| 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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| 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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| DC75365 |
Pevonedistat (MLN-4924) |
Pevonedistat, also known as MLN-4924 and TAK-924, is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with potential antineoplastic activity. NAE inhibitor MLN4924 binds to and inhibits NAE, which may result in the inhibition of tumor cell proliferation and survival. NAE activates Nedd8 (Neural precursor cell expressed, developmentally down-regulated 8), an ubiquitin-like (UBL) protein that modifies cellular targets in a pathway that is parallel to but distinct from the ubiquitin-proteasome pathway (UPP). |
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| DC75366 |
Exherin free base |
Exherin, also known as ADH-1, 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 201350A |
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| DC75367 |
Miriplatin hydrate |
Miriplatin (MPT) is a novel platinum complex used in TACE that shows promise for the treatment of hepatocellular carcinoma (HCC). Miriplatin is a lipophilic platinum complex that can be easily suspended in Lipiodol and gradually releases active platinum compounds in tumor tissue. Miriplatin is less severe toxicity profile compared to other platinum anticancer agents. |
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| DC75368 |
Migalastat HCl |
Migalastat HCl, also known as AT1001 or GR181413A, is a pharmacological chaperone that selectively binds, stabilizes, and increases cellular levels of α-Gal A. Oral administration of migalastat HCl reduces tissue GL-3 in Fabry transgenic mice, and in urine and kidneys of some FD patients. Migalastat HCl may provide a potential novel genotype-specific treatment for Fabry Disease (FD). Phase 3 studies are ongoing. Fabry disease (FD) is a genetic disorder resulting from deficiency of the lysosomal enzyme α-galactosidase A (α-Gal A) which leads to globotriaosylceramide (GL-3) accumulation in multiple tissues. |
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| DC75369 |
Abemaciclib free base |
Abemaciclib, also known as LY2835219, is orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 inhibits CDK4 and CDK6 with low nanomolar potency. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. |
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| DC75370 |
Fingolimod HCl |
Fingolimod, also known as FTY720, is an immunosuppressive drug. It is derived from the myriocin (ISP-1) metabolite of the fungus Isaria sinclairii. It is a structural analogue of sphingosine and gets phosphorylated by sphingosine kinases in the cell (most importantly sphingosine kinase. The molecular biology of phospho-fingolimod is thought to lie in its activity at one of the five sphingosine-1-phosphate receptors, S1PR1. |
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| DC75371 |
Epirubicin hydrochloride |
Epirubicin is an anthracycline drug used for chemotherapy. It can be used in combination with other medications to treat breast cancer in patients who have had surgery to remove the tumor. Similarly to other anthracyclines, epirubicin acts by intercalating DNA strands. Intercalation results in complex formation which inhibits DNA and RNA synthesis. It also triggers DNA cleavage by topoisomerase II, resulting in mechanisms that lead to cell death. Binding to cell membranes and plasma proteins may be involved in the compound's cytotoxic effects. Epirubicin also generates free radicals that cause cell and DNA damage.||Epirubicin is favoured over doxorubicin, the most popular anthracycline, in some chemotherapy regimens as it appears to cause fewer side-effects. Epirubicin has a different spatial orientation of the hydroxyl group at the 4' carbon of the sugar - it has the opposite chirality - which may account for its faster elimination and reduced toxicity. Epirubicin is primarily used against breast and ovarian cancer, gastric cancer, lung cancer and lymphomas. |
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| DC75372 |
Icotinib HCl |
Icotinib, also known as BPI-2009, is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, is upregulated in a variety of cancer cell types. |
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| DC75373 |
BPDBA |
BPDBA is a noncompetitive inhibitor of the betaine/GABA transporter 1 (BGT1). |
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| DC75374 |
Entospletinib |
Entospletinib, also known as GS-9973, is a highly selective and orally efficacious Syk inhibitor which is currently undergoing clinical evaluation for autoimmune and oncology indications. In Phase II clinical trials, Entospletinib demonstrates clinical activity in subjects with relapsed or refractory CLL with acceptable toxicity. |
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| DC75375 |
Filgotinib |
Filgotinib, also known as GLPG0634, is a potent and selective JAK1 inhibitor under investigation for the treatment of rheumatoid arthritis (RA) and Crohn's disease. It is considered a promising agent as it inhibits JAK1 selectively. Filgotinib displayed a selectivity of 30-fold for JAK1- over JAK2-dependent signaling. GLPG0634 dose-dependently inhibited Th1 and Th2 differentiation and to a lesser extent the differentiation of Th17 cells in vitro. |
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