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 GSK 650394 890842-28-1 10mM (in 1mL DMSO)
GSK 650394 is a small-molecule inhibitor selectively targeting serum- and glucocorticoid-regulated kinase 1 (SGK1) showing inhibition through competitive binding mechanism with an IC50 of approximately 13 nM in fluorescence polarization assays SGK1 functions as an androgen-regulated kinase inhibition of this signaling reduces androgen-driven growth in prostate cancer cell lines Experimental studies demonstrate that GSK 650394 blocks SGK1 and SGK2 kinase activity with IC50 values of 62 nM and 103 nM respectively assessed by scintillation proximity assays Additionally GSK 650394 reduces androgen-induced phosphorylation of SGK substrate Nedd4-2 and suppresses androgen-stimulated proliferation of prostate cancer LNCaP cells (IC50 1 M) suggesting its use in prostate cancer research as a potential therapeutic strategy
Apexbio Technology LLC PF-670462 950912-80-8 10mM (in 1mL DMSO)
PF-670462 (CAS 950912-80-8) is a selective inhibitor of casein kinase 1 (CK1) isoforms CK1 and CK1 serine/threonine kinases involved in circadian rhythm regulation It exhibits inhibitory activity toward CK1 and CK1 with IC50 values of approximately 80 nM and 13 nM respectively In cellular models co-transfected with GFP-tagged PER3 and human CK1 PF-670462 blocks nuclear translocation of PER3 In primary fibroblasts from wild-type mice it dose-dependently prolongs circadian cycle length PF-670462 serves as a useful chemical tool for studying CK1-mediated modulation of circadian rhythms
Apexbio Technology LLC Golvatinib (E7050) 928037-13-2 10mM (in 1mL DMSO)
Golvatinib (E7050 CAS 928037-13-2) is a small-molecule inhibitor targeting the tyrosine kinases c-Met and VEGFR-2 Golvatinib inhibits phosphorylation of c-Met in MKN45 gastric cancer cells and VEGFR-2 in human umbilical vein endothelial cells (HUVECs) with IC50 values of 14 nM and 16 nM respectively Additionally it suppresses proliferation of various tumor cells including MKN45 EBC-1 Hs746T and SNU-5 and inhibits tumor growth in xenograft models via reduction of c-Met and VEGFR-2-mediated pathways Golvatinib is utilized in cancer research to explore targeted antitumor efficacy related to angiogenesis and oncogenic signaling
Apexbio Technology LLC Marimastat 154039-60-8 10mM (in 1mL DMSO)
Marimastat (CAS 154039-60-8) also known as BB-2516 is an orally bioavailable inhibitor of matrix metalloproteases (MMPs) Structurally it contains a collagen-mimicking hydroxamate moiety that facilitates covalent binding to the zinc atom at MMP active sites Marimastat exhibits broad-spectrum inhibitory activity against MMP-1 MMP-2 MMP-7 MMP-9 and MMP-14 with IC50 values of 5 nM 6 nM 13 nM 3 nM and 9 nM respectively In animal models of metastatic cancers Marimastat reduces tumor dissemination and progression Clinically Marimastat is investigated for potential therapeutic effects against metastatic and non-metastatic solid tumors such as pancreatic and gastric cancers
Apexbio Technology LLC Lomustine 13010-47-4 10mM (in 1mL DMSO)
Lomustine (CAS 13010-47-4) is an anticancer small molecule belonging to the nitrosourea class of alkylating agents It exerts its antitumor effects primarily by forming DNA cross-links leading to impaired replication and selective cytotoxicity in rapidly dividing tumor cells Lomustine shows inhibitory activity against various cancer cell lines including breast cancer (ZR-75-1 IC50 25 M) astrocytoma (U87MG IC50 8 8 M) and colon carcinoma (LS174T IC50 13 M) Due to its lipophilic nature lomustine efficiently crosses the blood-brain barrier facilitating its use in research involving central nervous system malignancies and related leukemia models
Apexbio Technology LLC NU7441 (KU-57788) 503468-95-9 10mM (in 1mL DMSO)
NU7441 (KU-57788 CAS 503468-95-9) is a selective inhibitor targeting DNA-dependent protein kinase (DNA-PK) via competition with ATP exhibiting an IC50 of approximately 13 nM and a Ki of 0 65 nM It demonstrates high specificity showing minimal inhibition of related kinases ATM and ATR at concentrations up to 100 M and substantially weaker activity towards mTOR and PI3K (IC50 values of 1 7 and 5 M respectively) NU7441 sensitizes HeLa cells to etoposide enhancing cytotoxicity and augments tumor growth delay when co-administered in SW620 xenograft mouse models The molecule serves as a tool compound in DNA repair and oncology research
Apexbio Technology LLC SP2509 1423715-09-6 10mM (in 1mL DMSO)
SP2509 (CAS 1423715-09-6) is a small molecule antagonist of lysine-specific demethylase 1 (LSD1/KDM1A) a histone-modifying enzyme responsible for demethylating mono- and dimethylated histone H3 lysine 4 (H3K4) SP2509 potently inhibits LSD1 activity (IC50 13 nM) without affecting monoamine oxidase isoforms MAO-A or MAO-B In acute myeloid leukemia (AML) cells SP2509 suppresses LSD1 function reduces colony formation induces apoptosis enhances promoter-specific H3K4 trimethylation and stimulates differentiation through upregulation of p53 p21 and C/EBP Its efficacy has been demonstrated in AML xenograft models supporting its utility as a tool compound for cancer research