Dimethyl Sulfoxide
Apexbio Technology LLC Hesperadin 422513-13-1 10mM (in 1mL DMSO)
Hesperadin is a small-molecule ATP-competitive inhibitor targeting Aurora B kinase a serine/threonine-protein kinase involved in mitotic regulation By occupying the ATP-binding pocket of Aurora B and adjacent hydrophobic regions Hesperadin suppresses kinase activity with an IC50 approximately 250 nM In mitotic cells Aurora B-mediated phosphorylation of histone H3 Ser-10 is inhibited by Hesperadin this phosphorylation event is widely utilized as a mitotic biomarker Furthermore experimental applications of Hesperadin include investigating cell-cycle dynamics chromosome alignment and spindle checkpoint mechanisms as evidenced by its ability to disrupt proper chromosome alignment and segregation at approximately 40 nM IC50
Apexbio Technology LLC Entecavir Hydrate 209216-23-9 10mM (in 1mL DMSO)
Entecavir hydrate is an antiviral compound that acts as a reverse transcriptase (RT) inhibitor specifically targeting hepatitis B virus (HBV) infection It inhibits HBV DNA replication by interacting with the viral reverse transcriptase enzyme thus preventing the synthesis of complementary DNA from the viral RNA template Entecavir hydrate is frequently employed in antiviral studies and clinical research related to hepatitis B treatment regimens In studies involving chronic HBV-infected patients entecavir hydrate combined with peginterferon alpha-2b therapy has shown significant suppression of viral DNA levels and reduced covalently closed circular DNA (cccDNA) within hepatocytes The reported IC50 value of entecavir hydrate against HBV DNA polymerase activity typically ranges below 10 nM in cellular assay systems enabling its utility in both preclinical and clinical antiviral investigations
Apexbio Technology LLC BI 2536(Synonyms: BI-2536, BI2536, Plk1 inhibitor BI 2536), 10mM (in 1mL DMSO), CAS: 755038-02-9.
BI 2536 (CAS number 755038-02-9) is an ATP-competitive inhibitor selectively targeting human polo-like kinase 1 (PLK1) exhibiting an IC50 value of approximately 0 83 nM Comparatively BI 2536 shows substantially less affinity towards other kinases In vitro studies demonstrate that BI 2536 inhibits proliferation of various human tumor cell lines (EC50 values ranging from 2 to 25 nM) and induces G2/M cell cycle arrest accompanied by apoptosis as evidenced in HeLa cervical cancer cells In vivo data from xenograft tumor models indicate that BI 2536 administered intravenously on a weekly or biweekly schedule possesses antitumor efficacy
Apexbio Technology LLC Latrepirdine 97657-92-6 10mM (in 1mL DMSO)
Latrepirdine (CAS 97657-92-6) is an orally bioavailable small molecule investigated for its neuroprotective properties in preclinical studies of neurodegenerative diseases including Alzheimer s and Huntington s diseases Although its precise mechanism remains under investigation latrepirdine has demonstrated the ability to inhibit neuronal cell death pathways in animal disease models Moreover preliminary evidence indicates potential cognitive enhancement in normal physiological conditions Latrepirdine serves as a relevant tool compound to study neuronal survival mechanisms and cognitive function regulation
Apexbio Technology LLC Olmesartan 144689-24-7 10mM (in 1mL DMSO)
Olmesartan (CAS 144689-24-7) is a small molecule angiotensin II receptor antagonist primarily acting by selectively blocking the binding of angiotensin II to AT1 receptors This mechanism interrupts angiotensin II-mediated vasoconstriction and aldosterone secretion resulting in antihypertensive effects In biomedical research Olmesartan serves as a valuable tool for examining hypertensive disease models elucidating angiotensin II signaling pathways and exploring therapeutic strategies targeting cardiovascular regulation
Apexbio Technology LLC PCI-32765 (Ibrutinib) 936563-96-1 10mM (in 1mL DMSO)
PCI-32765 (Ibrutinib) is a small-molecule inhibitor targeting Bruton s tyrosine kinase (BTK) a cytoplasmic kinase integral to B-cell receptor (BCR) signaling By covalently binding to BTK active sites PCI-32765 disrupts downstream signaling cascades essential for B-cell maturation and activation Dysfunction or inhibition of BTK correlates with impaired B-cell development and reduction in autoantibody production PCI-32765 is commonly utilized in biomedical research to explore BTK-dependent signaling pathways elucidate molecular mechanisms underlying B-cell mediated disorders and examine therapeutic potential in B-cell malignancies and autoimmune models
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 MK 0893 870823-12-4 10mM (in 1mL DMSO)
MK 0893 is a small molecule antagonist targeting both the glucagon receptor (GCGR) and insulin-like growth factor-1 receptor (IGF-1R) It competitively and reversibly inhibits glucagon binding to GCGR subsequently reducing receptor-mediated cAMP production In cell-based assays utilizing CHO cells expressing human GCGR MK 0893 showed nanomolar-level inhibitory potency with a receptor binding IC50 around 6 6 nM and a cellular cAMP inhibition IC50 near 15 7 nM Additionally MK 0893 exhibits potent inhibitory activity on IGF-1R demonstrated in IGF-1-driven mouse xenograft tumor models Therefore MK 0893 serves as a relevant pharmacological tool in research related to type 2 diabetes and IGF-1R-mediated oncogenic signaling pathways
Apexbio Technology LLC BML-210(CAY10433) 537034-17-6 10mM (in 1mL DMSO)
BML-210 (CAY10433 CAS 537034-17-6) is a small molecule inhibitor targeting histone deacetylases (HDACs) enzymes responsible for removing acetyl groups from lysine residues on histone proteins leading to chromatin compaction and transcriptional repression BML-210 demonstrates HDAC inhibitory activity with an IC50 of 87 M In cellular assays this compound increases FXN mRNA expression and histone H4 acetylation induces G1 cell cycle arrest and apoptosis and enhances erythroid and granulocytic differentiation in human leukemia cell lines (K562 HL-60) BML-210 is utilized in research investigating epigenetic modulation leukemia biology and gene regulation mechanisms
Apexbio Technology LLC Go 6983(Synonyms: GO-6983, GO6983, PKC Inhibitor GO 6983, Pan-PKC Inhibitor GO-6983, PKC inhibitor GO6983, 133053-19-7), 10mM (in 1mL DMSO), CAS: 133053-19-7.
Go 6983 (CAS 133053-19-7) is a selective inhibitor of protein kinase C isoforms PKC PKC PKC PKC and PKC with reported IC50 values of approximately 7 nM 7 nM 6 nM 10 nM and 20 mM respectively Protein kinase C (PKC) isoforms act as receptors for tumor-promoting phorbol ester mediating various downstream cellular functions In cancer cell models Go 6983 suppresses PKC and PKC activation induced by phorbol esters and reduces PKC expression inhibiting cell survival pathways It is frequently employed in biomedical studies examining PKC-dependent signaling in cancer progression and epithelial-to-mesenchymal transition (EMT)
Apexbio Technology LLC Teriflunomide 108605-62-5 10mM (in 1mL DMSO)
Teriflunomide (CAS 108605-62-5) the active metabolite of the antirheumatic agent Leflunomide acts primarily by selectively inhibiting dihydroorotate dehydrogenase (DHODH) a mitochondrial enzyme critical for pyrimidine nucleotide synthesis By restricting pyrimidine production teriflunomide exerts antiproliferative effects on activated lymphocytes resulting in immunosuppressive and anti-inflammatory activity Due to these properties teriflunomide is extensively studied as an oral therapeutic candidate in multiple sclerosis research addressing autoimmune-mediated disorders
Apexbio Technology LLC Methotrexate 59-05-2 10mM (in 1mL DMSO)
Methotrexate is a folate antagonist commonly utilized in biomedical research due to its inhibitory action on dihydrofolate reductase (DHFR) a critical enzyme in folate metabolism This inhibition disrupts nucleotide synthesis thereby interfering with cell proliferation Upon cell uptake methotrexate is converted intracellularly into polyglutamate derivatives which prolong its biochemical activity through sustained enzyme inhibition Additionally methotrexate promotes extracellular adenosine release at inflammatory sites mediating immunological effects In cellular assays for DHFR inhibition methotrexate demonstrates potent inhibitory activity with reported IC50 values typically ranging from 5 to 50 nM depending on the cell type and experimental conditions Methotrexate is widely utilized in research on inflammation oncology and rheumatoid arthritis-related mechanisms
Apexbio Technology LLC FK866 (APO866) 658084-64-1 10mM (in 1mL DMSO)
FK866 (APO866 CAS 658084-64-1) is a small-molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) an enzyme involved in NAD biosynthesis FK866 inhibits NMPRTase with reported IC50 values ranging from 0 09 to 27 2 nM Due to elevated NAD turnover in cancer cells inhibition of NAD synthesis selectively induces cell death in cancerous cells FK866 reduces ATP production by decreasing cellular NAD availability resulting in mitochondrial membrane depolarization and caspase-independent cell death Preclinical studies demonstrate activity against hematologic cancer cell lines including AML with minimal toxicity to normal hematopoietic progenitors FK866 suppresses tumor growth in vivo and prolongs survival making it useful in oncology research related to NAD metabolism