Dimethyl Sulfoxide
Apexbio Technology LLC RO5126766(CH5126766) 946128-88-7 10mM (in 1mL DMSO)
RO5126766 (CH5126766 CAS 946128-88-7) is a dual Raf/MEK inhibitor that targets the RAS/RAF/MEK/ERK signaling pathway involved in cellular proliferation survival and differentiation By inhibiting RAF-dependent MEK1 phosphorylation and subsequent MEK-mediated ERK activation RO5126766 suppresses downstream signaling In vitro kinase assays show IC50 values of 0 0082 0 056 M for MEK1 phosphorylation and 0 16 M for MEK1-induced ERK2 activation Studies in KRAS-mutant cancer cell lines such as HCT116 and NCI-H460 demonstrate that RO5126766 blocks MEK and ERK phosphorylation effectively inducing cell cycle arrest at the G1 stage Thus RO5126766 serves as a valuable research tool for investigating tumor biology driven by MAPK signaling dysregulation
Apexbio Technology LLC Losmapimod 585543-15-3 10mM (in 1mL DMSO)
Losmapimod (CAS 585543-15-3) also known as GW856553 is a selective orally bioavailable inhibitor of p38 mitogen-activated protein kinase (MAPK) It exhibits potent inhibitory activity against p38 and p38 isoforms with reported pKi values of 8 1 and 7 6 respectively By inhibiting p38 MAPK a kinase essential in inflammatory signaling pathways and cytokine production Losmapimod has demonstrated beneficial effects in preclinical and clinical models It improves nitric oxide-mediated vasodilation and reduces markers of systemic inflammation such as C-reactive protein and fibrinogen This molecule is utilized in research studies addressing inflammation-driven cardiovascular disorders hypercholesterolemia and chronic obstructive pulmonary disease (COPD)
Apexbio Technology LLC RK-33 1070773-09-9 10mM (in 1mL DMSO)
RK-33 is a small molecule inhibitor targeting DDX3 an RNA helicase frequently overexpressed in various cancer types including lung cancer DDX3 overexpression correlates with poorer survival outcomes in lung cancer patients suggesting therapeutic relevance Mechanistically RK-33 inhibits DDX3 enzymatic activity thereby disrupting downstream signaling pathways particularly the -catenin-dependent Wnt signaling axis In vitro studies indicate RK-33 induces cell cycle arrest at G1 phase promotes apoptosis and enhances cellular radiosensitivity in DDX3-high expressing cell lines (e g A549 H1299 H23 and H460 IC50 4 4 8 4 M) In preclinical in vivo testing using a Twist1/KrasG12D mouse lung cancer model combined treatment of RK-33 with radiation resulted in reduced tumor growth compared with radiation alone RK-33 serves as a research tool to investigate DDX3 biology and potential therapeutic strategies for cancers with elevated DDX3 expression
Apexbio Technology LLC PF-4708671 1255517-76-0 10mM (in 1mL DMSO)
PF-4708671 (CAS 1255517-76-0) is a cell-permeable small molecule that specifically inhibits p70 ribosomal S6 kinase 1 (S6K1) S6K1 regulates diverse cellular processes including protein synthesis and insulin signaling pathways PF-4708671 inhibits S6K1 with an IC50 of 160 nM in HEK293 cell-derived enzyme assays and has a reported Ki value of 20 nM in vitro It selectively inhibits S6K1 over structurally related kinases such as RSK2 and MSK1 hindering phosphorylation of downstream substrates including ribosomal protein S6 mTOR and Rictor PF-4708671 is valuable in biomedical research involving cancer and insulin resistance
Apexbio Technology LLC Posaconazole 171228-49-2 10mM (in 1mL DMSO)
Posaconazole a triazole antifungal derivative of itraconazole acts by inhibition of sterol 14 -demethylase involved in fungal ergosterol biosynthesis It binds directly to the enzyme s heme cofactor blocking conversion of lanosterol into downstream sterol intermediates disrupting fungal membrane integrity and cellular function Posaconazole shows inhibitory activity in vitro against Candida albicans strains (IC50 0 007 0 3 g/ml) and Aspergillus species including A fumigatus and A flavus (IC50 0 03 g/ml) It is commonly utilized in biomedical research investigating fungal biology and drug resistance mechanisms
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 SAR245409 (XL765) 1349796-36-6 10mM (in 1mL DMSO)
SAR245409 (XL765 CAS 1349796-36-6) is a selective dual inhibitor of phosphatidylinositol-3-kinase (PI3K) and mammalian target of rapamycin (mTOR) with high potency against PI3K (IC50 9 nM) It suppresses the PI3K/Akt/mTOR signaling cascade by preventing formation of phosphatidylinositol-3 4 5-triphosphate (PIP3) at the cell membrane and downstream phosphorylation of AKT p70S6 kinase and S6 SAR245409 demonstrates antitumor activity in cancer models exhibiting genetic alterations in PI3K pathways enhancing growth suppression and apoptosis It is commonly employed in preclinical studies evaluating PI3K/mTOR-targeted approaches in cancer therapy
Apexbio Technology LLC AZD8931 (Sapitinib) 848942-61-0 10mM (in 1mL DMSO)
AZD8931 (Sapitinib CAS 848942-61-0) is a reversible small-molecule inhibitor that targets EGFR (HER1) HER2 (erbB2) and HER3 (erbB3) with similar potency It suppresses receptor phosphorylation with IC50 values of 4 nM (EGFR) 3 nM (HER2) and 4 nM (HER3) Preclinical studies using HER2-non-amplified inflammatory breast cancer (IBC) cell lines demonstrate reduced tumor cell proliferation and increased apoptosis upon AZD8931 administration In mouse xenograft models AZD8931 alone or combined with paclitaxel significantly delays tumor growth AZD8931 is under clinical evaluation as combination therapy in advanced breast cancer
Apexbio Technology LLC Doxercalciferol 54573-75-0 10mM (in 1mL DMSO)
Doxercalciferol chemically known as 1 -Hydroxyvitamin D2 is a synthetic analog of vitamin D2 characterized by selective activation of the vitamin D receptor (VDR) Upon metabolic activation Doxercalciferol undergoes hepatic transformation to its biologically active form inducing gene transcription mediated via the VDR signaling pathway Central to its mechanism activated VDR regulates calcium and phosphate homeostasis influencing cellular differentiation proliferation and parathyroid hormone expression In biomedical research Doxercalciferol serves as a tool compound to investigate the molecular pathways regulated by vitamin D receptor activation particularly in renal insufficiency models bone metabolism studies and parathyroid physiology experiments
Apexbio Technology LLC MK-8776 (SCH-900776) 891494-63-6 10mM (in 1mL DMSO)
MK-8776 (SCH-900776 CAS number 891494-63-6) is a selective small molecule inhibitor targeting the serine/threonine kinase checkpoint kinase 1 (Chk1) Chk1 is involved in detecting DNA damage and regulating DNA replication particularly in stabilizing replication forks during genotoxic stress SCH-900776 selectively inhibits Chk1 activity (IC50 3 nM) over Chk2 and Cdk3 In cellular assays SCH-900776 treatment results in dose-dependent inhibition of Chk1 autophosphorylation at Ser296 accompanied by increased phosphorylation at Ser345 a cellular marker consistent with checkpoint disruption In preclinical models combining SCH-900776 with DNA-damaging agents such as gemcitabine enhances anti-tumor efficacy marking its potential utility in cancer research
Medchemexpress LLC Carbocysteine sulfoxide | 5439-87-2 | MFCD21364079 | 99.0% | 195.19 g/mol | C5H9NO5S | 10 MG
Carbocysteine sulfoxide is a small-molecule impurity of carbocisteine intended for research use. The substance is identified by CAS number 5439-87-2, has the molecular formula C5H9NO5S, and a molecular weight of 195.19 g/mol. It is provided in small-mass packages for laboratory and analytical applications.
- Used as an impurity reference for analytical method development.
- Supplied in small-mass packages suitable for laboratory research.
- Identified by CAS number 5439-87-2 for substance tracking.
- Molecular formula C5H9NO5S and molecular weight 195.19 g/mol.
- Intended for research use only; not for human or clinical use.
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 CH5138303 959763-06-5 10mM (in 1mL DMSO)
CH5138303 (CAS 959763-06-5) is a potent inhibitor targeting Heat Shock Protein 90 (HSP90) exhibiting strong binding affinity with a Kd of 0 48 nM HSP90 a molecular chaperone regulates protein folding stability and degradation and maintains oncogenic proteins crucial to tumor cell proliferation CH5138303 effectively reduces protein levels and phosphorylation of HSP90 client proteins including Raf1 AKT EGFR and HER2 in NCI-N87 cancer cells In animal studies using human gastric cancer NCI-N87 xenografts oral administration of CH5138303 demonstrates significant antitumor activity achieving a tumor growth inhibition (TGI) rate of 136% at an ED of 3 9 mg/kg
Apexbio Technology LLC GDC-0449 (Vismodegib) 879085-55-9 10mM (in 1mL DMSO)
GDC-0449 (Vismodegib CAS 879085-55-9) is a small molecule that selectively inhibits the Hedgehog (Hh) signaling pathway by binding to the Smoothened (SMO) receptor thus preventing downstream activation of Hh target genes implicated in cellular proliferation and differentiation This compound emerged from screening small-molecule libraries followed by medicinal chemistry optimization Preclinical evaluation demonstrated antitumor activity in murine models of medulloblastoma and xenograft models derived from human colon and pancreatic cancers Currently GDC-0449 is under investigation for locally advanced and metastatic solid tumors