balb/c

Capmatinib (INCB28060) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

Capmatinib 2HCl.H2O (NVP-INC280 2HCl.H2O) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10, 000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.

Capmatinib xHCl (INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor, potently blocking in vitro kinase activity (IC50 = 0.13 nM) as well as constitutive or HGF-stimulated activity in cells (IC50 values range from 0.3 to 1.1 nM).

Traxanox TFA is an orally available diuretic. Traxanox TFA enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox TFA restores inhibition of antibody production in BALB c mice. Traxanox TFA is also effective in restoring antibody production in BALB c mice. Traxanox TFA has been shown to enhance phagocytosis in BALB c mice.

Traxanox is an orally available diuretic.Traxanox enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro.Restorative effect of Traxanox on inhibition of antibody production in BALB c mice.

TAK-041 (NBI-1065846) is a potent and selective GPR139 agonist.

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day.

KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007/s10637-010-9584-2. Epub 2010 Nov 16. ).

Reveromycin B is a spiroketal bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb MK cells (IC50 = 6 μg ml) and exhibits pH-dependent antifungal activity against C. albicans [MICs = 15.6 and >500 μg ml at pH 3.0 and 7.4, respectively]. Unlike reveromycin A and reveromycin C, reveromycin B does not inhibit the proliferation of KB and K562 cells.

OVA Peptide (323-339) represents a T and B cell epitope of Ovalbumin (Ova), which play an important role in the development and development of immediate hypersensitivity in BALB/c mice.

Oxiconazole nitrate (Ro 13-8996) is the nitrate salt form of oxiconazole, a broad-spectrum imidazole derivative with antifungal activity. Likely inhibiting cytochrome P450-dependent demethylation of lanosterol, it prevents ergosterol synthesis, a crucial component of the fungal cell membrane. This disruption of membrane synthesis and integrity alters permeability, promotes loss of essential intracellular components, and inhibits fungal cell growth.

Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor with an IC50 of 1.09 μM. It inhibits cell migration and tube formation, exhibits anti-angiogenic properties, and effectively hinders tumor growth in HT29 xenograft Balb c nude mice [1].

Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause any apparent toxic effect on other tissues.Xylocydine is a good candidate for an anti-cancer drug for HCC therapy.

Receptor for advanced glycation end products (RAGE) antagonist. Blocks S100P, S100A4 and HMGB-1 mediated RAGE activation in vitro and in vivo. Inhibits growth and metastasis of rat glioma tumors. Reduces cell growth and RAGE-mediated NF-κB activity in hum

Antitubercular agent-20 is an orally active antitubercular agent. agent-20 showed low cytotoxicity and good tolerability in BALB/c mice.

Traxanox sodium is an orally available diuretic. Traxanox sodium enhances phagocytosis of yeast granules by mouse peritoneal macrophages or rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox sodium restores inhibition of antibody production in BALB/c mice. Traxanox sodium is also effective in restoring antibody production in BALB/c mice. Traxanox sodium has been shown to enhance phagocytosis in BALB/c mice.

RPR-200765A is a potent and selective inhibitor of p38 MAP kinase (IC50 = 50 nM). It inhibits LPS-stimulated TNFalpha release both in vitro, from human monocytes (EC50 = 110 nM), and in vivo in Balb/c mice (ED50 = 6 mg/kg). At oral doses between 10 and 30 mg/kg/day it reduces the incidence and progression in the rat streptococcal cell wall (SCW) arthritis model when administered in either prophylactic or therapeutic dosing regimens. The compound, which is a mesylate salt and exists as a stable monohydrate, shows good oral bioavailabiltiy (F = 50% in the rat) and excellent chemical stability. The data from the SCW disease model suggests that RPR200765A could exhibit a profile of disease modifying activity in rheumatoid arthritis (RA) patients which is not observed with current drug therapies.

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb MK cells (IC50 = 0.7 μg ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 μM.

Lyoniside and saracoside are cytotoxic to promastigotes and intracellular amastigotes, they demonstrate strong anti-leishmanial efficacies in BALB/c mice model of leishmaniasis, suggests that these two compounds potential anti-leishmanial candidates. The

Antitubercular agent-19 is an antitubercular agent. antitubercular agent-19 showed good antitubercular effects against MTB H37Rv and MDR-MTB (MIC <0.016 μg/ml). antitubercular agent-19 showed low cytotoxicity and relatively high acute lethality in BALB/c mice. Antitubercular agent-19 exhibited low cytotoxicity and relatively high acute lethal toxicity in BALB/c mice.

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM, exhibiting antimalarial activity by inducing developmental arrest of malaria parasites at the schizont stage[1][2].

Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM and an IC50 value of 0.109 μM. It tightly binds to TNF-α, blocking its interaction with TNFR1, and has potential for TNF-α mediated inflammatory and autoimmune disease research [1].

OVA Peptide (323-339) constitutes a T and B cell epitope derived from Ovalbumin (Ova), crucial for eliciting immediate hypersensitivity reactions in BALB c mice.

HKI12134085 (compound 3), an orally administered nitrobenzothiazinone (BTZ) derivative, demonstrates antibacterial efficacy against Mycobacterium tuberculosis. This compound exhibits significant in vivo inhibitory potency within a BALB c mouse model of Mycobacterium tuberculosis infection [1].

Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb MK cells and exhibits pH-dependent antifungal activity against C. albicans [MICs = 2 and >500 μg ml at pH 3 and 7.4, respectively]. Reveromycin D also inhibits the proliferation of KB and K562 cells [IC50s = 1.6 and 1.3 μg ml, respectively].

Redaporfin, also known as F-2BMet or LUZ-11, is a photosensitizer for Photodynamic Therapy (PDT) of cancer. Redaporfin showed a high efficacy in the treatment of male BALB/c mice with subcutaneously implanted colon (CT26) tumours. Vascular-PDT with 1.5 mg