Supplier: G-Biosciences

Inhibitor of the JAK2/STAT3 pathway as well as STAT5 and AKT1-3. It downregulated Bcl-XL, Mcl-1, and c-myc while activating Bax and inducing apoptosis1. Active against human malignant glioma U87-MG (IC50=5.6µM) and U373-MG (IC50=3.7 µM) cells. Enhances T-cell cytotoxicity via inhibition of regulatory T-cells4,5. WP1066 abrogated PD-L1 expression in lymphoma cell lines.

Supplier: G-Biosciences

A potent and selective inhibitor of tryptophan 2,3-dioxygenase (TDO) Ki=42 nM)1,2. Displays no activity against indoleamine 2,3-dioxygenase, MAO-A and B and does not effect serotonin uptake. Elevates CSF tryptophan by up to 260% and CSF serotonin by 170% of basal2. TDO inhibition by 680C91 in glioma cells blocked the release of kynurenine, an endogenous tumor promoting AHR ligand.

Supplier: G-Biosciences

Selective activator of protein kinase C which displays antileukemic activity mediated via PKCδ. In contrast, it provides a strong survival signal to resting and activated human T cells via activation of PKC and downstream activation of NFκB. Treatment of subcutaneous tumors results in anti-cancer CD8 T cells, also displays adjuvant activity and synergizes with cancer immunotherapies. Induces senescence-like growth arrest in solid tumor cells. Inhibits HIV-1 infection at an early pathway of viral entry.

Supplier: G-Biosciences

Thymidine derivative that acts as an HIV nucleoside reverse transcriptase inhibitor (NRTI) (EC50=8.8 nM for HIV-1 replication in human PBMCs)1,2. Down-modulates P2X7-mediated NLRP3 inflammasome activation independent of reverse transcriptase inhibition3. Reduces production of IL-18 and caspase-1 and stimulates Aβ-induced autophagy in macrophages.

Supplier: G-Biosciences

Potent and selective ALK4, ALK5 and ALK7 inhibitor (TGFβ superfamily Type I activin receptor-like kinase). (ALK5 IC50=94 nM)1,2. Inhibits TGFβ-induced proliferation of human osteosarcoma cells3. Ehances growth and integrity of embryonic stem cell-derived endothelial cells4. A frequently used agent employed in numerous stem cell differentiation protocols5. Cell permeable.

Supplier: QUALITY BIOLOGICAL, INC.

PBS (phosphate buffered saline) is a balanced salt solution used for a variety biological and cell culture applications.

Supplier: BioVendor

96 wells (1 kit) - ELISA is a sandwich enzyme immunoassay for the quantitative measurement of Ghrelin Acylated.

Supplier: G-Biosciences

Potent inhibitor (IC50 = 21 nM) of HSP90.1 It is active against various human tumor xenograft models acting via several processes including cytostasis, apoptosis, invasion, and angiogenesis.2,3 Luminespib enhances tumor susceptibility to T-cell-based immunotherapy by re-invigorating the cancer-immunity cycle in NANOG+ cancer cells.4 It also acts as a radiosensitizer against various tumor cells.

Supplier: G-Biosciences

PF-4136309 (1341224-83-6) is a potent (hIC50 = 5.2 nM, mIC50 = 13 nM, rIC50 = 17 nM) and selective inhibitor of CCR2.1 PF-4136309 significantly decreased inflammatory monocytes in a mouse model of pancreatic cancer.2 In combination therapy with the FOLFIRINOX regimen, PF-4136309 reversed immune suppression in the tumor microenviro nMent causing an influx of tumor infiltrating lymphocytes leading to overall enhanced efficacy in a phase 1b study.

Supplier: G-Biosciences

Potent estrogen ERβ receptor agonist. Displays a 70-fold selectivity over ERα, EC50 = 0.85 and 66 nM, respectively.1 Regulates expression of GluR1, 2 and 3 in rat hippocampus.2 Ameliorates portal hypertension in a carbon tetrachloride-induced liver cirrhosis rat model.3 Stimulates proliferation of androgen-independent prostate cancer cell line PC-3 via a novel pathway involving ERβ-mediated activation of β-catenin.4 A useful tool for elucidating the biological function of ERβ.

Supplier: G-Biosciences

Sphingosine-1-phosphate transporter (Spns2) inhibitor. It inhibited sphingosine-1-phosphate (S1P) release in HeLa cells: IC50 = 1.93 µM. SLF1081851 is active in vivoand decreased lymphocyte counts and plasma S1P levels in mice and rats. Spns2 inhibitors represent potential alternative immunomodulatory agents to S1P receptor agonists as they are able in induce lymphopenia without drastic changes to systemic S1P levels or stimulating the S1P1-5 signaling pathway.

Supplier: G-Biosciences

Preladenant is a potent (Ki=1.1 nM) and selective (>1000-fold over other adenosine receptors) adenosine A2A antagonist.1 It has shown efficacy in rodent and primate models of Parkinsons disease without inducing dyskinesias and displays antidepressant effects.1-3 It has been shown that activation of the adenosine A2A receptor blocks the activation of immune cells and increases the number of regulatory T-cells.4-6 Currently in clinical trials as combination therapy with pembrolizumab.

Supplier: G-Biosciences

A synthetic folic acid analog with immunosuppressant and cancer chemotherapeutic activity. Inhibits thymidylate synthetase and de novo purine synthesis. Displays beneficial effects in rheumatoid arthritis by inhibiting the production of cytokines induced by T-cell activation and stimulation of adenosine release. It is the classic disease-modifying antirheumatic drug (DMARD).

Supplier: G-Biosciences

Clinically useful antidepressant that inhibits monoamine transporters DAT, NET, and SERT (Kis for dopamine uptake = 2.8, 1.4, 45 µM)1. Also acts as a noncompetitive antagonist at nicotinic acetylcholine receptors (AChRs)2. At higher concentrations (50 µM), stimulates pro-inflammatory cytokines and TLR2/TLR4 and JAK2/STAT3 in human peripheral blood mononuclear cells (PBMCs)3.

Supplier: G-Biosciences

A potent and selective inhibitor of p38 MAP kinase, IC50=50 and 500 nM for p38 and p38β2 respectively. No other kinases (in a panel of 30) were significantly inhibited including p38γ and δ at 10 μM2. A potent inhibitor of inflammatory cytokine production (IC50=15-25 mg/kg in mice and rats) in animal models of arthritis, bone resorption, endotoxin shock and immune function3.

Supplier: G-Biosciences

Displays antiapoptotic, anti-inflammatory1 activity. Prevents neuropathic pain in a rat sciatic nerve injury model1. Reduces MMP-9 activity2. Attenuates disease severity in mouse models of multiple sclerosis3. Displays neuroprotective activity4. May be effective in methotrexate-induced lung fibrosis5. Orally active and brain penetrant.

Supplier: G-Biosciences

Thalidomide analog. Inhibits cereblon (CRBN) an E3 ubiquitin ligase, IC50 ~3 µM for CRBN-DDB1 complex.1 Displays antiangiogenic and immunomodulatory activity in vivo potently inhibiting the production of TNFα and IL-2.2 Promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome.3 Conjugation with other ligands is a strategy to target proteins for in vivo proteasomal degradation via PROTACS.

Supplier: G-Biosciences

Potent and selective allosteric inhibitor (IC50 = 23.4 nM) of the EED subunit of the methyltransferase polycomb repressive complex 2 (PRC2).1,2 Strongly inhibits proliferation of lymphoma cells with EZH2 mutations and causes shrinkage and slower tumor growth in mice in a subcutaneous xenograft model of Karpas422.

Supplier: Rockland Immunochemical

Protein A Biotin Conjugated

Supplier: G-Biosciences

After incorporation into DNA, it disrupts cytosine methylation by DNA methyltransferases in vitroand acts as a DNA demethylating agent in vivo. It reactivates epigenetically silenced genes in acute lymphoblastic leukemia cells by facilitating proteasome-mediated degradation of DNA methyltransferase (D nMT1). Incorporates into DNA and induces double strand breaks which destabilize DNA structure resulting in cytotoxicity. Selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance in a xenograft model. Anticancer and immunosuppressive activity.

Supplier: G-Biosciences

Oxaprozin is a clinically useful non-steroidal anti-inflammatory drug.1 In addition to typical NSAID COX inhibition, Oxaprozin may also exert anti-inflammatory effects via inhibition of the Akt/IKK/NF-kappaβ pathway.2 The compound is capable of inhibiting both anandamide hydrolase in neurons (IC50= 85 µmol/l), with consequent potent analgesic activity, and NF-kappaB activation in inflammatory cells (IC50 = 50 µmol/L).

Supplier: G-Biosciences

Selective inhibitor of IκB kinase 2 (IKK2) (IC50 = 17.9 nM).1 Inhibits production of pro-inflammatory cytokines in arthritis and other animal models of inflammation.1,2 Also attenuates NLRP3 inflammasome activation in THP-1 myeloid cells, and suppresses IL1β-induced proliferation, migration, and invasion of HeLa cells.3,4 Continuous exposure to TPCA-1 promotes expansion of hematopoietic stem/progenitor cells (HSPCs) via improved glycolysis and limited ROS production.

Supplier: G-Biosciences

Potent and highly selective inhibitor of receptor interacting protein 3 (RIP3) (IC50=1.3 nM)1. Blocks necroptosis, as well as necrosis induced by virus or TLR31,2. At higher concentrations (~3 µM), GSK872 induces Caspase-8-mediated apoptosis independent of RIP3 inhibition2. Reduces HIF-1α and NLRP3 inflammasome, and ameliorates brain injury and inflammation in mouse models of ischemic brain injury and acute respiratory distress.

Supplier: G-Biosciences

Natural product derived from sesame seeds with anticancer1, antioxidant2, anti-inflammatory/immunomodulatory3, and antidiabetic4,5 effects. It also displayed effects on cholesterol and fatty acid metabolism.6 Sesamin was recently found to inhibit bacterial L-tryptophan indole lyase (Ki = 7 µM).7 This enzyme reacts with dietary tryptophan to produce the uremic toxin indoxyl sulfate which exacerbates chronic kidney disease.

Supplier: G-Biosciences

Potent inhibitor of NFκB in T-lymphocytes with almost complete inhibition at 200 nM1. Completely inhibits IL-4 and IFN-γ production and suppresses IL-2 and TNF-α production at 50 nM in T-cells, without inhibiting AP-1 and NF-κB2. Immunosuppresive activity is due to inhibition of cytokine gene expression via blocking NF-AT activity. Has anti-cancer properties via various pathways including ERK inhibition3, ATM/ATR-Chk1/Chk2 activation4, and p38 and JNK activation5.

Supplier: G-Biosciences

GSK583 (1346547-00-9) is a highly selective and potent inhibitor of RIP2 kinase, IC50=5 nM human and IC50=2 nM rat.1 It also potently inhibits isolated RIP3 kinase (IC50=5 nM) but is inactive against RIP3 in cellular assays due to a very low KM,ATP. GSK583 blocks NOD2 signaling by interfering with XIAP-RIP2 binding resulting in decreased cytokine and chemokine production.

Supplier: G-Biosciences

Major bioactive component of the medicinal plant Andrographis paniculate. Demonstrates anti-inflammatory anti-apoptotic, anti-viral and anti-proliferative effects in vitro and in vivo. Prevents hyperglycemia in rat diabetes model. Irreversible antagonist of NK-κB and AP-1 (IC50=15 µM).

Supplier: G-Biosciences

R428 (1037624-75-1) is a potent and selective inhibitor of AXL kinase (IC50 = 1.4 nM).1 R428 has been shown to overcome chemotherapy resistance to various agents in multiple cancer models.2-5 AXL has been shown to suppress myeloid cell activation and function – combined AXL inhibition with R428 and PD-1 blockade showed potent synergistic antitumor effects.

Supplier: G-Biosciences

Potent and selective inhibitor of Cdk4, IC50 = 11 nM and Cdk6, IC50 = 16 nM.1 Inhibits phosphorylation of Rb protein and cell cycle progression through G1 in primary 5T33MM cells and sensitized these cells to killing by a proteasome inhibitor (bortezomib) in mouse models.2 Induces autophagy and senescence in AGS gastric cancer cells.3 Clinically useful breast cancer agent.4 Cell cycle inhibitors boost tumor immunogenicity.

Supplier: G-Biosciences

CRAC (calcium release-activated calcium) channel blocker1, a prototypic store-operated calcium channel2. Inhibits antigen-induced histamine release via modulation of mast cell responses3. Displays potent analgesic actions in various pain models in mice and is orally active4. Inhibits T cell-mediated immune responses in vivo5.