2209 Results for: "Immunology"

Supplier: G-Biosciences

Imiquimod is a Toll-like receptor 7/8 agonist with anti-viral and anti-tumor properties.1 Enhances innate immune system leading to Th1-mediated antitumor immune response.2 Increases levels of IFNa, TNFa, and IL-12. Imiquimod has also been shown to act as an antagonist at adenosine A1 and A2A receptors augmenting its proinflammatory effects.3,4 Clinically useful for the treatment of basal cell carcinoma, actinic keratosis, and genital warts. Imiquimod also upregulates the expression of opioid growth factor receptor(OGFr).5,6 OGF is involved in regulation of inhibitory kinases in the cell cycle process.

Supplier: G-Biosciences

MCC-950 was originally found to act as a cytokine release inhibitory drug (CRID), arresting activated monocytes and preventing activation of caspase-11. Discovered to be a novel inhibitor of the NLRP3 and AIM2 inflammasomes2. Blocks canonical and noncanonical NLRP3 activation at nanomolar concentrations3. Inhibits interleukin 1β (IL-1β) secretion in vivo and attenuates the severity of experimental autoimmune encephalomyelitis (an MS disease model)3. Disrupts the interaction between AIM2 and ASC in a reconstituted cell-free inflammasome4. A valuable new tool for exploring the pathophysiology of NLRP.

Supplier: G-Biosciences

Metabolite resulting from the action of cholesterol 25-hydroxylase on cholesterol. However, since cholesterol 25-hydroxylase knock-out mice still have significant levels of 25-hydroxycholesterol there must be alternate pathways of generation that have yet to be determined.1 Likewise, the biological role of 25-hydroxycholesterol remains somewhat unclear. 25-Hydroxycholesterol is frequently mentioned as an important regulator of cholesterol metabolism, but apparently normal cholesterol regulation in organisms with both high and low levels of the compound make this association unclear. More recent reports have linked 25-hydroxycholesterol and one of it’s metabolites to immunoregulatory roles2, but more information is needed before it’s clear if that is indeed a primary role for the compound.

Supplier: G-Biosciences

Anacardic acids occur in cashew nut shells and are similar in structure to urushiols, the irritating components of poison ivy. Anacardic acid inhibits histone acetyltransferases (HATs) p300 (IC50 = 8.5 µM) and PCAF (IC50 = 5.0 µM) with no effect on HDACs 1. It also suppresses expression or activity of proteins involved in invasion and angiogenesis, e.g. MMP-2 (IC50 = 11 µM) and -92. 6-PDSA, a saturated form of anacardic acid, induces macrophage activation via MAPK and NF-κB3. When used at 125 µM, it sensitized cancer cells to radiation therapy by reducing histone expression4. It also blocks inducible and constitutive activation of NF-κB in leukemia cells5.

Supplier: G-Biosciences

Sitravatinib is a broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels.1 Sitravatinib has been tested in mouse models of sarcoma and showed better efficacy than both imatinib and crizotinib. Because of its unique kinase inhibition profile (especially that of TAM receptors), it has been used to restore response to anti-PD-1 therapy (nivolumab) in NSCLC patients.2 Sitravatinib was able to significantly alter the immunosuppressive tumor microenviro nMent in three preclinical tumor models to enhance the effects of PD-1 blockade therapy.

Supplier: TED PELLA INC MS

This barrier bag is ideal for storage of materials sensitive to moisture and/or oxygen. The inside dimensions measures with a resealable lock and a tear notch above the zipper.

Supplier: G-Biosciences

Selective Toll-like receptor 8 (TLR8) agonist (EC50 = 100 nM). It stimulates the production of TNFα and IL-12 from monocytes and myeloid dendritic cells. Motolimod also stimulated IFNγ production from NK cells and increased their toxicity against K562 and ADCC by rituximab and trastuzumab.1,2 It induced apoptosis in monocytic myeloid-derived suppressor cells.3 Motolimod is being investigated in combination with other cancer immunotherapies.4,5 Motolimod has also been shown in induce secreted IL-1b and IL-8 via activation of the NLRP3 inflammasome.

Supplier: G-Biosciences

Selective RORα partial inverse agonist (IC50=480 nM) – displays no activity at RORß, RORγ, or FXR.1 It was able to suppress gluconeogenesis in diet-induced obese mice. SR3335 was able to upregulate uncoupling protein 1 (UCP1), a unique mitochondrial protein devoted to thermogenesis, in wild type mice leading to decreased body weight and fat mass.2,3 It inhibited the development of mouse and human TH17 cells in vitro and in vivo leaving thymic T cells intact.4 SR3335’s ability to block pathogenic, but not protective TH17 cell function makes it an important new tool in the study of TH17-mediated inflammatory and autoimmune diseases.

Supplier: G-Biosciences

Epacadostat is a potent (IC50 = 10 nM)1 and selective inhibitor of indoleamine-2,3-dioxygenase 1 (IDO1) with no activity at IDO2 or TDO2. It restored tryptophan levels and significantly impaired kynurenine generation in CT26 colon carcinoma (IC50 = 76 nM) and PAN02 pancreatic carcinoma (IC50 = 27 nM) cells. Epacadostat increases the number and activity of tumor-infiltrating lymphocytes as well as increasing the ratio of effector T cells to regulatory T cells1,2. Because of these immune system enhancing properties3, it is being investigated as a synergistic agent for use with other immuno-oncology agents such as anti-PD-1 and anti-CTL4 antibodies4,5.

Supplier: G-Biosciences

Pexidartinib (1029044-16-3) is a potent and selective dual inhibitor of CSF1R (IC50 = 20 nM) and c-KIT (IC50 = 10 nM).1 Inhibition of CSF1R with Pexidartinib resulted in a reprogrammed immune microenviro nMent that fosters antitumor immunity in a CD8+ T-cell-dependent manner in a breast cancer model.1 CSF1R recruits tumor-infiltrating myeloid cell that suppress tumor immunity – Pexidartinib increased the efficacy of adoptive cell immunotherapy (ACT) in a mouse melanoma model by inhibiting the intratumoral accumulation of immunosuppressive macrophages.2,3 It has also been shown to increase the efficacy of anti-PD-14,5 and DC immunotherapy 6.

Supplier: Promocell, Inc.

PromoCell Mononuclear Cells (MNC) represent the lymphocyte and monocyte fraction isolated from umbilical cord blood or peripheral blood. They are prepared by optimized low-density gradient centrifugation, which effectively reduces the granulocyte content. Red blood cells are gently but thoroughly depleted by proprietary techniques instead of osmotic lysis. This results in ultra-pure mononuclear cells with superior viability and unchanged biological function. In addition, the cells do not clump after thawing, allowing for easy handling and reproducible results.

Supplier: G-Biosciences

A mycophenolic acid prodrug. Immunosuppressive agent useful in prevention of organ allograft rejection.1 Is metabolized to mycophenolic acid in vivowhich acts by inhibiting the biosynthesis of guanine nucleotides via inhibition of inosine 5’-monophosphate dehydrogenase, suppressing the production of proinflammatory cytokines, nitric oxide and LDH in macrophages.2,3 IL-2-dependent T cell proliferation is also inhibited.4 Inhibits microglial and astrocytic activation reducing cell death after neuronal injury.5 Active in vivo.

Supplier: G-Biosciences

URMC-099 is a potent (IC50=14 nM), brain penetrant mixed-lineage kinase 3 inhibitor (MLK3). It also potently inhibits FLT3 (4 nM in vitro, but 560 nM in vivo), LRRK2 (11 nM), and ABL1 (3 nM)1. URMC-099 displayed neuroprotective effects in HIV-associated neurocognitive disorders2 and facilitated microglial amyloid-β degradation and clearance in mouse models3,4. URMC-099 increased CD8+ T cells in mice and increased the CD8+GZMB+ T cell population in blood mononuclear cells isolated from breast cancer patients.

Supplier: G-Biosciences

Potent (IC50 ~ 1 nM) and specific inhibitor of T cell antigen receptor (TCR)-dependent T cell activation. Does not inhibit B cell proliferation triggered by B cell antigen receptor (BCR), TLR4, CD40 agonists nor IL-2-dependent proliferation of T lymphoblasts. Binds to the SH3.1 domain of the adaptor protein Nck blocking its interaction with the CD3ε subunit on the T cell antigen receptor. AX-024 displays protective effects in mouse models of psoriasis, allergic asthma, and multiple sclerosis. In contrast to fingolimod, the therapeutic effect of AX-024 persisted after removal of the drug, suggesting a persistent modification of autoimmune T cells. Currently in clinical trials.

Supplier: Rockland Immunochemical

Rat Neuropilin-1 AccuSignal ELISA Kit

Supplier: G-Biosciences

A clinically useful anticancer agent1. It exerts its cytotoxic effects via the metabolites gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP). dFdCTP is an inhibitor of DNA polymerase and is incorporated into DNA resulting in termination of chain elongation and apoptosis. dFdCDP is an inhibitor of ribonucleotide reductase which results in depletion of deoxyribonucleotides needed for DNA synthesis. The phosphates have also been reported to inhibit cytidine triphosphate synthetase (CTP synthetase)2 and deoxycytidylate deaminase (dCMP deaminase)3. Topoisomerase 1 has also been shown to be a target for gemcitabine4.

Supplier: G-Biosciences

Potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced tumor regression in 17 of 26 KRASG12C-positive cell lines and xenograft models from multiple tumor types.2 MTRTX849 reversed the immunosuppressive tumor enviro nMent in a genetically modified mouse model and sensitized tumors to checkpoint inhibitor therapy in a genetically modified mouse KRASG12C lung adenocarcinoma model.3 It reversed ABCB1-mediated multidrug resistance in vitroand in vivovia attenuating ABCB1 efflux in drug-resistant cancer cells.

Supplier: G-Biosciences

Potent inhibitor (IC50=2 nM) of the facilitative glucose transporter GLUT1, an enzyme frequently overexpressed in many cancers.1 It shows greater than 100-fold selectivity over GLUT2-4. BAY-876 displayed potent antitumor activity in ovarian cancer xenograft models2 and in triple negative breast cancer cells displaying high glycolytic and low oxidative phosphorylation rates3. It reduced CD4+ T cell proliferation and IFN-γ secretion via GLUT1 inhibition suggesting utility against auto-inflammatory diseases.4 BAY-876 induces disulfidptosis in SLCA11high cancer cells.

Supplier: G-Biosciences

Inhibitor of cyclic GMP-AMP synthase (cGAS), an important innate immune system sensor of foreign cytoplasmic double-stranded DNA.1,2 IC50 = 0.70 µM in dsDNA-stimulated RAW macrophages1 and ~0.80 µM in wild type human THP-1 cells2. It is selective for cGAS with no targeting of IFNB1 protein, interferon receptors, or downstream signaling components of the JAK/STAT pathway. RU.521 was able to significantly increase cardiac output in a mouse model of sepsis.3 Active in both mouse and human cell lines.

Supplier: G-Biosciences

A Toll-like receptor 7/8 agonist.1 May be used as an immune adjuvant in cancer vaccines.2 Resiquimod-carrying synthetic vaccine particles augment the immune response to encapsulated antigen and exhibit strong local immune activation without inducing systemic cytokine release.3 Topical treatment of wild-type mice induces systemic autoimmune disease which may be used as a model of systemic Lupus erythematosus.4 Effect on stem cells depends on cell type5,6.

Supplier: G-Biosciences

A potent immunoregulator that suppresses IgE production.1 Suppresses innate immunity by down-regulating TLR2, TLR4 and CD14 gene expression on splenocytes stimulated with LPS and TLR2/TLR4 agonists.2 Prevents bleomycin-induced pulmonary fibrosis in mouse models.3 Potent inhibitor of Th2 cells in vivo and together with a Treg cell inhibitor promotes BCG vaccine efficacy against tuberculosis.4 Antiasthmatic agent effective for antileukotriene nonresponders.5 Orally active.

Supplier: G-Biosciences

A lysosomotropic agent which inhibits autophagy and triggers apoptosis in a variety of cell types1,2. Augments the anticancer activity of DNA-damaging chemotherapy3. Antiinflammatory activity. Decreases cell surface expression of TNFα receptors in U937 cells4. Has been used to treat alopecia successfully5. Clinically useful antimalaria agent. Cell permeable and active in vivo.

Supplier: G-Biosciences

Novel Class I phosphatidylinositol 3-kinase (PI3K) inhibitor. ZSTK474 is an ATP-competitive inhibitor of all four Class I PI3K isoforms. However, it inhibits PI3Kδ most potently, with a Ki of 1.8 nM, while inhibiting the α, β and γ isoforms at slightly higher concentrations (6.7 nM, 10.4 nM and 11.7 nM, respectively)1. Displays potent antitumor activity against human cancer xenografts (A549, PC-3 and WiDr) when administered to mice2. It displays potent anti-inflammatory activity via modulation of human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis3. Ameliorates the progression of adjuvant-induced arthritis in a rat model.

Supplier: G-Biosciences

Potent and selective prolyl-tRNA synthetase (PRS) inhibitor (Ki=18.3 nM) derived from febrifugine1. Also attenuates TGF-β signaling, including reversibly reducing Smad3 protein levels and inhibiting fibroblast differentiation2. Blocks fibrosis, angiogenesis, and tumor progression2,3. Inhibition of PRS results in amino acid starvation which activates the integrated stress response (ISR) and mTOR signaling4 and thus preventing differentiation of TH17 cells, suppressing the autoimmune response5. Reduces TMPRSS2 protein levels via enhanced ubiquitination and proteasomal degradation, limiting SARS-CoV-2 cellular entry.

Supplier: G-Biosciences

Immunomodulator. Inhibits secretion of IL-1β, TNF-α, and IL-10 from murine macrophages stimulated with LPS and spares T cell function.1 Ameliorates the course of acute and chronic immunoinflammatory conditions such as carrageenan-induced pleurisy, LPS-induced lethality and type II collagen-induced arthritis in mouse models.1 Prevents spontaneous and accelerated forms of autoimmune diabetes in a NOD mouse model.2 Moldulates genes involved in LPS-induced Toll-like receptor 4 activation in a mouse Lupus model.3 Displays protective effects in particulate matter-induced acute lung injury by blocking TLR4 signaling.

Supplier: G-Biosciences

Inhibits Wee1 tyrosine kinase (IC50=5.2 nM) thus preventing phosphorylation of CDC2 and abrogating the G2 DNA damage checkpoint, sensitizing a variety of tumor cells to DNA damaging agents1. Adavosertib also blocks Wee1 phosphorylation of E3 ubiquitin ligase SKP2 in human cells, ultimately preventing degradation of CDKs and further allowing cell cycle progression2. Stimulates anti-tumor immunity and enhances sensitivity to immune checkpoint blockade by activating ERV and the dsRNA pathway3. Potentiates sensitivity of tumors to PARP inhibitors.

Supplier: G-Biosciences

Highly potent pan-Bcr-Abl and multikinase inhibitor, suppressing the activity of native Bcr-Abl (IC50=0.37 nM) as well as the mutants T315I (IC50=2 nM), Q252H (IC50=0.44 nM), Y253F (IC50=0.3 nM), M351T (IC50=0.3 nM) and H396P (IC50=0.34 nM).1 Also inhibits PDGFRα, c-Src and c-Kit (IC50=1.1, 5.4 and 12.5 nM respectively)2 as well as FGFR-mediated signaling (IC50<40 nM)3. Protects against influenza A virus-induced death by suppressing cytokine storm in mouse models.

Supplier: G-Biosciences

Potent and selective inhibitor of the transforming growth factor beta 1 receptor, activin receptor-like kinase (ALK5), IC50 = 14.3 nM and ALK4 (IC50 = 58.5 nM) with no activity at ALK2, 3 and 61. Blocks fibrosis markers and renal injury in the puromycin-induced nephritis model1. It causes significant attenuation in Smad2/3 nuclear translocation, decrease in CTGF-expressing cells, myofibroblast proliferation and type 1 collagen deposition resulting in an overall attenuation in bleomycin-induced pulmonary fibrosis2. Sensitizes drug-resistant pancreatic cancer cells to gemcitabine3. Cell permeable and active in vivo.

Supplier: Stemcell Technologies

EasySep™ Buffer is recommended for EasySep™ cell separation protocols.

Supplier: Thermo Scientific Chemicals

A heterobifunctional coupling reagent useful for forming enzyme immunoconjugates