Dimethyl Sulfoxide
Apexbio Technology LLC XL335 629664-81-9 10mM (in 1mL DMSO)
XL335 (CAS 629664-81-9) is a selective orally bioavailable agonist of the farnesoid X receptor (FXR) displaying an EC50 of approximately 4 nM In Hep3B liver cancer cells XL335 activation of FXR reduces interleukin-6-induced C-reactive protein (CRP) expression at both mRNA and protein levels In vivo studies indicate that XL335 diminishes lipopolysaccharide (LPS)-stimulated inflammatory responses and fructose-induced hepatic inflammation by suppressing acute-phase proteins (e g SAP SAA3) and adipose differentiation-related protein (ADRP) Thus XL335 serves as a valuable tool for investigating FXR-mediated pathways involved in liver inflammation and metabolic disorders
Apexbio Technology LLC Dinaciclib (SCH727965)(Synonyms: SCH-727965, SCH727965, Dinaciclib, MK-7965, MK7965), 10mM (in 1mL DMSO), CAS: 779353-01-4.
Dinaciclib (SCH727965 CAS 779353-01-4) is a small-molecule inhibitor targeting cyclin-dependent kinases (CDKs) specifically CDK1 CDK2 CDK5 and CDK9 It exhibits inhibitory potencies with IC50 values of 3 nM for CDK1 1 nM for CDK2 and CDK5 and 4 nM for CDK9 By suppressing CDK activity dinaciclib interrupts cell cycle progression reduces phosphorylation of retinoblastoma (Rb) protein and triggers apoptosis In addition dinaciclib interacts with the acetyl-lysine binding regions within bromodomains Currently in clinical phases I/II it demonstrates antitumor activity both in vitro and in animal models highlighting its potential applicability in oncology research
Apexbio Technology LLC LCL161 1005342-46-0 10mM (in 1mL DMSO)
LCL161 (CAS 1005342-46-0) is a small-molecule antagonist targeting inhibitor of apoptosis (IAP) proteins specifically designed as a mimetic of the endogenous second mitochondria-derived activator of caspase (SMAC) LCL161 binds to and inhibits XIAP and cIAP1/2 proteins frequently overexpressed in malignant cells It demonstrates antiproliferative activity in vitro against selected hepatocellular carcinoma cell lines (Hep3B PLC5) and hematologic cancer models (ALL) with IC50 values in the micromolar range In in vivo tumor xenograft studies oral administration of LCL161 has led to significant growth delays across various malignancies including osteosarcoma and glioblastoma Its combination with AAVP-delivered TNF- results in synergistic antitumor effects indicating its utility in oncology research
Apexbio Technology LLC Thioridazine HCl 130-61-0 10mM (in 1mL DMSO)
Thioridazine HCl is a pharmacological inhibitor targeting dopamine receptor subtypes D2 and D4 as well as a calcium channel blocker It modulates dopaminergic neurotransmission by interfering with receptor-mediated signaling and reduces intracellular calcium influx via calcium channel inhibition (IC50 approximately 1 0 M) Thioridazine is frequently utilized in research contexts involving dopaminergic signaling pathways calcium-related cellular processes and investigations of pharmacological sensitivity shifts following prolonged receptor modulation Specifically it is employed experimentally to examine receptor-mediated cardiovascular responses such as hypotension and to assess alterations in dopamine receptor responsiveness induced by chronic exposure regimens
Apexbio Technology LLC U-73122 112648-68-7 10mM (in 1mL DMSO)
U-73122 (CAS 112648-68-7) is a phospholipase C (PLC) inhibitor utilized in biomedical research By selectively targeting PLC an enzyme responsible for hydrolyzing phosphatidylinositol 4 5-bisphosphate into intracellular messengers diacylglycerol and inositol-triphosphate U-73122 attenuates downstream signaling events such as protein kinase C activation and intracellular calcium release In vitro U-73122 inhibits recombinant human PLC- 2 with an IC50 of approximately 6 M while minimally affecting PLC- 1 3 and 4 isoforms In animal models U-73122 demonstrates anti-inflammatory properties reducing carrageenan-induced rat paw edema and TPA-induced mouse ear edema
Apexbio Technology LLC Axitinib (AG 013736) 319460-85-0 10mM (in 1mL DMSO)
Axitinib (CAS 319460-85-0) also known as AG 013736 is an orally bioavailable selective inhibitor targeting vascular endothelial growth factor receptor (VEGFR) tyrosine kinases 1 2 and 3 It inhibits VEGFR phosphorylation with IC50 values of approximately 0 1 nM (VEGFR-1) 0 2 nM (VEGFR-2) and 0 1 0 3 nM (VEGFR-3) and demonstrates significantly higher selectivity relative to FGFR-1 Axitinib reduces phosphorylation of VEGF-mediated intracellular signaling proteins Akt eNOS and ERK1/2 and exhibits in vivo suppression of VEGFR-2 activation (EC50 0 49 nM) Its antiangiogenic action results in tumor growth delay in human xenograft models (e g HCT-116 SN12C) highlighting its utility in cancer research
Apexbio Technology LLC LDN193189 Hydrochloride 1062368-62-0 10mM (in 1mL DMSO)
LDN193189 Hydrochloride is a selective pharmacological inhibitor targeting BMP type I receptor kinases specifically activin receptor-like kinase 2 (ALK2) and ALK3 The compound acts by blocking receptor-mediated activation of Smad-dependent signaling pathways (Smad1/5/8 phosphorylation) as well as mitigating associated non-Smad signaling including phosphorylation of Akt and p38 Commonly utilized in biomedical research involving cellular differentiation epithelial barrier integrity and heterotopic ossification LDN193189 has shown the capacity to modulate BMP-induced phenotypic changes in various cell lines such as C2C12 myoblasts and bronchial epithelial cells and to influence related in vivo processes
Apexbio Technology LLC Z-FA-FMK 105637-38-5;197855-65-5 10mM (in 1mL DMSO)
Z-FA-FMK is a peptidyl fluoromethyl ketone inhibitor targeting cysteine proteases specifically cathepsins such as cathepsin B and certain caspases It does not require a P1 aspartate residue for inhibition Mechanistically Z-FA-FMK suppresses the enzyme activity of effector caspases (including caspases-2 -3 -6 and -7) but shows minimal impact on initiator caspases (caspase-8 and caspase-10) and only partial attenuation of caspase-9 activity As a negative control inhibitor Z-FA-FMK is regularly applied in apoptosis research to differentiate specific caspase-dependent signaling pathways and to assess the role of cathepsins and caspases in biological contexts such as cell death mechanisms and related pathways
Apexbio Technology LLC GW9662(Synonyms: GW-9662, GW 9662, 2-Chloro-5-nitro-N-phenylbenzamide, PPAR gamma antagonist GW9662), 10mM (in 1mL DMSO), CAS: 22978-25-2.
GW9662 (CAS 22978-25-2) is an antagonist of peroxisome proliferator-activated receptor gamma (PPAR ) a nuclear receptor involved in various biological processes including tumor growth and inflammation GW9662 irreversibly blocks PPAR activity by covalently modifying cysteine residues at its ligand-binding site (IC50 3 3 M) In cellular assays GW9662 inhibits proliferation of breast cancer cell lines (MCF7 MDA-MB-231 MDA-MB-468 IC50 20 30 M) Additionally GW9662 reverses the protective impact of lipopolysaccharide on kidney ischemia/reperfusion injury demonstrating its utility for studying PPAR -mediated pathways in oncology and inflammation models
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
Apexbio Technology LLC UNC0638 1255580-76-7 10mM (in 1mL DMSO)
UNC0638 is a selective inhibitor of histone methyltransferases G9a and GLP enzymes responsible for mono- and dimethylation of histone H3 lysine-9 (H3K9) It inhibits G9a and GLP activity with IC50 values of 15 nM and 19 nM respectively UNC0638 reduces cellular H3K9 dimethylation levels demonstrated in MDA-MB-231 cells with an IC50 of 81 9 nM at 48 hours It has been utilized in models to study epigenetic regulation including neuroendocrine tumor xenografts and hair cell damage induced by aminoglycosides addressing roles of H3K9 methylation in disease pathogenesis and therapeutic responses
Apexbio Technology LLC Rocilinostat (ACY-1215) 1316214-52-4 10mM (in 1mL DMSO)
Rocilinostat (ACY-1215 CAS 1316214-52-4) is a selective inhibitor of histone deacetylase 6 (HDAC6) HDAC6 enzymatically regulates various cellular processes including protein trafficking cell-cycle progression and cytoskeletal organization and its dysregulated activity is implicated in tumor progression and cancer metastasis Rocilinostat potently inhibits HDAC6 (IC50 5 nM) while showing minimal activity against other HDAC isoforms and sirtuins (IC50 1 M) Preclinical studies using multiple myeloma (MM) cell lines and xenograft mouse models demonstrated rocilinostat can enhance acetylation of -tubulin disrupt protein stability pathways and sensitize cancer cells to proteasome inhibitors such as bortezomib and carfilzomib resulting in increased apoptosis and reduction in tumor growth
Apexbio Technology LLC SEA0400 223104-29-8 10mM (in 1mL DMSO)
SEA0400 (CAS 223104-29-8) is a selective inhibitor of the sodium-calcium exchanger (NCX) an antiporter responsible for cellular calcium homeostasis by facilitating sodium-calcium ion exchange across membranes SEA0400 inhibits NCX activity at nanomolar concentrations (IC50 between 5-33 nM in neuronal and glial cell cultures) with substantially higher potency than KB-R7943 By blocking reverse-mode NCX function during reperfusion scenarios SEA0400 reduces pathological intracellular calcium influx and downstream pro-inflammatory mediator production It has demonstrated neuroprotective effects by reducing infarction volumes in rodent cerebral ischemia models as well as anti-arrhythmic properties in myocardial infarction models
Apexbio Technology LLC Levonorgestrel 797-63-7 10mM (in 1mL DMSO)
Levonorgestrel is a synthetic progesterone analog structurally categorized as a progestin exhibiting agonistic activity primarily through progesterone receptor (PR) binding and also showing interaction with estrogen receptors (ER) Upon receptor binding levonorgestrel modulates transcriptional activity influencing downstream gene expression related to reproductive processes This molecular interaction reduces luteinizing hormone levels inhibits ovulation and induces alterations in uterine lining and cervical mucus thus contributing to contraceptive activity Biomedically levonorgestrel is widely utilized in research for studying progesterone receptor signaling pathways hormonal regulation mechanisms and contraceptive drug development
Apexbio Technology LLC Reserpine 50-55-5 10mM (in 1mL DMSO)
Reserpine a naturally derived alkaloid isolated from plants of the genus Rauvolfia functions primarily through the inhibition of vesicular monoamine transporter 2 (VMAT2) By blocking VMAT2-mediated uptake reserpine causes depletion of monoamine neurotransmitters such as dopamine norepinephrine and serotonin from synaptic storage vesicles In biochemical assays reserpine inhibits VMAT2 activity with an IC50 value typically ranging from 30-50 nM depending on assay specifics In biomedical and pharmacological research this compound is commonly utilized to model neurotransmitter depletion mechanisms in vitro and in animal models facilitating studies on monoamine-related neurological disorders neurotransmission pathways as well as serotonergic dopaminergic and adrenergic signaling