Dimethyl Sulfoxide
Apexbio Technology LLC Cyclophosphamide 50-18-0 10mM (in 1mL DMSO)
Cyclophosphamide is a nitrogen mustard alkylating prodrug activated via hepatic enzymes to its active metabolites These metabolites alkylate DNA primarily at guanine residues resulting in DNA cross-linking strand breaks and mutations consequently triggering cytotoxic effects Cyclophosphamide exhibits cytotoxicity in vitro with an IC50 of 37 6 M in mouse embryo BALB/c 3T3 cells and an IC50 of 8 79 M against human HL60 cells It impacts immune regulation by decreasing regulatory T cell counts and suppressive marker expression (FoxP3 GITR) facilitating immune response modulation Commonly applied in cancer and immunological research cyclophosphamide is also employed in genotoxicity assays due to its capacity to induce chromosomal aberrations and mutations
Apexbio Technology LLC Tivozanib (AV-951) 475108-18-0 10mM (in 1mL DMSO)
Tivozanib (AV-951 CAS 475108-18-0) is a quinoline-urea derivative functioning as a potent inhibitor of vascular endothelial growth factor receptors (VEGFR) It primarily targets VEGFR-2 kinase demonstrating significant inhibitory activity in picomolar ranges (IC50 of approximately 160 pM) Additionally Tivozanib displays considerable selectivity causing minimal off-target interaction with c-kit In cellular assays it inhibits PDGFR and c-kit phosphorylation at nanomolar levels Preclinical evaluations revealed antitumor activity across multiple solid tumor xenograft models particularly renal cell carcinoma (RCC) Its mechanism and selectivity profile render it valuable for cancer research clinical investigation and preclinical efficacy assessments
Apexbio Technology LLC Canagliflozin(Synonyms: Invokana, TA-7284, JNJ-28431754, Sulisent, Canagliflozin hemihydrate), 10mM (in 1mL DMSO), CAS: 842133-18-0.
Canagliflozin (CAS 842133-18-0) is a selective inhibitor of sodium-glucose cotransporter 2 (SGLT2) a transporter responsible for renal glucose reabsorption By inhibiting SGLT2 activity Canagliflozin decreases renal glucose reabsorption resulting in increased urinary glucose excretion In CHO cells expressing human rat or mouse SGLT2 Canagliflozin potently inhibits sodium-dependent glucose uptake with IC50 values of 4 4 3 7 and 2 0 nM respectively Animal studies using db/db mice and Zucker diabetic fatty (ZDF) rats demonstrate dose-dependent reductions in blood glucose as well as decreased respiratory exchange ratio and body weight Canagliflozin is suitable for in vivo research through oral administration
Apexbio Technology LLC SL-327 305350-87-2 10mM (in 1mL DMSO)
SL-327 (CAS 305350-87-2) is a selective inhibitor targeting MEK1 and MEK2 kinases exhibiting IC50 values of 0 18 M and 0 22 M respectively MEK1/2 mediate the phosphorylation and activation of extracellular signal-regulated kinases (ERK) crucial components of the MAPK/ERK signaling pathway SL-327 treatment lowers phosphorylated ERK levels and subsequent activation of transcription factors including CREB Elk-1 and c-Fos influencing gene expression linked to synaptic plasticity In animal models SL-327 modulates drug-induced behaviors and neuronal plasticity processes making it a relevant molecular tool to investigate MAPK/ERK signaling pathways in neuroscience research
Apexbio Technology LLC Dorsomorphin 2HCl 1219168-18-9 10mM (in 1mL DMSO)
Dorsomorphin 2HCl (CAS 1219168-18-9) is a small-molecule inhibitor targeting BMP signaling through selective blockade of BMP type I receptors ALK2 ALK3 and ALK6 It prevents phosphorylation of downstream effectors SMAD1/5/8 with an IC50 of approximately 0 47 mM Originally identified by zebrafish phenotypic screening as a disruptor of embryonic dorsoventral patterning Dorsomorphin has been employed to dissect BMP-regulated pathways in iron homeostasis significantly affecting hepcidin expression and iron metabolism in vitro and in vivo It is widely utilized in mechanistic studies of BMP function and signaling regulation
Apexbio Technology LLC Afatinib (BIBW2992) 439081-18-2 10mM (in 1mL DMSO)
Afatinib (BIBW2992 CAS 439081-18-2) is an irreversible inhibitor targeting receptor tyrosine kinases in the ErbB protein family specifically EGFR (ErbB1) and HER2 (ErbB2) By covalently binding to their kinase domains it suppresses downstream ErbB signaling showing demonstrated inhibition with IC50 values of 0 5 nM for EGFR and 14 nM for HER2 Afatinib blocks EGF-induced phosphorylation and cellular proliferation in multiple EGFR- or HER2-expressing lines including A431 NIH-3T3-HER2 NCI-N87 and BT-474 Research applications include tumor xenograft studies and transgenic lung cancer models evaluating EGFR-dependent oncogenic processes and therapeutic responses
Apexbio Technology LLC JNK-IN-8 1410880-22-6 10mM (in 1mL DMSO)
JNK-IN-8 (CAS 1410880-22-6) is a potent and specific inhibitor of c-Jun N-terminal kinase (JNK) isoforms JNK1 JNK2 and JNK3 It functions by forming a covalent bond with a conserved cysteine residue in JNKs inducing conformational alteration in the kinase activation loop consequently impairing substrate binding Its IC50 values for JNK1 JNK2 and JNK3 are 4 67 nM 18 7 nM and 0 98 nM respectively In cellular assays JNK-IN-8 prevention of c-Jun phosphorylation demonstrates robust selectivity towards the JNK signaling pathway thus making it valuable as a research tool in studying stress-related cellular responses and apoptosis
Apexbio Technology LLC RG7112 939981-39-2 10mM (in 1mL DMSO)
RG7112 (CAS 939981-39-2) is a selective small-molecule inhibitor of the interaction between the tumor suppressor protein p53 and its negative regulator MDM2 By blocking MDM2-p53 binding RG7112 releases and stabilizes p53 thereby enhancing the transcriptional activation of genes responsible for cell cycle arrest and apoptosis RG7112 preferentially inhibits proliferation in cancer cells harboring wild-type p53 exhibiting IC50 values ranging from 0 18 to 2 2 M whereas its efficacy diminishes significantly in p53-mutant cells RG7112 is used as a tool compound in biomedical research investigating p53-dependent antitumor mechanisms and pathways affecting hematopoiesis