| DC75194 |
Valylvaline |
Valylvaline is a bioactive chemical. |
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| DC75195 |
IACS-010759 free base |
IACS-010759 or IACS-10759 is a potent and selective Oxidative Phosphorylation Inhibitor (IC50 < 10 nM) with potential antineoplastic activity. IACS-010759 binds to and inhibits complex I of the electron transport chain (NADH ubiquinone oxidoreductase), thereby selectively depriving tumor cells of nutrients, and energy, and inhibiting nucleotide and amino acid production, which induces autophagy, causes tumor cell death and inhibits cell proliferation. Mitochondrial complex I, which is hyperactivated in cancer cells to meet their increased demands for energy, plays a key role in the promotion of cancer cell proliferation. |
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| DC75196 |
Cobimetinib |
Cobimetinib, also known as GDC-0973 and XL-518, RG 7420, is an orally bioavailable small-molecule inhibitor of mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), with potential antineoplastic activity. MEK inhibitor GDC-0973 specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation. Preclinical studies have demonstrated that this agent is effective in inhibiting the growth of tumor cells bearing a B-RAF mutation, which has been found to be associated with many tumor types. |
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| DC75197 |
RXDX-105 (CEP-32496) |
RXDX-105, also known as Agerafenib, CEP-32496 and AC013773, is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity. |
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| DC75198 |
Methyl leucylleucinate HCl |
Methyl leucylleucinate HCl is a lysosomal condensation product that has been reported to be cytotoxic towards natural killer cells and CD4+ and CD8+ T lymphocytes without affecting helper T cells and B cells.1,2 It has also been shown to induce death of monocytes, polymorphonuclear leukocytes, and myeloid tumor cells.2 Upon entry into cells via receptor-mediated endocytosis, LLME undergoes a condensation process catalyzed by dipeptidyl peptidase I (DPPI) in lysosomes. This condensation leads to lysosomal rupture and DNA fragmentation in DPPI-expressing immune cells such as cytotoxic T cells and natural killer cells.2 |
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| DC75199 |
Goserelin Acetate |
Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. Goserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of goserelin inhibits the secretion of pituitary gonadotropin, thereby decreasing levels of testosterone (in males) and estradiol (in females). Administration of this agent in a depot formulation may result in the regression of sex hormone-sensitive tumors and a reduction in sex organ size and function. |
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| DC75200 |
4-n-Nonylphenol |
Nonylphenols are a family of closely related organic compounds composed of phenol bearing a 9 carbon-tail. Nonylphenols can come in numerous structures, all of which may be considered alkylphenols. They are used in manufacturing antioxidants, lubricating oil additives, laundry and dish detergents, emulsifiers, and solubilizers. They are used extensively in epoxy formulation in North America but its use has been phased out in Europe. These compounds are also precursors to the commercially important non-ionic surfactants alkylphenol ethoxylates and nonylphenol ethoxylates, which are used in detergents, paints, pesticides, personal care products, and plastics. Nonylphenol has attracted attention due to its prevalence in the environment and its potential role as an endocrine disruptor and xenoestrogen, due to its ability to act with estrogen-like activity. The estrogenicity and biodegradation heavily depends on the branching of the nonyl sidechain. Nonylphenol has been found to act as an agonist of the GPER (GPR30). |
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| DC75201 |
LY2584702 free base |
LY-2584702, also known as LYS6K2, is an orally available inhibitor of p70S6K signaling, with potential antineoplastic activity. LY2584702 inhibits ribosomal protein S6 Kinase (p70S6K), and prevents phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation. P70S6K, a serine/threonine kinase, acts downstream of PIP3 and phosphoinositide-dependent kinase-1 in the PI3 kinase pathway, is often upregulated in a variety of cancer cells, and is involved in the regulation of cell growth, proliferation, motility, and survival. |
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| DC75202 |
Fosaprepitant free acid
Featured
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Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4 |
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| DC75203 |
Bisnafide mesylate |
Bisnafide is a Naphthalimide Analogue that acts as DNA intercalator and topo II inhibitor. It is also an antiangiogenic agent. Antiangiogenic agents can normalize tumor vessels and promote the delivery of cytotoxic agents to tumor sites. |
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| DC75204 |
Estramustine phosphate sodium |
Estramustine phosphate sodium is a synthetic molecule that combines estradiol and nornitrogen mustard through a carbamate link. Estramustine and its major metabolite estramustine bind to microtubule-associated proteins (MAPs) and tubulin, thereby inhibiting microtubule dynamics and leading to anaphase arrest in a dose-dependent fashion. This agent also exhibits anti-androgenic effects. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). |
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| DC75205 |
Sapropterin HCl |
Sapropterin, also known as Tetrahydrobiopterin (BH4, THB, trade name Kuvan) or sapropterin (INN) is a naturally occurring essential cofactor of the three aromatic amino acid hydroxylase enzymes, used in the degradation of amino acid phenylalanine and in the biosynthesis of the neurotransmitters serotonin (5-hydroxytryptamine, 5-HT), melatonin, dopamine, norepinephrine (noradrenaline), epinephrine (adrenaline), and is a cofactor for the production of nitric oxide (NO) by the nitric oxide synthases. Chemically, its structure is that of a reduced pteridine derivative. |
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| DC75206 |
Aftobetin free base |
Aftobetin, also known as ANCA11 and NCE-11, is a novel amyloid–binding compound applied topically in the form of an ophthalmic ointment. Aftobetin may be of useful as an aid in the diagnosis Alzheimer's disease. |
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| DC75207 |
A22 hydrochloride |
A22 is an inhibitor of MreB, an actin-like bacterial protein, and has been shown to act as an antiobiotic adjuvant. A22 inhibition of MreB disrupts the bacterial actin cytoskeleton, which can cause an increase in cell permeability and altered transport. |
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| DC75208 |
S38093 free base |
S38093 is an inverse agonist at histamine H3 receptors. S38093 has no affinity for other histaminergic receptors. |
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| DC75209 |
LY2389575 HCl |
LY2389575 is a selective negative allosteric modulator of mGlu3. LY2389575 exhibits > 65-fold selectivity for mGlu3 over other mGlu receptors. LY2389575 abolishes the neuroprotective action of LY 379268 against amyloid β toxicity in mixed cortical neuronal and astrocyte cell cultures. |
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| DC75210 |
Paraquat dichloride |
Paraquat is classified as a viologen, a family of redox-active heterocycles of similar structure. Paraquat is one of the most widely used herbicides. It is quick-acting and non-selective, killing green plant tissue on contact. It is also toxic to human beings and animals due to its redox activity, which produces superoxide anions. It has been linked to the development of Parkinson's disease. The name is derived from the para positions of the quaternary nitrogens. Paraquat may be in the form of salt with chloride or other anions; quantities of the substance are sometimes expressed by cation mass alone (paraquat cation, paraquat ion) |
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| DC75211 |
Gloxazone |
Gloxazone is an effective but toxic anaplasmacide. |
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| DC75212 |
Gusacitinib |
Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and Pfeiffer. |
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| DC75213 |
Naratriptan HCl |
Naratriptan is a selective 5-HT1 receptor subtype agonist for the treatment of migraine headache. Naratriptan binds with high affinity to human cloned 5-HT1B/1D receptors. Migraines are likely due to local cranial vasodilatation and/or to the release of sensory neuropeptides (including substance P and calcitonin gene-related peptide) through nerve endings in the trigeminal system. The therapeutic activity of AMERGE for the treatment of migraine headache is thought to be due to the agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels (including the arterio-venous anastomoses) and sensory nerves of the trigeminal system, which result in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release. |
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| DC75214 |
Raltegravir potassium |
Raltegravir, also known as MK-0518, is an antiretroviral drug used to treat HIV infection. Raltegravir is a human immunodeficiency virus (HIV) integrase strand transfer inhibitor (HIV-1 INSTI) with HIV-1 antiviral activity. Raltegravir binds to and inhibits integrase, an HIV enzyme that inserts viral genetic material into the genetic material of the infected human cell. Inhibition of integrase prevents insertion of HIV DNA into the human DNA genome, thus blocking HIV replication. It received approval by the U.S. Food and Drug Administration (FDA) in October 2007, the first of a new class of HIV drugs, the integrase inhibitors, to receive such approval. |
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| DC75215 |
Anlotinib free base |
Anlotinib, also known as AL3818 and Catequentinib, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth. |
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| DC75216 |
EOAI3402143 free base |
EOAI3402143 is a dose-dependent inhibitor of Usp9x and Usp24 activity. It acts by increasing tumor cell apoptosis and fully blocking or regressing myeloma tumors in mice. |
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| DC75217 |
FTI-277 HCl |
FTI-277 is a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for FTase over geranylgeranyltransferase I (GGTase I) (IC50 = 50 nM). FTI-277, the methyl ester derivative of FTI-276, was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. |
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| DC75218 |
ABT-751 |
ABT-751, also known as E7010, is an orally bioavailable antimitotic sulfonamide. ABT-751 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication. This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect. |
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| DC75219 |
AGN-201904 |
AGN 201904 is a slowly absorbed, acid-stable pro-proton pump inhibitor (pro-PPI) rapidly converted to omeprazole in the systemic circulation giving a prolonged residence time. AGN-201904 is a proton pump inhibitor; AGN-201904-Z is the sodium salt; AGN-201904 is an omeprazole prodrug. AGN 201904 produced a significantly greater and more prolonged acid suppression than esomeprazole, and nocturnal acid suppression was more prolonged over all 5 days. AGN 201904 should provide true once-a-day treatment and better clinical efficacy than current PPIs. |
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| DC75220 |
Cefcanel daloxate HCl |
Cefcanel daloxate, also known as KY-109, is a pro-drug to improve oral absorption of KY-087. The antimicrobial activities of KY-087 against clinically isolated Gram-positive organisms were superior to those of CEX and CCL. The antimicrobial activities of KY-087 against Gram-negative organisms, such as Enterobacter sp., Serratia, and Pseudomonas sp., were less active. KY-087 showed dose-related bactericidal activity against Staphylococcus aureus and Escherichia coli. The therapeutic efficacy of KY-109 against experimental intraperitoneal infections caused by Gram-positive and Gram-negative organisms in mice was comparable to that of CEX but inferior to that of CCL. In experimental granuloma pouch models in rats and kidney infection in rabbits, therapeutic efficacy of KY-109 was either comparable or superior to that of CEX and CCL. |
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| DC75221 |
E6446 HCl |
E6446 is a synthetic antagonist of nucleic acid-sensing TLRs. , In vitro, low doses of E6446 specifically inhibited the activation of human and mouse TLR9. Tenfold higher concentrations of this compound also inhibited the human TLR8 response to single-stranded RNA. In vivo, therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection. Furthermore, severe signs of ECM, such as limb paralysis, brain vascular leak, and death, were all prevented by oral treatment with E6446. |
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| DC75222 |
Tucidinostat HCl |
Tucidinostat (also known as HBI-8000, Chidamide, and CS-055) is a benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Tucidinostat selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. This agent also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. |
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| DC75223 |
Sorafenib free base |
Sorafenib, also known as BAY 43-9006, is a synthetic compound targeting growth signaling and angiogenesis. Sorafenib blocks the enzyme RAF kinase, a critical component of the RAF/MEK/ERK signaling pathway that controls cell division and proliferation; in addition, sorafenib inhibits the VEGFR-2/PDGFR-beta signaling cascade, thereby blocking tumor angiogenesis. Sorafenib was approved in 2005 for use in the treatment of advanced renal cancer. |
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