DC75335 |
TCS-401 HCl |
TCS-401 (HCI) is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B; Ki = 0.29 µM). It inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 at much higher concentrations (Kis = 59, 560, 1,100, >2,000, >2,000, and >2,000 μM, respectively).1 Several PTPs have been proposed to act as negative regulators of insulin signaling, thus this enzyme is a potential drug target in diabetes. |
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DC75336 |
Phosphatidyl choline (from Soybean) |
Phosphatidylcholines (PC) are a class of phospholipids that incorporate choline as a headgroup. They are a major component of biological membranes and can be easily obtained from a variety of readily available sources, such as egg yolk or soybeans, from which they are mechanically or chemically extracted using hexane. They are also a member of the lecithin group of yellow-brownish fatty substances occurring in animal and plant tissues. Dipalmitoyl phosphatidylcholine (aka: lecithin) is a major component of pulmonary surfactant and is often used in the L/S ratio to calculate fetal lung maturity. |
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DC75337 |
KN-93 (HCI) |
KN-93 is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II). It inhibits fibroblast CaMK-II activity and cell growth in a dose-dependent manner, reversibly arrests cells in G1 and induces apoptosis. |
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DC75338 |
PF-562271 Besylate |
PF-562271 Besylate, also known as PF-562,271 and PF-271, is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. PF-562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival. Note: PF-562271 benzesulfonate is also called PF-562271 besylate. |
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DC75339 |
Levomefolate calcium |
Levomefolate calcium, also known as LMCA and BAY 86-7660, is the calcium salt of 5-methyltetrahydrofolic acid, a biologically active form of folic acid that functions, in conjunction with Vitamin B12 , as a methyl-group donor involved in the conversion of homocysteine to methionine. Levomefolate is included in formulations of certain oral contraceptives to ensure adequate folic acid levels in women of child-bearing age to reduce the risk of neural tube defects. |
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DC75340 |
Glasdegib (PF-04449913) |
Glasdegib, also known as PF-04449913, is an orally bioavailable small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. Hedgehog inhibitor PF-04449913 appears to inhibit Hh pathway signaling. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies. |
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DC75341 |
Gemcitabine Hydrochloride |
Gemcitabine hydrochloride is the hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. |
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DC75342 |
SNS-032 |
SNS-032, also known as BMS-387032, is a 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDK inhibitor SNS-032 selectively binds to CDKs 2, 7, and 9, preventing their phosphorylation and activation; inhibition of CDK activity may result in cell cycle arrest, the induction of apoptosis and decreased tumor cell proliferation in susceptible tumor cell populations. This agent has been shown to sensitize radioresistant tumor cells to ionizing radiation. |
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DC75343 |
SB-334867 free base |
SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorectic effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes. |
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DC75344 |
Semaglutide |
Semaglutide is a glucagon-like peptide-1 receptor agonist. The drug decreases blood sugar levels. The decrease is theorized to be caused by the mimicking of the incretin glucagon-like peptide-1 (GLP-1). It also appears to enhance growth of pancreatic beta cells, which are responsible for insulin production and release. Additionally, it inhibits the production of glucagon, the hormone that increases glycogenolysis (release of stored carbohydrate from the liver) and gluconeogenesis (synthesis of new glucose). It reduces food intake by lowering appetite and slowing down digestion in the stomach, helping reduce body fat. |
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DC75345 |
Sitagliptin Phosphate Monohydrate |
Sitagliptin, also known as MK-0431, is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses. |
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DC75346 |
BIBO-3304 TFA |
BIBO-3304 is a selective Y1 receptor antagonist. Y1 receptor proteins from neuropeptide Y have a roll in appetite stimulation. |
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DC75347 |
Avadomide HCl |
Avadomide, also known as CC-122, is an orally available pleiotropic pathway modulator with potential antineoplastic activity. CC-122 mimics an interferon response and has antitumor activity in DLBCL CC-122 binds Cereblon (CRBN) and promotes degradation of Aiolos and Ikaros in diffuse large B-cell lymphoma (DLBCL) and T cells in vitro, in vivo, and in patients, resulting in both cell autonomous as well as immunostimulatory effects. |
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DC75348 |
Semaxanib |
Semaxanib, also known as SU5416, is a quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature. This agent also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. |
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DC75349 |
Gentamicin sulfate |
Gentamicin is an antibiotic used to treat several types of bacterial infections. This may include bone infections, endocarditis, pelvic inflammatory disease, meningitis, pneumonia, urinary tract infections, and sepsis among others. It is not effective for gonorrhea or chlamydia infections. Gentamicin is a complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1(subA), obtained from Micromonospora purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit protein synthesis. |
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DC75350 |
Semapimod HCl |
Semapimod, known as CNI-1493, is a cytokine inhibitor. Semapimod is an investigational new drug which has anti-inflammatory, anti-cytokine, immunomodulatory, antiviral and antimalarial properties. Structurally, semapimod is synthetic guanylhydrazone mitogen-activated protein kinase blocker, as a potential treatment for Crohn's disease and other inflammatory conditions. |
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DC75351 |
LGH447 dihydrochloride |
LGH447 dihydrochloride is potent and specific pan-PIM inhibitor that inhibits proliferation of several AML cell lines showing dual antitumoral and bone antiresorptive effects. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency. |
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DC75352 |
SB-743921 HCl |
SB-743921 is a synthetic small molecule with potential antineoplastic properties. SB-743921 selectively inhibits kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. Inhibition of KSP results in inhibition of mitotic spindle assembly and interrupts cell division, thereby causing cell cycle arrest and induction of apoptosis. |
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DC75353 |
Diphenhydramine HCl |
Diphenhydramine is a first-generation antihistamine possessing anticholinergic, antitussive, antiemetic, and sedative properties that is mainly used to treat allergies. It is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms. |
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DC75354 |
Fostamatinib sodium |
Fostamatinib, also known as R 788 and R-935788, is an orally active, potent and selective Syk kinase inhibitor with potential anti-inflammatory and immunomodulating activities. Fostamatinib is also a pro-drug of R-406. Fostamatinib inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage. |
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DC75355 |
BI-44370 |
BI-44370 is a CGRP (calcitonin gene-related peptide) receptor antagonist that can be used to treat migraines and other chronic pain.Efficacy of BI 44370 TA was shown in a dose-dependent manner in the treatment of acute migraine attacks. |
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DC75356 |
Prefolic A |
Prefolic A, also known as 5-Methyltetrahydrofolate, is a biologically active form of folic acid that functions, in conjunction with vitamin B12, as a methyl-group donor involved in the conversion of homocysteine to methionine. Prefolic A has applications as a fertility supplement. |
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DC75357 |
SEL120-34A HCl |
SEL120-34A is a potent and selective CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. EL120-34A inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells in vitro. Consistently, regulation of STATs- and NUP98-HOXA9- dependent transcription has been observed as a dominant mechanism of action in vivo. |
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DC75358 |
Neomycin sulfate |
Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eyedrops. The discovery of neomycin dates back to 1949. It was discovered in the lab of Selman Waksman. Neomycin belongs to aminoglycoside class of antibiotics that contain two or more aminosugars connected by glycosidic bonds. |
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DC75359 |
MS049 free base |
MS049 is a potent and selective inhibitor of PRMT4,6 and is active in cells. |
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DC75360 |
BMS-1166 HCl |
BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor. BMS-1166 binds to human PD-L1 and blocks its interaction with PD-1. BMS-1166 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. Moreover, BMS-1166 was effective in attenuating the inhibitory effect of the cell surface-associated PD-L1. |
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DC75361 |
Ezatiostat |
Ezatiostat is a liposomal small-molecule glutathione analog inhibitor of glutathione S-transferase (GST) P1-1 with hematopoiesis-stimulating activity. After intracellular de-esterification, the active form of ezatiostat binds to and inhibits GST P1-1, thereby restoring Jun kinase and MAPK pathway activities and promoting MAPK-mediated cellular proliferation and differentiation pathways. This agent promotes the proliferation and maturation of hematopoietic precursor cells, granulocytes, monocytes, erythrocytes and platelets. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). |
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DC75362 |
Oclacitinib |
Oclacitinib, also known as PF03394197, is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. Oclacitinib inhibited JAK family members by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nm). Oclacitinib was most potent at inhibiting JAK1 (IC50 = 10 nm). Oclacitinib also inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50 's ranging from 36 to 249 nM. |
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DC75363 |
Exherin TFA |
Exherin TFA salt, also known as ADH-1 TFA, is the TFA salt form of exherin, which is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell-cell adhesion and signaling mechanisms; may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels. Note the old CAT# for this product was 201350b |
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DC75364 |
Olodanrigan sodium |
Olodanrigan, also known as EMA-401 and PD-126055, is an angiotensin AT2 antagonist potentially for treatment of postherpetic neuralgia (PHN). EMA401 targets angiotensin II type 2 receptors, which may have importance for painful sensitization. EMA401 may alleviate pain and provides relief by blocking the AngII induced potentiation which is thought to be coupled to protein kinase A |
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