2209 Results for: "Immunology"

Baricitinib, approved by the FDA for two inflammatory disorders, rheumatoid arthritis and alopecia areata, selectively inhibits Janus kinase 1 (IC50 = 5.9 nM) and 2 (5.7 nM), over 3 (0.56 µM)1. It thereby blocks JAK/STAT signaling, reducing cytokine release and suppressing the innate and adaptive immune systems1,2. Was recently shown to significantly improve COVID-19 symptoms in a preliminary human trial, presumably through suppression of the cytokine release syndrome (“cytokine storm”) induced by SARS-CoV-2 infection3.

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Defactinib >98% Potent FAK inhibitor

Supplier: G-Biosciences

Defactinib (1073154-85-4) is a potent inhibitor of FAK (IC50=0.6 nM) and Pyk2 (IC50=0.6 nM).1 It is active in vivo (EC50=26 nM). FAK inhibition prevents tumor invasion and dissemination rather than tumor size reduction. Defactinib has been shown to preferentially target cancer stem cells in a mouse xenograft model of triple negative breast cancer.2 It is in multiple clinical trials for various cancers3 and in shows synergistic activity when used in combination with checkpoint immunotherapy.

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Boceprevir >98% Antiviral; SARS-CoV-2 Mpro inhibitor

Supplier: G-Biosciences

Boceprevir directly inhibits Hepatitis C virus (HCV) NS3 protease (overall binding constant for formation of covalent adduct, Ki*=14 nM; initial inhibition constant Ki=7.8 µM). This blocks NS3 autoactivation, and subsequent cleavage and maturation of other viral proteins necessary for replisome assembly. This reversible, slow-binding ketoamide also restores host interferon signaling obstructed by HCV, thus reactivating the immune response1. Recently, it was also found to inhibit the key SARS-CoV-2 protease, Mpro (3CLpro) in vitro (Ki=1.18 µM) and in cells (EC50=1.9 µM, virus-induced cytopathic effects (CPE).

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Piperine >98% Up-regulator of skeletal muscle metabolism

Supplier: G-Biosciences

Component of black pepper that activates TRPV1 (EC50=38 µM), inhibits MAO-A/B (Ki=19.0/3.19 μM), and stimulates chloride currents through GABAA receptors (EC50=52.4 μM)1-3. At 20 mg/kg, piperine significantly lowers blood glucose in alloxan-induced diabetic mice4. Also modulates cytochrome P450 family members, inhibiting MDR1, CYP3A4, CYP2E1, CYP2C9 while also increasing their expression4-6. Exhibits anti-inflammatory and anti-cancer effects5. Increases the metabolic rate of resting muscle (fast twitch skeletal fibers) without affecting slow twitch or cardiac fibers via destabilization of the super-relaxed state of myosin heads.

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BI-D1870 >98% p90 Ribosomal S6 kinase inhibitor

Supplier: G-Biosciences

BI-D1870 is an inhibitor of p90 ribosomal S6 kinase (RSK; IC50’s=RSK1, 31 nM; RSK2, 24 nM; RSK3, 18 nM; RSK4, 15 nM) with selectivity over other AGC kinases.1 It protected mice from experimental autoimmune encephalomyelitis suggesting a new strategy to treat multiple sclerosis.2 BI-D1870 has also been found to alter mTORC1 signaling in an RSK-independent manner.3 BI-D1870 induced apoptosis in oral squamous cell carcinoma cells4, suppressed growth and induced apoptosis in pediatric medulloblastoma cell lines as well as sensitizing these lines to Sonic hedgehog agents5, and blocked cell proliferation and protein synthesis in dual BRAF and MEK inhibitor-resistant melanoma.

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Polyethylene Transfer Pipettes

Supplier: VWR International

Disposable transfer pipettes for liquid handling.

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Fludarabine >98% DNA synthesis inhibitor

Supplier: G-Biosciences

A synthetic adenosine analog that inhibits DNA biosynthesis and is a clinically useful antineoplastic agent1. In cells fludarabine accumulates as its 5’-triphosphate (F-ara-ATP) for which the rate-limiting step in formation is the conversion of fludarabine to its monophosphate2. F-ara-ATP has multiple mechanisms of action including inhibition of ribonucleotide reductase, DNA polymerase, ligase and primase2. A frequently used agent in myeloablative conditioning regimens for allogeneic hematopoietic cell transplantation3. Immunosuppressive effects are mediated via inhibition of TNFα-stimulated production of IL-2 and IFN-γ through inactivation of NFκB4. Antagonist at adenosine A1 receptors.

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Dp44mT >98% Metal chelator

Supplier: G-Biosciences

A metal chelator with potent antitumor activity.1,2 Displays an average IC50 of 30 nM over 28 cancer cell lines (IC50 range 5 nM to 400 nM).2 Dp44mT retained its antiproliferative activity in both etoposide-resistant MCF-7/VP clones (MCF-7 breast cancer cells) and vinblastine-resistant KB-VB1 clones (KB3-1 epidermoid carcinoma cells) with an IC50 = 12 nM for both lines.2 The potency of Dp44mT has been attributed to the high redox activity of the Dp44mT-Fe complex leading to cytotoxic ROS generation. The antitumor activity of Dp44mT may also be mediated by a redox active copper complex that causes cellular glutathione depletion and lysosomal damage.3,4 It also inhibits T-cell activation and prevented CD25 up-regulation via a copper-dependent mechanism.

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Human Recombinant LEP

Supplier: Rockland Immunochemical

Leptin Human Recombinant control protein

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Pigeon Serum Sterile, Rockland Immunochemicals

Supplier: Rockland Immunochemical

Sterile Serum

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Human Recombinant IL3

Supplier: Rockland Immunochemical

IL-3 Recombinant Human control protein

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Mouse Recombinant CCL2

Supplier: Rockland Immunochemical

Recombinant Mouse CCL2 control protein

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hOVA antibody development

Supplier: AAT Bioquest

hOVA is the ovalbumin (OVA) modified with hexamethylenediamine to make the proteins bear more amine groups (thus more positive charges at neutral pH).

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Anti-CA1 Goat Polyclonal Antibody

Supplier: Genetex

Goat polyclonal to Carbonic Anhydrase I

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Luminol and oxidizing solutions (each bottle)

Supplier: Thermo Scientific Chemicals

For chemiluminecent detection of HRP-based Western blotting systems.

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AMG 510 >98% Covalent KRASG12C Inhibitor

Supplier: G-Biosciences

AMG 510 is a potent (IC50’s=6 nM NCI-H358; 9 nM MIA PaCa-2) covalent KRASG12C inhibitor.1,2 It significantly inhibited tumor growth in NCI-H358 and MIA PaCa-2 cell lines as well as CT-26 tumors (mouse syngeneic model) and caused tumor regression at higher doses.1 AMG 510 improved the efficacy of various other chemotherapeutic agents including inhibitors of HER kinases, EGFR, SHP2, PI3K, AKT, and MEK 1,3 and synergized with immune checkpoint reagents1. FDA approved for use in KRASG12C-positive non-small cell lung cancer. AMG 510 displayed efficacy alone4,5 and in combination5 with trametinib and/or buparlisib in pancreatic ductal adenocarcinoma cell lines.