Dimethyl Sulfoxide
Apexbio Technology LLC DMOG 89464-63-1 10mM (in 1mL DMSO)
DMOG (Dimethyloxalylglycine CAS 89464-63-1) is a small molecule inhibitor of prolyl-4-hydroxylase domain (PHD) enzymes thereby modulating the stability of hypoxia-inducible factor (HIF) PHD inhibition by DMOG prevents HIF-1 prolyl hydroxylation and subsequent degradation stabilizing HIF-1 protein even under normoxic conditions (0 1 1 mmol/L in vitro) Additionally DMOG treatment suppresses NF- B signaling during LPS-induced inflammatory responses in animal models improving survival rates and enhancing IL-10 expression predominantly in peritoneal B-1 cells Thus DMOG serves as a valuable research tool to explore hypoxia signaling pathways and inflammatory responses
Apexbio Technology LLC THZ2 1604810-84-5 10mM (in 1mL DMSO)
THZ2 (CAS 1604810-84-5) is a selective inhibitor of cyclin-dependent kinase 7 (CDK7) demonstrating an IC50 of 13 9 nM CDK7 a serine/threonine kinase bound and activated by cyclins regulates cell cycle progression and transcriptional control through phosphorylation of RNA polymerase II (RNAPII) In triple-negative breast cancer (TNBC) cell models THZ2 reduces cellular proliferation induces apoptotic cell death without affecting cell-cycle distribution and inhibits colony formation at low-nanomolar concentrations (IC50 10 nM) In xenograft mouse models THZ2 suppresses tumor growth without noticeable toxicity Thus THZ2 is useful in research investigating CDK7-mediated oncogenic mechanisms in cancer
Apexbio Technology LLC Ezetimibe 163222-33-1 10mM (in 1mL DMSO)
Ezetimibe (CAS 163222-33-1) is a cholesterol absorption inhibitor that targets the intestinal cholesterol transporter Niemann-Pick C1 Like 1 (NPC1L1) It reduces intestinal uptake of cholesterol and dietary carotenoids including - and -carotene lycopene lutein and -cryptoxanthin through downregulating transport proteins such as SR-BI ABCA1 NPC1L1 and transcription factors including SREBP-1/-2 and LXR- In ApoE-deficient mouse models ezetimibe significantly decreases plasma cholesterol levels and attenuates atherosclerotic lesion formation Clinically it lowers LDL cholesterol total cholesterol and triglycerides while elevating HDL cholesterol
Apexbio Technology LLC RO4929097(Synonyms: RO-4929097, RO 4929097, Gamma-Secretase Inhibitor RO4929097, RO4929097 γ-secretase inhibitor), 10mM (in 1mL DMSO), CAS: 847925-91-1.
RO4929097 (CAS 847925-91-1) is a potent selective small-molecule inhibitor of -secretase an essential protease in the Notch signaling pathway It inhibits -secretase with high specificity (IC50 4 nM EC50 5 nM) showing minimal inhibitory activity against closely related proteases and over 100-fold selectivity versus a broad spectrum of other proteases By preventing Notch receptor cleavage and subsequent signaling activation RO4929097 suppresses proliferation and tumorigenesis across various tumor models including melanoma breast colorectal pancreatic and lung cancers Clinical studies have assessed RO4929097 alone or combined with other anticancer agents for advanced solid tumors
Apexbio Technology LLC (-)-JQ1 1268524-71-5 10mM (in 1mL DMSO)
(-)-JQ1 (CAS 1268524-71-5) is a stereoisomer of ( )-JQ1 designed as a negative control in bromodomain inhibition studies Unlike ( )-JQ1 a competitive BET bromodomain inhibitor known to displace BRD4 fusion oncoproteins from chromatin the (-)-enantiomer shows negligible interaction with tested bromodomains It exhibits minimal inhibitory activity against BRD4(1) with an IC50 of 10 000 nM Due to the lack of significant bromodomain binding (-)-JQ1 serves widely as an appropriate negative control compound in experiments investigating BET protein functions and related signaling
Apexbio Technology LLC Argatroban 74863-84-6 10mM (in 1mL DMSO)
Argatroban is a synthetic small-molecule inhibitor acting as a direct binder to thrombin s active site thereby blocking the thrombin-mediated conversion of fibrinogen into fibrin It competitively inhibits thrombin-induced platelet activation and blood clot formation exhibiting an inhibitory constant (Ki) of approximately 19 nM Due to its specificity and direct mechanism Argatroban is frequently employed in experimental research scenarios to investigate thrombin-dependent coagulation pathways platelet aggregation studies and antithrombotic effects in various in vitro assays and animal thrombosis models
Apexbio Technology LLC Macitentan 441798-33-0 10mM (in 1mL DMSO)
Macitentan (CAS 441798-33-0) is a small molecule endothelin receptor antagonist acting as a dual inhibitor of ETA and ETB receptors Experimental data using recombinant ETA-expressing CHO cells show that macitentan exhibits potent inhibition of ET-1 ligand binding with an IC50 of approximately 0 5 nM whereas its inhibitory effect on ETB receptors in similar CHO cell systems is weaker (IC50 391 nM) In vivo rodent studies indicate macitentan rapidly converts into ACT-132577 a circulating metabolite with extended half-life and retained dual receptor antagonism This pharmacological profile makes macitentan relevant for biomedical research on endothelin-associated vascular pathologies
Apexbio Technology LLC ML216 1430213-30-1 10mM (in 1mL DMSO)
ML216 (CAS 1430213-30-1) is a small molecule inhibitor targeting Bloom (BLM) helicase a DNA unwinding enzyme essential for homologous recombination-mediated DNA repair ML216 inhibits DNA unwinding activity of full-length BLM (IC50 3 0 M) and a truncated form BLM636-1298 (IC50 0 97 M) displaying sub-micromolar selectivity relative to other helicases such as RECQ1 RECQL5 and bacterial UvrD In cellular assays ML216 selectively suppresses proliferation in BLM-containing fibroblasts increasing sister chromatid exchange frequency consistent with BLM functional deficiency By inhibiting BLM helicase ML216 may sensitize tumor cells to conventional DNA-damaging therapeutics indicating potential application in cancer research and therapy development
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 Pazopanib (GW-786034) 444731-52-6 10mM (in 1mL DMSO)
Pazopanib (GW-786034 CAS 444731-52-6) is a second-generation multitargeted receptor tyrosine kinase inhibitor selectively targeting vascular endothelial growth factor receptors (VEGFR) platelet-derived growth factor receptors (PDGFR) and c-kit Through blockade of these kinase activities pazopanib suppresses signaling cascades essential for angiogenesis and cellular proliferation Preclinical tumor models indicate that pazopanib alone or combined with chemotherapy demonstrates substantial anti-angiogenic and antitumor efficacy Its distinct inhibitory profile of intracellular VEGFR tyrosine kinases offers valuable applications in oncology research particularly in investigating angiogenesis-driven signaling pathways
Apexbio Technology LLC Taxifolin 480-18-2 10mM (in 1mL DMSO)
Taxifolin (CAS number 480-18-2) a bioactive flavonoid isolated primarily from coniferous species of the Pinaceae family exhibits notable antioxidant anti-inflammatory and chemopreventive properties It functions primarily through free radical scavenging and modulation of oxidative stress pathways reducing cellular damage associated with reactive oxygen species (ROS) Taxifolin further influences various signaling cascades involved in inflammation and apoptosis regulation Due to these pharmacological attributes it is widely utilized in biomedical research exploring oxidative stress-related diseases inflammatory conditions and potential cancer therapeutic avenues For optimal stability maintain storage conditions sealed dry and cool
Apexbio Technology LLC Piceatannol 10083-24-6 10mM (in 1mL DMSO)
Piceatannol (CAS 10083-24-6) is a naturally occurring small molecule exhibiting anti-inflammatory immunomodulatory and antiproliferative activities It functions primarily by inhibiting protein tyrosine kinases including p56lck and syk kinases and suppressing tumor necrosis factor (TNF)-induced nuclear factor-kappa B (NF- B) activation and downstream gene expression Biologically piceatannol arises as a metabolite of resveratrol through oxidation by cytochrome P450 1B1 This compound is employed in biomedical research to explore kinase signaling pathways inflammatory response regulation and potential therapeutic interventions
Apexbio Technology LLC Veliparib dihydrochloride 912445-05-7 10mM (in 1mL DMSO)
Veliparib dihydrochloride (CAS 912445-05-7) is a selective inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 enzymes responsible for DNA repair processes frequently upregulated in various cancers Veliparib inhibits PARP1 and PARP2 with K(i) values of 5 2 and 2 9 nmol/L respectively In colon cancer cell lines (HCT-116 HT-29) veliparib enhances DNA damage and induces G2/M arrest when combined with SN38 or oxaliplatin In preclinical murine melanoma (B16F10) breast cancer (MX-1) and colon cancer (HCT-116) xenografts combination therapy with DNA-damaging agents shows improved antitumor effects