Dimethyl Sulfoxide
Medchemexpress LLC ML-792 | CAS No. : 1644342-14-2 | 10 mM * 1 mL in DMSO
ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50> values of 32 μM and >100 μM, respectively).
Apexbio Technology LLC Fludarabine(Synonyms: Fludarabine Phosphate, Fludara, Fludarabinum, 2-Fluoro-ara-AMP, 9H-Purin-6-amine), 10mM (in 1mL DMSO), CAS: 21679-14-1.
Fludarabine (CAS 21679-14-1) is a purine analog prodrug that inhibits DNA synthesis Upon cellular uptake it undergoes phosphorylation to its active triphosphate form (F-ara-ATP) disrupting DNA replication through inhibition of critical enzymes such as DNA primase DNA ligase I ribonucleotide reductase and DNA polymerases and In human myeloma RPMI8226 cell assays fludarabine suppressed cell growth reduced Akt phosphorylation and lowered anti-apoptotic proteins XIAP and Survivin In vivo studies demonstrated marked tumor growth inhibition in RPMI8226 xenograft models Fludarabine serves as a tool in oncology research particularly leukemia and multiple myeloma-related studies
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 Org 27569 868273-06-7 10mM (in 1mL DMSO)
Org 27569 (CAS 868273-06-7) is an allosteric modulator targeting the cannabinoid CB1 receptor It enhances the binding of the agonist CP55940 to purified CB1 receptors while simultaneously inhibiting receptor functionality In electrically-stimulated mouse vas deferens assays Org 27569 reduced WIN55212-induced contractions exhibiting a pEC50 of 8 24 0 12 and a maximal response (Emax) of approximately 45 4% Binding studies suggest its interaction at a putative allosteric site on CB1 receptors reflected by parameters such as a pKB of 5 67 0 23 and a Log of 1 14 0 17 Org 27569 serves as a tool compound for studying CB1 receptor allosteric modulation
Apexbio Technology LLC AZD6244 (Selumetinib) 606143-52-6 10mM (in 1mL DMSO)
AZD6244 (Selumetinib CAS 606143-52-6) is a small-molecule inhibitor selectively targeting MEK1/2 components of the MAP kinase signaling cascade It inhibits MEK1 via a non-ATP-competitive mechanism with an IC50 of 14 1 nM leading to decreased phosphorylation of downstream targets ERK1/2 (IC50 10 3 nM cellular assays) AZD6244 exhibits minimal off-target activity against related kinases including MKK6 EGFR ErbB2 and B-Raf In tumor cell lines harboring activated Ras or B-Raf mutations AZD6244 reduces cell proliferation and inhibits growth in xenograft models Thus AZD6244 is useful for investigating MAP kinase pathway-driven malignancies
Apexbio Technology LLC PF-562271 HCl 939791-41-0 10mM (in 1mL DMSO)
PF-562271 HCl (CAS 939791-41-0) is a potent ATP-competitive reversible inhibitor targeting focal adhesion kinase (FAK) and its homolog proline-rich tyrosine kinase 2 (Pyk2) It inhibits FAK and Pyk2 enzymatic activity with reported IC50 values of 1 5 nmol/L and 14 nmol/L respectively FAK is a non-receptor tyrosine kinase regulating cell adhesion migration and growth while Pyk2 shares structural similarity to FAK In animal models of cancer PF-562271 reduces tumor progression and metastatic spread with dose-dependent suppression of FAK phosphorylation (EC50 93 ng/mL) Thus PF-562271 serves as an important tool for investigating FAK/Pyk2-mediated pathways in oncology research
Apexbio Technology LLC PKI-402 1173204-81-3 10mM (in 1mL DMSO)
PKI-402 (CAS 1173204-81-3) is an ATP-competitive inhibitor targeting class I PI3Ks (PI3K ) with IC50 values of 1 nM 7 nM 16 nM and 14 nM respectively PI3Ks are enzymes central to the PI3K/Akt/mTOR signaling pathway impacting cellular proliferation survival differentiation and migration processes critically involved in cancer progression PKI-402 reduces cell growth and phosphorylation of PI3K/mTOR downstream signaling proteins in human tumor cell lines including breast glioma pancreatic and non-small cell lung cancers In xenograft mouse models (MDA-MB-361) PKI-402 administration suppresses Akt phosphorylation triggers apoptosis (PARP cleavage) and inhibits tumor growth highlighting its significance for cancer biology research
Apexbio Technology LLC R428 1037624-75-1 10mM (in 1mL DMSO)
R428 (CAS 1037624-75-1) is a potent selective inhibitor of the receptor tyrosine kinase Axl demonstrating an IC50 of 14 nM In comparison to related kinases such as Abl Mer Tyro3 InsR EGFR HER2 and PDGFR R428 displays greater than 50-fold selectivity for Axl By inhibiting Axl catalytic function R428 disrupts downstream intracellular signaling pathways including Akt phosphorylation cellular invasion pro-inflammatory cytokine production angiogenesis and epithelial-mesenchymal transition mediator expression (e g Snail) Preclinical studies utilizing animal xenograft tumor models indicate its capacity to reduce metastatic tumor burden and extend survival both alone and combined with cisplatin R428 is orally bioavailable and represents a valuable tool for cancer research targeting Axl-driven pathogenesis