently utilized to investigate AR-mediated cell biology androgen-dependent tumor development and as a pharmacological tool in model systems studying prostate cancer biology and therapeutic resistance mechanisms
Apexbio Technology LLC Ifosfamide 3778-73-2 10mM (in 1mL DMSO)
Ifosfamide (CAS 3778-73-2) is an oxazaphosphorine-type alkylating agent structurally analogous to cyclophosphamide As a prodrug it undergoes hepatic activation via cytochrome P450-mediated hydroxylation generating reactive metabolites that form crosslinks within the DNA double strands This alkylation induces DNA damage subsequently inhibiting cell proliferation and promoting apoptosis in rapidly dividing cells Due to these cytostatic and cytotoxic properties Ifosfamide is widely evaluated in oncology research contexts particularly for various hematological malignancies and solid tumors
Apexbio Technology LLC MK-8245 1030612-90-8 10mM (in 1mL DMSO)
MK-8245 (CAS 1030612-90-8) is a potent liver-selective small molecule inhibitor of stearoyl-CoA desaturase (SCD) SCD1 catalyzes fatty acid desaturation and represents a target for treating type II diabetes obesity dyslipidemia and other metabolic disorders MK-8245 demonstrates strong inhibitory activity against rat mouse and human SCD1 with an IC50 of approximately 1 nM and displays liver-specific tissue distribution mediated by organic anion transporting polypeptides (OATPs) Animal studies revealed MK-8245 reduces blood glucose levels and hepatic triglycerides dose-dependently supporting its application in metabolic disease research
Apexbio Technology LLC CUDC-907 1339928-25-4 10mM (in 1mL DMSO)
CUDC-907 (CAS 1339928-25-4) is a dual inhibitor targeting histone deacetylases (HDACs 1 2 3 10) and class I phosphatidylinositol 3-kinases (PI3K) It exhibits nanomolar inhibitory activity against these enzymes blocking PI3K-mediated Akt signaling and increasing acetylation of histones and non-histone substrates (e g tubulin p53) In cancer cell models CUDC-907 induces G2-M phase arrest and reduces phosphorylation of downstream proteins such as p70S6 4EBP-1 MEK STAT3 and SRC Preclinical studies demonstrate its anti-tumor activity in lymphoma and NSCLC xenografts making it relevant for oncology research
Apexbio Technology LLC EPZ015666 1616391-65-1 10mM (in 1mL DMSO)
EPZ015666 (CAS 1616391-65-1) is a potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) an enzyme implicated in several cellular pathways including tumorigenesis EPZ015666 inhibits PRMT5 with an IC50 of 22 nM and displays a Ki value of approximately 5 nM It exhibits over 20 000-fold selectivity for PRMT5 relative to other protein methyltransferases tested In mantle cell lymphoma (MCL) cell lines treatment with EPZ015666 reduced methylation levels of the PRMT5 substrate SmD3 and exerted concentration-dependent anti-proliferative effects Additionally EPZ015666 demonstrated dose-dependent tumor growth inhibition in mouse xenograft models of MCL highlighting its potential utility as a molecular tool in cancer biology research
Apexbio Technology LLC PF-477736 952021-60-2 10mM (in 1mL DMSO)
PF-477736 is an ATP-competitive small-molecule inhibitor of checkpoint kinase 1 (Chk1) It selectively inhibits Chk1 kinase activity demonstrating nanomolar inhibitory potency in kinase assays and exhibits lower affinity toward related kinases such as CDK1 and Chk2 In vitro studies utilizing human cancer cell lines show PF-477736 disrupts Chk1-dependent G2-phase cell-cycle arrest induced by DNA-damaging agents preferentially targeting tumor cells with compromised p53 function while minimizing cytotoxicity to normal cells PF-477736 is widely utilized experimentally to study DNA damage response mechanisms potential chemosensitizing effects and therapeutic implications for cancers harboring p53 mutations