Dimethyl Sulfoxide
Apexbio Technology LLC AG-1478 153436-53-4 10mM (in 1mL DMSO)
AG-1478 is a selective inhibitor of epidermal growth factor receptor (EGFR) a receptor tyrosine kinase involved in cellular proliferation and survival It inhibits EGFR-mediated Erk1/2 phosphorylation induced by EGF stimulation with an IC50 of approximately 10 M in Ishikawa ovarian cell lines In experimental cancer research AG-1478 has been applied to study EGFR signaling mechanisms by reducing receptor phosphorylation and downstream pathway activation Studies using diverse cancer cell lines including ovarian (CAOV-3 SKOV-3) colorectal (SW480) hepatocellular (HA22T/VGH) and lung (A549) carcinomas employ AG-1478 to investigate EGFR s role in tumor growth and chemoresistance Additionally AG-1478 is utilized in preclinical xenograft models to assess tumor growth modulation via EGFR inhibition
Apexbio Technology LLC Axitinib (AG 013736) 319460-85-0 10mM (in 1mL DMSO)
Axitinib (CAS 319460-85-0) also known as AG 013736 is an orally bioavailable selective inhibitor targeting vascular endothelial growth factor receptor (VEGFR) tyrosine kinases 1 2 and 3 It inhibits VEGFR phosphorylation with IC50 values of approximately 0 1 nM (VEGFR-1) 0 2 nM (VEGFR-2) and 0 1 0 3 nM (VEGFR-3) and demonstrates significantly higher selectivity relative to FGFR-1 Axitinib reduces phosphorylation of VEGF-mediated intracellular signaling proteins Akt eNOS and ERK1/2 and exhibits in vivo suppression of VEGFR-2 activation (EC50 0 49 nM) Its antiangiogenic action results in tumor growth delay in human xenograft models (e g HCT-116 SN12C) highlighting its utility in cancer research
Apexbio Technology LLC PP 2 (AG 1879) 172889-27-9 10mM (in 1mL DMSO)
PP 2 (AG 1879 CAS 172889-27-9) is a selective inhibitor targeting Src family tyrosine kinases such as Lck and Fyn with reported IC50 values of approximately 4 nM and 5 nM respectively Src family kinases are composed of nine closely related tyrosine kinases including Src Yes Fyn Fgr Yrk Lyn Blk Hck and Lck PP 2 suppresses early T-cell signaling by blocking Lck- and Fyn-mediated tyrosine phosphorylation following anti-CD3 stimulation Research in glioma cell models (U251) has demonstrated PP 2-mediated inhibition of Src-dependent cellular invasion and proliferation at micromolar concentrations PP 2 exhibits moderate inhibitory activity toward EGF-R (IC50 480 nM) and minimal effect on ZAP-70 and JAK2 Thus PP 2 serves as a research tool for studying Src kinase-dependent signaling pathways implicated in cancer and immunological responses
Apexbio Technology LLC Rucaparib (AG-014699,PF-01367338) 459868-92-9 10mM (in 1mL DMSO)
Rucaparib (AG-014699 PF-01367338 CAS 459868-92-9) is a small molecule inhibitor targeting poly(ADP-ribose) polymerase (PARP) a nuclear enzyme activated by DNA damage and central to the base excision repair pathway By blocking PARP activity rucaparib impairs DNA repair especially in cells with pre-existing DNA repair deficiencies such as those induced by genotoxic stress In prostate cancer research rucaparib induces radiosensitization notably in PTEN-deficient cells expressing ETS fusion proteins through inhibition of non-homologous end joining (NHEJ) It is thus relevant in studies investigating DNA damage response pathways cancer biology and therapeutic radiosensitization strategies
Apexbio Technology LLC Pterostilbene(Synonyms: 3,5-Dimethoxy-4'-hydroxy-trans-stilbene, Trans-3,5-dimethoxy-4'-hydroxystilbene), 10mM (in 1mL DMSO), CAS: 537-42-8.
Pterostilbene (CAS 537-42-8) is a naturally occurring stilbenoid identified in extracts derived from the plant Pterocarpus indicus Structurally related to resveratrol it demonstrates improved bioavailability and enhanced biological activity Mechanistically pterostilbene exhibits antioxidant anti-inflammatory and antitumor properties primarily mediated through activation of sirtuins and modulation of cell-signaling pathways such as NF- B AMPK and PI3K/Akt Due to these activities pterostilbene is widely utilized in biochemical research exploring cellular aging oxidative stress inflammation and cancer biology Storage is recommended under airtight conditions in cool dry environments
Apexbio Technology LLC GMX1778 (CHS828) 200484-11-3 10mM (in 1mL DMSO)
GMX1778 (CHS828 CAS 200484-11-3) is a small-molecule inhibitor targeting nicotinamide phosphoribosyltransferase (NAMPT) an enzyme crucial for NAD biosynthesis with a reported Kd value of 120 nM NAD functions as a cofactor essential for enzymatic oxidation-reduction processes and diverse cellular events including metabolism genomic integrity calcium signaling aging and apoptosis In cultured IM-9 cells exposure to GMX1778 substantially decreases NAD and NM levels in a time-dependent manner GMX1778 displays anti-tumor activity preferentially in NAPRT1-deficient cancer models highlighting its potential utility for investigating metabolic vulnerabilities and targeted cancer therapies
Apexbio Technology LLC NVP DPP 728 dihydrochloride 247016-69-9 10mM (in 1mL DMSO)
NVP DPP 728 dihydrochloride (CAS 247016-69-9) is a potent orally active inhibitor of dipeptidyl peptidase IV (DPP-IV) Mechanistically it reversibly inhibits human DPP-IV enzyme through formation of a nitrile-dependent complex characterized by transitional-state kinetic properties exhibiting a Ki of 11 nM In aged rat models oral administration of NVP DPP 728 reduces plasma DPP-IV activity enhances early-phase insulin secretion and improves glucose tolerance following glucose challenge This compound is under preclinical investigation for type 2 diabetes research targeting the DPP-IV/glucagon-like peptide-1 pathway
Apexbio Technology LLC Resveratrol 501-36-0 10mM (in 1mL DMSO)
Resveratrol is a naturally occurring polyphenolic phytoalexin known to function as an activator of the NAD-dependent protein deacetylase SIRT1 Through SIRT1 activation resveratrol modulates downstream pathways implicated in cellular metabolism inflammation aging and tumorigenesis Commonly employed in biomedical research settings resveratrol serves as a molecular tool to explore the regulatory roles and signaling mechanisms involving sirtuin-mediated pathways Cellular assays have demonstrated resveratrol s inhibitory activity against multiple targets with reported IC50 values typically ranging from 20 to 50 M depending on cell type and experimental conditions Therefore resveratrol is widely utilized in vitro and in vivo to elucidate its roles in metabolic regulation inflammation responses cardiovascular function and cancer biology
Apexbio Technology LLC Tretinoin (Aberela) 302-79-4 10mM (in 1mL DMSO)
Tretinoin (Aberela) is a pharmacologically active derivative of vitamin A (retinoic acid) widely utilized in biomedical research primarily for its therapeutic effects against acne vulgaris and keratosis follicularis At the cellular level tretinoin increases intracellular reduced glutathione levels and enhances catalase enzyme activity thus helping ameliorate oxidative stress caused by hydrogen peroxide in renal mesangial cell models It modulates inflammatory responses by suppressing expression of TNF- 1 and osteopontin proteins in renal tissue of aged rat models and regulates immunity in murine models by inhibition of lymphocyte proliferation and IL-17 secretion coupled with enhanced IL-10 production Additionally topical application in acne treatment research investigates its anti-inflammatory properties in combination formulations
Apexbio Technology LLC SLx-2119 911417-87-3 10mM (in 1mL DMSO)
SLx-2119 (CAS 911417-87-3) also known as KD-025 is a selective inhibitor targeting Rho-associated protein kinase 2 (ROCK2) exhibiting an IC50 of approximately 105 nM ROCK2 is a serine/threonine kinase central to cytoskeletal modulation and cellular signaling particularly expressed within neuronal and vascular cells SLx-2119 reduces connective tissue growth factor (CTGF) mRNA expression selectively in human intestinal smooth muscle cells isolated from radiation-induced fibrosis tissue (RE-SMC) whereas normal smooth muscle cells remain unaffected Additionally in a murine model of focal cerebral ischemia SLx-2119 treatment yields a dose-dependent decrease in infarct size across aged and diabetic models highlighting its research applicability in ischemic stroke and fibrotic disorders