Dimethyl Sulfoxide
AdipoGen DAF-4T Solution 5 mM in DMSO
Chemical. CAS 212558-80-0. Formula C20H7Cl2N3O5. MW 440.19. Fluorescent reference compound for DAF-4 DA CDX-D0216. Spectral data lambdaEx=505nm lambdaEm=530nm.
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 SU6656 330161-87-0 10mM (in 1mL DMSO)
SU6656 (CAS 330161-87-0) is a selective small-molecule inhibitor targeting Src family tyrosine kinases enzymes involved in pathways promoting cellular survival proliferation angiogenesis and invasion In NIH 3T3 cells SU6656 suppresses PDGF- and Src-induced cell cycle progression and c-Myc expression In UT-7/TPO leukemia cells SU6656 induces cell cycle arrest with increased DNA content and elevates CD41/CD61 surface expression Additionally SU6656 enhances radiation-mediated endothelial apoptosis and vascular disruption by inhibiting Src-dependent Akt phosphorylation suggesting its potential utility in antitumor angiogenesis research
Apexbio Technology LLC Bosutinib (SKI-606)(Synonyms: SKI-606, Bosulif, SKI606, Bosutinib monohydrate), 10mM (in 1mL DMSO), CAS: 380843-75-4.
Bosutinib (SKI-606 CAS 380843-75-4) is a dual inhibitor targeting c-Src and Abl kinases with IC50 values of approximately 1 2 nM and 1 nM respectively It suppresses phosphorylation of Bcr-Abl Src and Stat5 in chronic myeloid leukemia (CML) cells thereby decreasing proliferation and inducing regression in K562 xenograft tumor models Bosutinib also reduces Src autophosphorylation and inhibits -catenin signaling by blocking its interaction with TCF4 transcription factor consequently downregulating cyclin D1 expression in colorectal cancer cells This mechanism results in decreased cell motility and enhanced -catenin binding to E-cadherin highlighting utility in cancer research
Apexbio Technology LLC PCI-24781 (CRA-024781) 783355-60-2 10mM (in 1mL DMSO)
PCI-24781 (CRA-024781 CAS 783355-60-2) is a histone deacetylase (HDAC) inhibitor targeting HDAC1 HDAC2 HDAC3 HDAC6 HDAC8 and HDAC10 with reported Ki values of 7 19 8 2 17 280 and 24 nM respectively HDAC enzymes catalyze the removal of acetyl groups from lysine residues on histone proteins thereby regulating chromatin structure and gene expression PCI-24781 induces dose-dependent hyperacetylation of histones and tubulin in human cancer cells (HCT116 DLD-1) leading to apoptosis via p21 upregulation PARP cleavage and H2AX accumulation PCI-24781 demonstrates antitumor activity against multiple tumor cell lines and in xenograft models highlighting its utility for oncology research
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 Linsitinib(Synonyms: OSI-906, ASP7487, IGF-1R inhibitor OSI-906, IGF-1R/IR inhibitor OSI-906, OSI906), 10mM (in 1mL DMSO), CAS: 867160-71-2.
Linsitinib (CAS 867160-71-2) also known as OSI-906 is a small-molecule inhibitor targeting both insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF-1R) kinases It exhibits potent inhibitory effects with IC50 values of 75 nM against IR and 35 nM against IGF-1R In vitro studies using the 3T3/hulGF-1R (LISN) cell line demonstrate that Linsitinib inhibits IGF-1R ligand-dependent autophosphorylation and downstream signaling via pERK1/2 pAKT and p-p70S6K It shows antiproliferative activity across multiple cancer cell lines and exhibits dose-dependent tumor growth inhibition in LISN xenograft animal models supporting its utility in oncology research
Apexbio Technology LLC Mesna 19767-45-4 10mM (in 1mL DMSO)
Mesna chemically classified as a sulfhydryl-containing compound functions primarily as a protective adjuvant during chemotherapy with oxazaphosphorine agents (such as cyclophosphamide and ifosfamide) Its mode of action involves direct binding and detoxification of urotoxic metabolites notably acrolein thereby facilitating their conversion into stable non-toxic derivatives and mitigating associated bladder toxicity Due to this detoxifying effect Mesna is widely utilized in oncology research and clinical studies investigating chemotherapy-induced urotoxicity prevention Additionally given its structural feature as a thiol donor Mesna finds applications in experimental studies exploring its antioxidant activity and potential cytoprotective effects
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 Avasimibe 166518-60-1 10mM (in 1mL DMSO)
Avasimibe (CAS 166518-60-1) is an orally bioavailable inhibitor of acyl-coenzyme A cholesterol acyltransferase (ACAT) an enzyme involved in cholesterol esterification It exhibits potent inhibition with an IC50 of approximately 60 nM In cell-based studies avasimibe reduces intracellular cholesterol esters in a dose-dependent manner without elevating free cholesterol levels suggesting an advantageous safety profile Additionally avasimibe reduces synthesis and secretion of Apo B 100 a constituent of very low-density lipoprotein (VLDL) in HepG2 cells and increases bile acid synthesis in rat hepatocytes Beyond dyslipidemic modulation and anti-atherogenic activities it influences amyloid precursor protein (APP) trafficking reducing its maturation and subsequent amyloid-beta (A ) peptide generation providing avenues for Alzheimer s disease research
Apexbio Technology LLC GSK2656157 1337532-29-2 10mM (in 1mL DMSO)
GSK2656157 (CAS 1337532-29-2) is a highly selective inhibitor of protein kinase R-like endoplasmic reticulum kinase (PERK) demonstrating an IC50 of 0 9 nM In kinase selectivity assays involving 300 kinases GSK2656157 displays marked specificity for PERK In cellular studies using BxPC3 pancreatic cancer cells this compound blocks PERK signaling reducing phosphorylation of downstream targets including eIF2 ATF4 and CHOP and subsequently suppressing protein synthesis In animal models bearing human tumor xenografts including pancreatic (BxPC3 HPAC Capan2) and multiple myeloma (NCI-H929) oral administration of GSK2656157 results in dose-dependent inhibition of tumor growth with notable sensitivity in Capan2 tumors
Apexbio Technology LLC MK-1775 955365-80-7 10mM (in 1mL DMSO)
MK-1775 (CAS 955365-80-7) is a selective inhibitor targeting Wee1 kinase a nuclear Ser/Thr kinase involved in regulating entry into mitosis Mechanistically it inhibits Wee1-mediated Tyr15 phosphorylation of cyclin-dependent kinase 1 (CDC2) thus activating CDC2 and disrupting the G2 DNA damage checkpoint MK-1775 exhibits potent inhibition of Wee1 kinase with an in vitro IC50 of 5 2 nM and demonstrates substantial selectivity over related kinases including Myt1 In cell models harboring mutant p53 (e g WiDr) co-treatment with MK-1775 sensitizes tumor cells to DNA-damaging agents such as gemcitabine carboplatin and cisplatin highlighting its utility in cancer research