Dimethyl Sulfoxide
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 Anacetrapib (MK-0859) 875446-37-0 10mM (in 1mL DMSO)
Anacetrapib (MK-0859 CAS 875446-37-0) is a selective inhibitor of cholesteryl ester transfer protein (CETP) an enzyme involved in mediating the transfer of cholesteryl esters and triglycerides between lipoproteins In biochemical assays anacetrapib exhibits potent inhibition of CETP-driven lipid transfer with reported IC50 values of 16 nM for cholesteryl ester transfer and 29 nM for triglyceride transfer Metabolically it undergoes oxidation via CYP3A4 to form metabolites M1 M2 and M3 Due to its effect of significantly lowering LDL cholesterol and elevating HDL cholesterol anacetrapib is studied in research related to primary hypercholesterolemia and mixed dyslipidemia
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 Santacruzamate A (CAY10683) 1477949-42-0 10mM (in 1mL DMSO)
Santacruzamate A (CAY10683 CAS 1477949-42-0) is a selective histone deacetylase (HDAC) inhibitor originally identified in the marine cyanobacterium cf Symploca sp Its mechanism of action involves targeting HDAC enzymes particularly demonstrating high selectivity towards HDAC2 (IC 0 112 nM) when compared with HDAC6 (IC 433 nM) and minimal potency against HDAC4 (IC 1 M) In cellular assays Santacruzamate A reduces growth of tumor cell lines such as HCT-116 colon cancer cells (GI 28 M) and HuT-78 cutaneous T-cell lymphoma cells (GI 1 3 M) It is valuable in epigenetics and oncology research for selectively modulating HDAC2 activity
Apexbio Technology LLC AZD1152 722543-31-9 10mM (in 1mL DMSO)
AZD1152 (CAS 722543-31-9) is a highly selective inhibitor of Aurora kinase a family of serine/threonine kinases involved in cancer cell proliferation It preferentially targets Aurora B kinase (IC50 0 37 nM) with lesser affinity toward Aurora A (IC50 1 37 M) and exhibits no notable activity against other kinases such as JAK2 FLT3 and Abl AZD1152 induces tumor cell cycle arrest in the G2/M phase triggers apoptosis and enhances radiosensitivity in androgen-resistant prostate cancer models In vivo AZD1152 demonstrates anti-tumor potency both alone and combined with chemotherapeutics or tubulin-targeting drugs offering a valuable research tool for oncology studies
Apexbio Technology LLC MI-77301 (SAR405838) 1303607-60-4 10mM (in 1mL DMSO)
MI-77301 (SAR405838 CAS 1303607-60-4) is a selective antagonist targeting the murine double minute 2 (MDM2) protein an E3 ubiquitin ligase responsible for negatively regulating tumor-suppressor p53 via ubiquitination and degradation By inhibiting the MDM2-p53 interaction (Ki 0 88 nM) MI-77301 stabilizes p53 elevates protein levels of p53 p21 and MDM2 and induces apoptosis Preclinical studies demonstrate selective growth inhibition in tumor cell lines harboring wild-type p53 (e g SJSA-1 RS4 11 LNCaP HCT-116) and potent tumor regressions in corresponding xenograft mouse models highlighting its utility for mechanistic studies and cancer therapeutic research
Apexbio Technology LLC BKM120 944396-07-0 10mM (in 1mL DMSO)
BKM120 (CAS 944396-07-0) is a potent orally bioavailable inhibitor of class I phosphatidylinositol 3-kinases (PI3Ks) specifically targeting the isoforms p110 p110 p110 and p110 with IC50 values of 52 nM 166 nM 262 nM and 116 nM respectively By blocking PI3K activity this molecule suppresses downstream phosphorylation of AKT an important mediator within the PI3K-AKT-mTOR signaling cascade implicated in tumor growth and survival Preclinical studies demonstrate that BKM120 restricts tumor cell proliferation promotes cell cycle arrest at G1 phase and induces apoptosis particularly noted in PTEN-deficient cancer models Thus BKM120 serves as a useful tool for studying PI3K pathway-dependent cancers
Apexbio Technology LLC KN-93 139298-40-1 10mM (in 1mL DMSO)
KN-93 (CAS 139298-40-1) is a selective inhibitor of calcium/calmodulin-dependent protein kinase II (CaMKII) a serine/threonine kinase activated by calcium-bound calmodulin KN-93 inhibits CaMKII enzymatic activity with reported IC50 values of approximately 0 37 0 5 M in vitro and a Ki value of 2 58 M against cardiac CaMKII In NIH 3T3 cells KN-93 (12 M) induces G1 cell-cycle arrest and at higher concentrations (24 M) promotes apoptosis Due to CaMKII s role in neuronal function cardiac signaling immune activation and disease states including Alzheimer s and arrhythmias KN-93 serves as a tool compound for studying CaMKII-mediated processes in biomedical research