spleen

Fostamatinib (R788)(IC50 of 41 nM), which is a prodrug of the active metabolite R406, is a Syk inhibitor. It does not work on Lyn.

RO9021 is an orally bioavailable, novel ATP-competitive SYK inhibitor [average IC50: 5.6 nM].

Azobenzene is a phototrigger that can be used to design and synthesize a variety of photoresponsive systems.Azobenzene is genotoxic and induces aggressive sarcomas of the spleen and other abdominal organs.

1-Stearoyl-rac-glycerol is a monoacylglycerol that contains stearic acid at the sn-1 position. 1-Stearoyl-rac-glycerol levels are decreased in tumor tissue in a mouse model of azoxymethane-induced colorectal carcinogenesis. 1-Stearoyl-rac-glycerol has been used in the composition of transfersomes for transdermal delivery of doxorubicin in rats, leading to doxorubicin accumulation in lymph nodes, spleen, and heart.

Aniline-d5 is a deuterated isotope marker of Aniline, which can be used for isotope tracing.Aniline induces toxicity to the spleen through iron overload and oxidative stress via heme oxygenase 1 up-regulation and is able to lead to a significant increase in p-IKKα and p-IKKβ, which in turn increases NF-κB and AP-1 binding activity.

Rottlerin (NSC-56346) is a natural product purified from Mallotus Philippinensis and is a specific PKC inhibitor (IC50: PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM). Rottlerin causes apoptosis via caspase 3 activation.

Ginsenoside-F3 has immunoenhancing activity by regulating production and gene expression of type 1, type 2 cytokines in murine spleen cells. Ginsenoside-F3 enhances the NF-kappaB DNA binding activity induced by ConA in murine spleen cells (10 μM).

1. Telocinobufagin (Telobufotoxin) is the major endogenous digitalis-like factor. 2. Telocinobufagin significantly decreases the bacterial burdens in the spleen and prolongs the survival time of FIST-immunized mice challenged with live S. typhimurium. 3. Telocinobufagin has immunomodulatory activity, can enhance a Th1 immune response to control intracellular infections, could be developed as a novel immunotherapeutic agent to treat cancer and other immune-mediated diseases.

Entospletinib (GS-9973) (IC50= 7.7 nM)is a specific Syk inhibitor, which is orally bioavailable.

MNS is a tyrosine kinases inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

BAY 61-3606 dihydrochloride (BAY 61-3606) is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).

The impact of spleen tyrosine kinase (Syk) signaling might be prominent in lupus because (i) Syk is a shared downstream signaling molecule among circulating immune complex, LPS, and (1→3)-β-D-glucan (BG), and (ii) all of these factors are detectable in the serum of Fc gamma receptor IIb-deficient (FcgRIIb- -) mice with sepsis. Syk inhibition downregulated several inflammatory pathways in FcgRIIb- - macrophages activated with BG + LPS suggesting the potential anti-inflammatory impact of Syk inhibitors in lupus. Indeed, administration of a Syk inhibitor prior to cecal ligation and puncture (CLP) sepsis in FcgRIIb- - mice reduced baseline lupus-induced proinflammatory cytokines and attenuated sepsis severity as evaluated by mortality, organ injury, serum LPS, and post-sepsis serum cytokines.

Cevidoplenib dimesylate hydrochloride is a spleen tyrosine kinase (Syk) inhibitor showing potential immunomodulating and anti-inflammatory properties.

TMTD (Tetramethylthiuram disulfide) reduces the growth performance of chickens by reducing liver index, while increasing kidney, heart and spleen index. In addition, TMTD also induces tibial chondrodysplasia (TD) by regulating the expression of VEGF, HIF-1α and WNT4. As a super accelerator in rubber processing, TMTD plays an important role in the low-temperature vulcanization process and is a key pesticide in agriculture.

Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

Gusacitinib (ASN-002) (ASN-002) is spleen tyrosine kinase (SYK) and janus kinase (JAK) inhibitor (IC50: 5-46 nM).

DSPE-PEG(2000)-mannose, a pegylated and mannosylated derivative of 1,2-DSPE, has been employed in both in vitro and in vivo studies for delivering peptides, oligodeoxynucleotides, and siRNA via liposomes and lipid nanoparticles (LNPs). Fluorescently labeled LNPs containing DSPE-PEG(2000)-mannose predominantly accumulate in the liver and spleen of mice, significantly more so than in the brain, lungs, heart, kidneys, and pancreas. In immunization studies, liposomes encapsulating Human Papillomavirus type 16 (HPV16) E7 peptides with CpG oligodeoxynucleotides as an adjuvant led to reduced tumor volume and decreased numbers of CD4+ or CD8+ T cells and angiogenesis within tumors in a mouse lung cancer model using TC-1 cells.

Lipid 29 is an unsaturated, ionizable cationic lipid that facilitates the formation of lipid nanoparticles (LNP) used for intrabody mRNA delivery. When integrated into LNPs encapsulating luciferase reporter gene mRNA, intravenous injection of these LNPs induces bioluminescence in the lungs and spleen of mice.

119-23 is an ionizable cationic lipid frequently utilized in the preparation of lipid nanoparticles (LNPs) for in vivo mRNA delivery. Lipid nanoparticles that include 119-23 and encapsulate mRNA reporter molecules demonstrate a higher transfection efficiency in mouse muscle compared to LNPs containing SM-102 or DLin-MC3-DMA. Additionally, the accumulation of 119-23-containing LNPs in immune cells within the liver and spleen of mice is significantly greater than that of LNPs with SM-102. Furthermore, LNPs containing 119-23 and encoding human erythropoietin (hEPO) mRNA can elevate serum hEPO levels in mice.

6,6′-Trehalose dioleate (6,6′-TDO) is a glycolipid extensively used for in vivo and in vitro mRNA delivery. This compound effectively encapsulates mRNA encoding hemagglutinin A (HA) from influenza A virus for use within lipid nanoparticles (LNPs), enhancing the secretion of Ifn-γ, Il-2, and Tnf-α from isolated murine spleen cells. When administered via intramuscular injection in mice, LNPs containing 6,6′-TDO predominantly accumulate in the liver and spleen. Unlike LNP formulations without 6,6′-TDO, those containing 6,6′-TDO do not reduce serum levels of blood urea nitrogen (BUN) or elevate levels of lactate dehydrogenase (LDH), troponin I, alanine aminotransferase (ALT), or aspartate aminotransferase (AST). Additionally, these LNPs enhance the serum titers of IgG1 and IgG2a antibodies in mice.

BI-894416 is a novel and highly selective spleen tyrosine kinase inhibitor, designed for the treatment of severe asthma.

Lipid C2 is an ionizable cationic lipid utilized in the formation of lipid nanoparticles (LNP) for the delivery of mRNA in vivo. LNPs containing Lipid C2 and encapsulating mRNA reporter genes specifically accumulate in the liver and spleen of mice, while avoiding the heart, lungs, and kidneys. Additionally, LNPs with Lipid C2 that encapsulate mRNA encoding Epstein-Barr virus (EBV) protein Latent Membrane Protein 2 (LMP-2), when combined with anti-programmed cell death protein 1 (PD-1) antibodies, have been shown to reduce tumor size, reverse T cell exhaustion, increase the percentage of CD3+CD8+ central T cells and CD3+CD8+ effector memory T cells in the spleen, and decrease the percentage of CD3+T cells expressing Pd-1 in a CT26 mouse model of EBV-infected colon cancer.

DBMB is a spleen tyrosine kinase (Syk) inhibitor that significantly suppresses Syk enzyme activity. It possesses anti-inflammatory properties by inhibiting NF-κB signaling, thereby reducing the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB can be utilized in research on inflammatory diseases.

TAK-659 is a spleen tyrosine kinase (SYK) inhibitor.