Dimethyl Sulfoxide
Apexbio Technology LLC Zebularine 3690-10-6 10mM (in 1mL DMSO)
Zebularine (CAS number 3690-10-6) is a chemically stable cytidine analog containing a 2-(1H)-pyrimidinone ring structure It acts primarily through inhibition of DNA methylation by forming covalent complexes with DNA methyltransferases Zebularine treatment leads to demethylation and reactivation of hypermethylation-mediated silenced genes exemplified by the p16 gene Additionally induced myogenic differentiation has been observed upon zebularine administration in 10T1/2 cells Zebularine displays minimal cytotoxicity in certain cell models such as T24 cells and retains stability in aqueous solutions across a broad pH range (up to pH 12) These properties make zebularine relevant for studies in epigenetic regulation and cellular differentiation
Apexbio Technology LLC A-803467 944261-79-4 10mM (in 1mL DMSO)
A-803467 (CAS 944261-79-4) is a potent selective blocker of the voltage-gated sodium channel subtype NaV1 8 It inhibits human and rat recombinant NaV1 8 channels with IC50 values of approximately 79 nM and 45 nM respectively Its selectivity for NaV1 8 over other sodium channel subtypes (e g NaV1 2 NaV1 3 NaV1 5 and NaV1 7) is 300 1000 fold By specifically reducing activity in tetrodotoxin-resistant sodium currents of dorsal root ganglion neurons A-803467 suppresses induced and spontaneous action potential firing exhibiting analgesic properties in animal models of neuropathic and inflammatory pain
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
Apexbio Technology LLC BV6 1001600-56-1 10mM (in 1mL DMSO)
BV6 (CAS 1001600-56-1) is a selective inhibitor targeting the inhibitor of apoptosis protein (IAP) family The IAP family includes proteins such as XIAP c-IAP1 and c-IAP2 that regulate programmed cell death pathways BV6 induces apoptosis and sensitizes cancer cells to chemotherapeutic agents and radiation by decreasing expression levels of IAPs including XIAP and c-IAP1 In vitro treatment with BV6 exhibited an IC50 of 7 2 M in H460 non-small cell lung carcinoma cells and enhanced their response to radiation BV6 is employed in research exploring cancer cell apoptosis modulation and therapeutic resistance
Apexbio Technology LLC Roscovitine (Seliciclib,CYC202) 186692-46-6 10mM (in 1mL DMSO)
Roscovitine (Seliciclib CYC202 CAS number 186692-46-6) is a selective inhibitor of cyclin-dependent kinases (CDKs) It targets cdc2 (CDK1/cyclin B) CDK2 (CDK2/cyclin A and CDK2/cyclin E) and CDK5 (CDK5/p35) with reported IC50 values of 0 65 M 0 7 M 0 7 M and 0 16 M respectively Additionally roscovitine inhibits extracellular signal-regulated kinases Erk1 and Erk2 displaying IC50 values of 34 M and 14 M respectively In cellular studies roscovitine has been shown to delay or halt transitions during early mitosis specifically preventing cell progression from prophase to metaphase as observed in Xenopus oocyte maturation induced by progesterone Due to its distinct inhibitory profile roscovitine is commonly utilized in research examining cell cycle regulation and kinase signaling pathways relevant to oncology
Apexbio Technology LLC BAPTA-AM 126150-97-8 10mM (in 1mL DMSO)
BAPTA-AM (CAS 126150-97-8) is a selective membrane-permeable calcium (Ca ) chelator widely utilized in biomedical research After entering cells intracellular esterases cleave BAPTA-AM releasing the active BAPTA which binds free Ca to modulate calcium-dependent cellular processes In human leukemia HL-60 and U937 cells BAPTA-AM induces apoptosis characterized by DNA fragmentation and reduced c-jun expression Additionally it inhibits voltage-gated and Ca -activated potassium currents in bovine chromaffin cells and blocks hERG Kv1 3 and Kv1 5 channels in HEK293 cells (IC 1 2 1 5 M) In mice models BAPTA-AM alters ethanol-induced behavioral responses and consumption highlighting its applicability in neuroscience and apoptosis research
Apexbio Technology LLC GSK-923295 1088965-37-0 10mM (in 1mL DMSO)
GSK-923295 (CAS 1088965-37-0) is a highly potent inhibitor targeting the centromere-associated protein E (CENP-E) a kinesin motor protein essential for proper chromosome alignment and progression from metaphase to anaphase during cell division By blocking microtubule-stimulated ATPase activity of CENP-E GSK-923295 stabilizes an ATP-bound intermediate resulting in significantly reduced enzymatic function (IC50 3 2 nM) In cellular models GSK-923295 induces mitotic arrest with morphological changes similar to CENP-E knockdown In mouse xenograft models using Colo205 colon carcinoma cells administration of GSK-923295 leads to tumor growth inhibition and increased apoptosis supporting its utility in cancer research
Apexbio Technology LLC JNJ-26481585 875320-29-9 10mM (in 1mL DMSO)
JNJ-26481585 (CAS 875320-29-9) is a small-molecule inhibitor targeting class I histone deacetylases (HDACs) specifically HDAC1 HDAC2 and HDAC3 with reported IC50 values of 0 11 0 33 and 4 8 nM respectively It exhibits potent anti-proliferative activity across various human cancer cell lines including lung breast colon prostate ovarian and brain cancers (IC50 range 3 1 246 nM) Mechanistically JNJ-26481585 induces histone H3 acetylation alleviates HDAC-mediated repression of the p21waf1 cip1 promoter and promotes apoptosis in colorectal cancer cell models Consequently this compound serves as a research tool for cancer epigenetics and therapeutic assessment
Apexbio Technology LLC GW501516 317318-70-0 10mM (in 1mL DMSO)
GW501516 is a subtype-selective synthetic agonist targeting peroxisome proliferator-activated receptor delta (PPAR ) exhibiting a Ki value of approximately 1 1 nM PPAR widely expressed in various tissues mediates cholesterol metabolism and interacts with retinoid X receptor (RXR) In cellular reporter assays utilizing a GAL4-driven system GW501516 activates PPAR -dependent transcription with an EC50 value close to 1 2 nM and demonstrates roughly 1000-fold greater selectivity toward PPAR compared to other PPAR isoforms Experimental studies in primate models of metabolic disease have shown GW501516 promotes HDL-cholesterol elevation reduces fasting triglycerides modifies LDL/VLDL particle profiles to larger forms enhances cholesterol efflux via increasing ABCA1 expression and partially reduces hyperinsulinemia without adverse effects on glucose handling GW501516 serves as a research tool for exploring the mechanisms and functions of PPAR activation in metabolic regulation
Apexbio Technology LLC Cyclopamine 4449-51-8 10mM (in 1mL DMSO)
Cyclopamine (CAS 4449-51-8) is a naturally occurring steroidal alkaloid that selectively inhibits the Hedgehog (Hh) signaling pathway a conserved cascade involved in cellular proliferation and differentiation In human breast cancer cell lines (MCF-7 and MDA-MB-231) cyclopamine treatment (10 20 M) significantly suppresses proliferation induces cell cycle arrest at G1 phase and reduces invasive capabilities In FXR-bla assays cyclopamine exhibits an EC50 of 10 57 M As an Hh-antagonist it is widely utilized in research examining embryogenesis cancer biology tumor invasiveness and developmental defects
Apexbio Technology LLC BYL-719 1217486-61-7 10mM (in 1mL DMSO)
BYL-719 (CAS 1217486-61-7) is a selective inhibitor of PI3K demonstrating minimal activity against PI3K or isoforms Through targeting PI3K an essential node frequently dysregulated via PIK3CA mutations in various cancers BYL-719 effectively disrupts downstream proliferative signaling In biochemical assays BYL-719 shows potent inhibition of PI3K with an IC50 of 5 nM Preclinical evaluations indicate dose-dependent antitumor efficacy in xenograft tumor models and proliferation arrest and apoptosis induction in multiple myeloma cell lines exhibiting PIK3CA overexpression Clinically initial studies reveal manageable safety profiles and preliminary antitumor responses notably in PIK3CA-mutant malignancies supporting continued exploration in oncology research settings
Apexbio Technology LLC Didanosine 69655-05-6 10mM (in 1mL DMSO)
Didanosine is a nucleoside analogue known to inhibit reverse transcriptase enzymes by acting as a competitive inhibitor and terminator of viral DNA elongation Mechanistically didanosine is phosphorylated intracellularly to its active metabolite dideoxyadenosine triphosphate (ddATP) an analog of dATP Incorporation of ddATP into viral DNA by viral reverse transcriptase causes premature termination of DNA synthesis thereby inhibiting retroviral replication Didanosine is frequently employed as an experimental tool in studies examining antiviral activity and resistance mechanisms in retroviral infection models particularly HIV research In vitro assays commonly report IC50 values for didanosine against HIV reverse transcriptase in the range of approximately 0 5 to 10 M varying according to experimental conditions and viral strain sensitivity evaluated
Apexbio Technology LLC Roflumilast 162401-32-3 10mM (in 1mL DMSO)
Roflumilast is an orally available selective inhibitor of phosphodiesterase-4 (PDE-4) with an IC50 value of approximately 0 11 nM PDE-4 enzymes catalyze the hydrolysis of cyclic adenosine monophosphate (cAMP) and are predominantly expressed in various inflammatory and immune cells By selectively inhibiting PDE-4 activity Roflumilast elevates intracellular cAMP levels thus regulating cellular inflammatory signaling pathways This mechanism supports its use in the reduction of inflammatory responses associated with chronic obstructive pulmonary disease (COPD) Additionally Roflumilast has been investigated experimentally regarding its potential influence on glucose metabolism in early-stage type 2 diabetes mellitus
Apexbio Technology LLC Calcifediol 19356-17-3 10mM (in 1mL DMSO)
Calcifediol also termed calcidiol is a hydroxylated vitamin D3 metabolite and the primary circulating form of vitamin D3 in humans Functioning as a prehormone it undergoes further hydroxylation to calcitriol which activates vitamin D receptor (VDR) signaling pathways In vitro assays indicate that calcifediol induces CYP24A1 expression (EC50 70 nM) and thrombomodulin expression at concentrations between 10-100 nM Calcifediol dose-dependently promotes nuclear translocation of VDR at concentrations from 0 1 to 10 M in cultured cells In vivo experiments demonstrated that calcifediol administration influences calcium binding protein expression and calcium transport Clinically calcifediol administration rapidly elevates circulating 25(OH)D3 concentrations facilitating precise modulation of vitamin D status Therefore calcifediol is utilized in biomedical research related to vitamin D metabolism calcium homeostasis and VDR-associated pathways