2209 Results for: "Immunology"
Red Blood Cell Depletion Magnetic Beads, Rockland Immunochemicals
Supplier: Rockland Immunochemical
Red Blood Cell Depletion Magnetic Beads
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PF-06840003 >98% IDO1 inhibitor
Supplier: G-Biosciences
PF-06840003 (198474-05-4) is a potent (IC50=150 and 410 nM via two methods) and selective inhibitor of Indoleamine-2,3-dioxygenase (IDO1).1 In mice with syngeneic tumor grafts, it reduced intratumoral kynurenine levels by over 80%, inhibited tumor growth as monotherapy, and increased the efficacy of anti-PD-L1 therapy.2 PF-06840003 treatment combined with GM-CSF-secreting allogenic pancreatic tumor cell vaccine (GVAX) resulted in increased antitumor efficacy in a murine model of pancreatic ductal adenocarcinoma.
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CPI-455 >98% Lysine demethylase KDM5 inhibitor
Supplier: G-Biosciences
CPI-455 (1628208-23-0) is a potent (IC50 = 10 nM) and selective inhibitor of the lysine demethylase KDM5 (equal inhibition of KDM5A, 5B, 5C).1 CPI-455 reduced the number of drug-tolerant persister cancer cells (DTPs) in a dose-dependent, KDM5-dependent manner in multiple cell lines treated with standard chemotherapy or targeted agents. CPI-455 synergized with 5-aza-2’-deoxycytidine (DAC) to reduce the viability of luminal breast cancer cells in vitro.2 KDM5 demethylases have recently been shown to repress the immune response to tumors via suppression of STING.
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CID1067700 >98% Rab7 GTPase inhibitor
Supplier: G-Biosciences
A specific competitive inhibitor of nucleotide binding to Rab7, an endosome-localized small GTPase1. It interferes with the Rab7-RILP interaction, locking the GTPase in an inactive conformation2. Impairs B cell class switching and plasma cell survival dampening, the pathogenic autoantibody response in lupus3. Inhibits the Arf-like small GTPase Arl8b, blocking cellular egress of β-coronaviruses (SARS-CoV-2) which utilize a lysosomal exocytosis pathway4.
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Belumosudil >98% ROCK2 inhibitor
Supplier: G-Biosciences
Selective inhibitor of Rho kinase 2 (ROCK2) – IC50’s: ROCK2=105 nM, ROCK1=24 µM in enzyme assays.1 It downregulated the ability of T cells to secrete IL-21 and IL-17, but not IFN-γ, in response to T cell stimulation in vitro via a STAT3-dependent mechanism.2 Belumosudil ameliorated graft-versus-host disease in multiple models3,4 and was recently approved by the FDA for the treatment of GVHD (July 2021). It has also been shown to suppress adipogenesis.5-7 Suppression of adipocyte differentiation is mediated via casein kinase 2 inhibition (IC50=50 nM) and not ROCK2 inhibition.
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I-BET762 >98% BET Bromodomain inhibitor; Suppresses Myc transcription
Supplier: G-Biosciences
I-BET762 is a potent inhibitor of the BET family of bromodomains with no activity at bromodomains BAZ2B, SP140, ATAD2, CREBBO, and PCAF.1,2 IC50’s for H4Ac peptide displacement: BRD2 = 32.5 nM, BRD3 = 42.4 nM, BRD4 = 36.1 nM.1 It was able to suppress proinflammatory proteins by macrophage, block acute inflammation in mice1, and suppressed the inflammatory function of T cells3. Inhibition of BET bromodomains results in downregulation of Myc transcription, an important oncogene.
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Triacetylresveratrol >98% SIRT activator, prodrug
Supplier: G-Biosciences
A resveratrol prodrug. One method for increasing the half-life of resveratrol in vivois acetylation of the phenolic OH groups. Deacetylation takes place in vivoor in intact cells via the action of intracellular esterases releasing active resveratrol. CWR22Rv1 cells when exposed to triacetyl resveratrol showed a G1S block concomitant with increased p53 and p21 expression1. In MCF-7 cells it induced both ERK and p38 phosphorylation2.
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Artesunate >98% Cancer stem cell inhibitor
Supplier: G-Biosciences
A semisynthetic derivative of the natural product artemisinin which is clinically useful for treatment of malaria and other parasitic diseases. Depolarizes mitochondrial the membrane via generation of reactive oxygen species which disrupt the electron transport chain.1 Generation of mitochondrial ROS is dependent on RIP1.2 Inhibits TNFα-induced production of proinflammatory cytokines in human RA fibroblast-like synoviocytes.3 Displays cytotoxicity against a variety of cancer cells4 and cancer stem cells.
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CH-223191 >98% Arylhydrocarbon receptor antagonist
Supplier: G-Biosciences
Arylhydrocarbon (AhR) receptor antagonist, IC50=30 nM.1 Blocks endogenous AhR agonist-induced differentiation of Th17 cells.2 Promotes expansion of human hematopoietic stem cells.3 Mitigates cytokine-mediated inflammatory signaling in human fibroblast-like synoviocytes.4 An important tool for probing the involvement of AhR in the toxicity of various enviro nMental toxins such as TCDD and other dioxins.
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a-Mangostin >98% STING agonist (human)
Supplier: G-Biosciences
α-Mangostin is a xanthone natural product that has historically been used in traditional folk medicine.1 It is a potent agonist of human STING (Stimulator of Interferon Genes) and also weakly activates mouse STING.2 Induces IFN-β production and repolarizes human monocyte-derived M2 macrophages to M1. Improves insulin secretion and protects INS-1 cells from streptozotocin-induced damage.3 Suppresses the metastasis of human renal carcinoma cells.4 Synergizes with kinase inhibitors in suppression of proliferation of SK-MEL-2 malignant melanoma cells.
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Apilimod >99% IL12/23 inhibitor/Inhibits SARS-CoV2 infection
Supplier: G-Biosciences
Potent and selective inhibitor of the TLR signaling lipid kinase PIKfyve (IC50=14 nM), but not other lipid or protein kinases1. Blocks transcription of IL-12 p35 and IL-12/IL-23 p40 genes via transcriptional repressor ATF32, leading to suppression of Th1, but not Th2, immune response3. Cytotoxic against B-cell non-Hodgkin lymphoma in vivo4, and reduces PtdIns5P and PtdIns(3,5)P2 levels in transformed and immortalized cell lines5. Blocks SARS-CoV-2 infection in vitro, likely via reduction in cathepsin protease activation.
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Parthenolide >97% IκB Kinase inhibitor
Supplier: G-Biosciences
Parthenolide is a natural product that inhibits NF-κB signaling via two mechanisms: direct inhibition of IκB kinase, and prevention of NOD2 dimerization1,2. It inhibited expression of COX-2 and proinflammatory cytokines TNF alpha and IL-1 in lipopolysaccharide (LPS)-stimulated macrophages3. Parthenolide demonstrates antisecretory4 and spasmolytic5 activities in vivo. It also causes proteasomal degradation of HDAC1 (but not other class I/II HDACs), and cell death through the ATM pathway6.
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Grapiprant >98% EP4 receptor antagonist.
Supplier: G-Biosciences
Grapiprant (415903-37-6) is a potent (Ki=13 nM for human and 20 nM for rat) and selective prostaglandin EP4 receptor antagonist.1 It produces antihyperalgesic effects in animal models of pain, and has significant anti-inflammatory effects in a rat model of adjuvant-induced arthritis.2 EP4 receptors have been shown to be involved in PGE2 stimulation of Th1 differentiation and Th17 expansion revealing a potential role for PGE2 receptors in immunosuppression.3,4 Grapiprant/Pembrolizumab combination is in clinical trials for advanced or metastatic NSCLC adenocarcinoma.
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Human Recombinant IL33
Supplier: Rockland Immunochemical
IL-33 Human Recombinant control protein
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CellPro™ X-Gal Solution
Supplier: Alkali Scientific
CellPro X-Gal solution, ready-to-use, is stable, 0.22 µm membrane filtered solution formulated for direct use in conjunction with IPTG for blue/white colony screening.
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Brequinar sodium >99% Dihydroorotate dehydrogenase inhibitor, antiviral
Supplier: G-Biosciences
Inhibitor of dihydroorotate dehydrogenase (DHODH)1,2 with IC50’s between 0.2 and 5.8 µM in various cell lines3 and 20 nM for isolated enzyme4. Reduced leukemic cell burden, decreased levels of leukemia-initiating cells, and improved survival in human and mouse models of acute myeloid leukemia.4 Displays broad antiviral activity against flaviviruses, positive-strand RNA alphaviruses, negative-strand RNA rhabdoviruses, Influenza A and B viruses, and HIV.
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Acalabrutinib >98% Highly selective BTK inhibitor
Supplier: G-Biosciences
Acalabrutinib (1420477-60-6) is a highly selective, potent (IC50=3 nM), and irreversible inhibitor of Bruton’s tyrosine kinase (BTK).1 Improved target selectivity (especially against TEC family kinases and EGFR) decreased the number of serious side effects observed with Ibrutinib.2 Acalabrutinib significantly inhibits BCR signaling, inhibits tumor proliferation, and reduces tumor burden.3 Clinically useful agent for treating B-cell cancers. BTK has also been shown to have a role in modulating the innate immune system, especially in dendritic cells and macrophages, suggesting a possible role in immunotherapy.
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SX-682 >98% CXCR1/2 inhibitor
Supplier: G-Biosciences
Novel CXCR1/2 inhibitor (IC50s: CXCR1 = 42 nM, CXCR2 = 20 nM)1. It displayed robust synergistic activity with immune checkpoint blockade against castration resistant prostate cancer.2 It significantly reduced tumor burden in a Ptenfl/fl/Lkb1fl/fl mouse model of lung squamous cell cancer when used in combination with anti-PD1 therapy.3 SX-682 significantly inhibited trafficking of neutrophilic myeloid-derived suppressor cells (PMN-MDSCs) enhancing anti-PD1 immune checkpoint blockade, T cell-based immunotherapy, and NK-cell immunotherapy.
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Metformin ∙ HCl >98% Antidiabetic agent; Life extension agent
Supplier: G-Biosciences
Clinically useful antidiabetic agent. Lowers plasma glucose levels and improves insulin sensitivity. Inhibits hepatic gluconeogenesis by activation of the AMP-activated protein kinase (AMPK) pathway.1,2 Displays antiproliferative and pro-apoptotic actions in a variety of cancer cell lines.3,4 Induces autophagy via inhibition of the mTOR pathway. Activates PGC1α and improves mitochondrial dynamics in renal tubular cells.5 Upregulates SIRT1 activity in endothelial cells.6 Neuroprotective and lowers α-synuclein phosphorylation in the Parkinson’s disease MPTP mouse model.
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Iberdomide >98% Cereblon modulator/Molecular glue
Supplier: G-Biosciences
Modulator of the cullin ring ligase 4-cereblon E3 ubiquitin ligase complex with higher affinity (IC50 = 60 nM) than lenalidomide and pomalidomide leading to more potent degradation of Ikaros (IKZF1; EC50 = 1 nM)) and Aiolos (IKZF3; EC50 = 0.5 nM).1 It is more specific for the cereblon complex and does not degrade GSPT1 of CK1α. It displays antitumor and immunostimulatory activity in lenalidomide- and pomalidomide-resistant multiple myeloma cells.2 Iberdomide has also shown efficacy in treating the autoimmune disease cutaneous lupus erythematosus (CLE).3 It was also shown to act as an HIV-1 latency reversal agent in in CD4+ T-cells.
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DMXAA >98% STING activator (mouse); Tumor vascular disrupting agent
Supplier: G-Biosciences
STING (Stimulator of Interferon Genes) agonist selective for mouse STING.1,2 Intratumoral administration of DMXAA resulted in tumor regression and complete rejection in mouse xenografts.3 Tumor regression induced by DMXAA results from a cascade of cellular events which include disruption of tumor vasculature followed by the release of chemokines which trigger the recruitment of immune cells.4 DMXAA induced expression of IFN-β resulting in a striking expansion of leukemia-specific T cells extending survival in two acute myeloid leukemia models.
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DNA Neutralization solution
Supplier: Thermo Scientific Chemicals
Applications: Western Blot and ELISA Reagents
This solution contains: 1.5M NaCl and 1M Tris, pH range 7.0-7.2.
Physical Form: Liquid
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Blocking Reagents, Denhardt's Solution (100X), Thermo Scientific
Supplier: Thermo Scientific Chemicals
Denhardt's solution is used as a blocking reagent for northern or southern blots to prevent probe binding on open membrane space and non-target nucleic acids.
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25-Hydroxycholesterol >98% Cholesterol metabolite
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.
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Anacardic Acid >98% HAT Inhibitor
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.
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Sitravatinib >98% Multikinase inhibitor/Immuno-oncology agent
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.
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Human Recombinant CCL3
Supplier: Rockland Immunochemical
MIP-1α Human Recombinant control protein
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Mouse Recombinant Ccl3
Supplier: Rockland Immunochemical
MIP-1α Mouse Recombinant control protein
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Rapamycin >98% mTOR inhibitor
Supplier: G-Biosciences
Clinically useful immunosuppressant. Inhibits the response to interleukin-2 blocking activation of T- and B-cells.1 Rapamycin forms a complex with cytosolic FK-binding protein 12 (FKB12) that binds to mTOR Complex1(mTORC1) inhibiting the mammalian target of rapamycin (mTOR).2 Also binds to mTORC2 leading to decreased glucose tolerance and insensitivity to insulin.3 Induces autophagy.