| DC75245 |
Megestrol Acetate |
Megestrol acetate is the acetate ester of megestrol, a synthetic derivative of the naturally occurring female sex hormone progesterone, with progestogenic, antiestrogenic, and antineoplastic activities. Mimicking the action of progesterone, megestrol binds to and activates nuclear progesterone receptors (PRs) in the reproductive system and pituitary; ligand-receptor complexes are translocated to the nucleus where they bind to progesterone response elements (PREs) located on target genes. |
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| DC75246 |
Omecamtiv mecarbil |
Omecamtiv mecarbil, also known as CK-1827452, is a cardiac specific myosin activator. It is clinically tested for its role in the treatment of left ventricular systolic heart failure. Omecamtiv Mecarbil specifically targets and activates myocardial ATPase and improves energy utilization. Omecamtiv Mecarbil improves systolic function by increasing the systolic ejection duration/stroke volume, without consuming more ATP energy, oxygen or altering intracellular calcium levels causing an overall improvement in cardiac efficiency. (source: http://en.wikipedia.org/wiki/Omecamtiv_mecarbil) |
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| DC75247 |
Maropitant free base |
Maropitan, also known as CJ 11972, is a neurokinin (NK1) receptor antagonist, which was developed by Zoetis specifically for the treatment of motion sickness and vomiting in dogs. It was approved by the FDA in 2007 for use in dogs, and more recently has also been approved for use in cats. |
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| DC75248 |
Sardomozide HCl |
Sardomozide HCl, also known as SAM486A or CGP48664, is a second-generation polyamine synthesis inhibitor, which inhibits the activity of the polyamine biosynthetic enzyme S-adenosylmethionine decarboxylase (SAMDC). SAM486 is more potent and specific than the first-generation SAMDC inhibitor methylglyoxal (bis) guanylhydrazone (MGBG). Preclinical testing confirmed promising antiproliferative activity. The in vitro tests showed that p53 wild-type NB cells were highly sensitive to SAM486A treatment. Most notably, SAM486A treatment resulted in the rapid accumulation of proapoptotic proteins p53 and Mdm2. |
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| DC75249 |
Larotrectinib sulfate |
Larotrectinib, also known as ARRY-470 and LOXO-101, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons. |
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| DC75250 |
Abemaciclib mesylate |
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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| DC75251 |
Fedratinib |
Fedratinib, also known as TG101348 and SAR302503, is a JAK2 inhibitor, is also an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. JAK2 inhibitor TG101348 competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival. |
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| DC75252 |
STO-609 acetate |
STO-609 is a cell-permeable inhibitor of calcium/calmodulin-dependent kinase kinases (CaMKK) isoforms CaMKKα and CaMKKβ (Ki = 80 and 15 ng/ml, respectively). STO-609 is a selective and cell-permeable inhibitor of CaM-KK and that it may be a useful tool for evaluating the physiological significance of the CaM-KK-mediated pathway in vivo as well as in vitro. |
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| DC75253 |
Acyclovir |
Acyclovir, a GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes. Acyclovir is an antiviral medication. It is primarily used for the treatment of herpes simplex virus infections, chickenpox, and shingles. |
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| DC75254 |
Verubecestat free base |
Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. |
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| DC75255 |
Lapatinib (free base) |
Lapatinib is a synthetic, orally-active quinazoline with potential antineoplastic activity. Lapatinib reversibly blocks phosphorylation of the epidermal growth factor receptor (EGFR), ErbB2, and the Erk-1 and-2 and AKT kinases; it also inhibits cyclin D protein levels in human tumor cell lines and xenografts. EGFR and ErbB2 have been implicated in the growth of various tumor types. Check for active clinical trials or closed clinical trials using this agent. |
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| DC75256 |
GW-4869 HCl |
GW-4869 is a cell-permeable, non-competitive inhibitor of neutral sphingomyelinases (IC50 = 1 μM). It inhibits TNF-α-mediated sphingomyelin hydrolysis (100% inhibition at 20 μM). GW4869 is cytotoxic to high phosphatidylserine-expressing myeloma cells. Blockade of exosome generation with GW4869 dampens the sepsis-induced inflammation and cardiac dysfunction. |
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| DC75257 |
Idarubicin HCl |
Idarubicin is a semisynthetic 4-demethoxy analogue of the antineoplastic anthracycline antibiotic daunorubicin. Idarubicin intercalates into DNA and interferes with the activity of topoisomerase II, thereby inhibiting DNA replication, RNA transcription and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes more efficiently than other anthracycline antibiotic compounds. |
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| DC75258 |
BIX01294 HCl |
BIX01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3. BIX01294 suppresses osteoclast differentiation on mouse macrophage-like Raw264.7 cells. BIX01294 enhances the cardiac potential of bone marrow cells. |
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| DC75259 |
Pifithrin-beta HBr |
Pifithrin-beta, also known as QB102 and Cyclic-Pifithrin-α, is is p53 functional inhibitor. Pifithrin-β counteracts the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. |
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| DC75260 |
Degarelix acetate |
Degarelix, also known as FE-200486 and ASP-3550, is a long-acting, synthetic peptide with gonadotrophin-releasing hormone (GnRH) antagonistic properties. Degarelix targets and blocks GnRH receptors located on the surfaces of gonadotroph cells in the anterior pituitary, thereby reducing secretion of luteinizing hormone (LH) by pituitary gonadotroph cells and so decreasing testosterone production by interstitial (Leydig) cells in the testes. Degarelix acetate was approved in 2008. |
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| DC75261 |
Tenofovir alafenamide (free base) |
Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1. |
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| DC75262 |
LY2584702 tosylate salt |
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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| DC75263 |
Nigericin sodium |
Nigericin is a cationic ionophore that inhibits Golgi function and suppresses growth of gram positive bacteria. It also prevents viral activation and triggers activation of the NALP3 inflammasome. Nigericin acts as an H+, K+, Pb2+ ionophore. Most commonly it is an antiporter of H+ and K+. In the past nigericin was used as an antibiotic active against gram positive bacteria. It inhibits the Golgi functions in Eukaryotic cells. Its ability to induce K+ efflux also makes it a potent activator of the NLRP3 inflammasome. |
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| DC75264 |
Taladegib |
Taladegib, also known LY2940680, is a potent Hedgehog inhibitor with potential anticancer activity. LY2940680 inhibits cancer growth in cell lines containing a mutation in the gene encoding Smoothened that researchers had previously observed in patient with cancer who developed resistance to vismodegib. |
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| DC75265 |
Caspofungin acetate |
Caspofungin acetate is a lipopeptide antifungal drug. It is a member of a new class of antifungals termed the echinocandins. It works by inhibiting the enzyme (1→3)-β-D-glucan synthase and thereby disturbing the integrity of the fungal cell wall. Caspofungin acetate for injection was originally approved by FDA in USA, and the EMEA in Europe, in 2001. |
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| DC75266 |
Nepicastat HCl |
Nepicastat, also known as SYN117 and RS-25560-197, is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. It has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated. As of 2012, clinical trials to assess nepicastat as a treatment for post-traumatic stress disorder (PTSD) and cocaine dependence have been completed. In Phase 2 study treatment with nepicastat was not effective in relieving PTSD-associated symptoms when compared to placebo. |
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| DC75267 |
MRT-68921 HCl |
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively). |
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| DC75268 |
Telotristat etiprate |
Telotristat etiprate, its free base also known as LX1606 or LX1032, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor . Telotristat etiprate has activity in controlling diarrhea associated with carcinoid syndrome. LX1606 acts by inhibiting the enzyme tryptophan hydoxylase (TPH) and reduces serotonin production both inside and outside the GI tract without affecting brain serotonin levels. TPH is the rate-limiting enzyme involved in serotonin biosynthesis and is present in metastatic carcinoid tumor cells. |
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| DC75269 |
2-Iminothiolane HCl |
2-Iminothiolane HCl, or Traut's Reagent,is commonly used to convert primary amines into sulfhydryl groups in a one-step process is called thiolation. It is a useful RNA-protein crosslinking reagent and an effective thiolation reagent for polysaccharides. |
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| DC75270 |
Talazoparib tosylate |
Talazoparib, also known as BMN-673 and MDV-3800, is an orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential antineoplastic activity (PARP1 IC50 = 0.57 nmol/L). Talazoparib acts as an inhibitor of poly ADP ribose polymerase(PARP) which aids in single strand DNA repair. Cells that have BRCA1/2 mutations are susceptible to the cytotoxic effects of PARP inhibitors because of an accumulation of DNA damage. Talazoparib is theorized to have a higher potency than olaparib due to the additional mechanism of action called PARP trapping. PARP trapping is the mechanism of action where the PARP molecule is trapped on the DNA, which interferes with the cells ability to replicate. Talazoparib is found to be ~100 fold more efficient in PARP trapping than olaparib. |
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| DC75271 |
U-18666A |
U-18666A is an inhibitor of cholesterol synthesis. It acts by inhibiting desmosterol Δ24-reductase. U18666A inhibits classical swine fever virus replication through interference with intracellular cholesterol trafficking. U18666A or other cholesterol transport inhibitor may be considered as the antiviral drug for the treatment of cats with FIP. U18666A accumulated intracellular free cholesterol in the culture of normal medium but not cholesterol-free medium. U18666A also induced reactive oxygen species (ROS) generation in normal medium but much less in cholesterol-free medium. |
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| DC75272 |
OTS964 HCl |
OTS964 is a potent and selective TOPK inhibitor with potential anticancer activity. OTS964 inhibits TOPK kinase activity with high affinity and selectivity. Similar to the knockdown effect of TOPK small interfering RNAs (siRNAs), this inhibitor causes a cytokinesis defect and the subsequent apoptosis of cancer cells in vitro as well as in xenograft models of human lung cancer. Although administration of the free compound induced hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively caused complete regression of transplanted tumors without showing any adverse reactions in mice. ( Sci Transl Med. 2014 Oct 22;6(259):259ra145. ) |
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| DC75273 |
Grazoprevir potassium |
Grazoprevir, also known as MK5172, is a drug approved for the treatment of hepatitis C. Grazoprevir is a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets. It has good activity against a range of HCV genotype variants, including some that are resistant to most currently used antiviral medications. |
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| DC75274 |
LDN-193189 |
LDN193189 is a highly potent small molecule BMP inhibitor with IC50 of 5 and 30 nM for ALK2 and ALK3, respectively. LDN193189 also inhibits BMP type I receptors ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation. |
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