| 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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| 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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| DC75275 |
DDP-38003 2HCl |
DDP-38003 2HCl is an orally available inhibitor of histone lysine-specific demethylase 1A (LSD1). |
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| DC75276 |
Resminostat HCl |
Resminostat is an orally bioavailable inhibitor of histone deacetylase 1 (HDAC1), HDAC3, and HDAC6 (IC50s = 43-72 nM), |
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| DC75277 |
ICI-199441 HCl |
ICI-199441 HCl is a highly potent κ agonist. ICI 199441 was found to strongly inhibit the activity of cytochrome P450 2D6 (CYP2D6) (1: CYP2D6 IC50=26 nM). |
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| DC75278 |
Daunorubicin free base |
Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis. |
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| DC75279 |
Onvansertib free base |
Onvansertib, also know as NMS-P937, PCM-075 and NMS1286937, is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Onvansertib selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressing tumor cells. PLK1 is a serine/threonine protein kinase crucial in the regulation of mitosis. |
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| DC75280 |
JQ1-Carboxylic acid |
JQ1-Carboxylic acid also known as JQ1 Acid, is an inhibitor of bromodomain and extra terminal domain (BET) family proteins. |
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| DC75281 |
WCK-4234 sodium |
WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibited class A, C and D β-lactamases with unprecedented k2/K values against OXA carbapenemases. WCK-4234 inhibited class A, C and D β-lactamases with unprecedented k2/K values against OXA carbapenemases. WCK-4234 formed highly stable acyl-complexes via mass spectrometry. WCK-4234 is a novel β-lactamase inhibitor that demonstate potent cross-class inhibition and clinical studies targeting MDR infections are warranted. |
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| DC75282 |
Levomilnacipran HCl |
Levomilnacipran (brand name Fetzima) is an antidepressant approved for the treatment of major depressive disorder in the United States. It was developed by Forest Laboratories and Pierre Fabre Group, and was approved by the Food and Drug Administration in July 2013. Levomilnacipran is the levo- enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin-norepinephrine reuptake inhibitor (SNRI). (Source: http://en.wikipedia.org/wiki/Levomilnacipran) |
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| DC75283 |
PNU112455A |
PNU112455A is an ATP site competetive inhibitor of CDK2 and CDK5. PNU112455A effectively upregulates the tumorous PD-L1 level, promotes the response to anti-PD-1 immunotherapy,and prolongs the survival time of mice bearing HCC tumors. |
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| DC75284 |
GSK2983559-AM |
GSK2983559-AM, also known as GSK2983559 active metabolite, is an active metabolite of GSK2983559, also known as RIPK2-IN-1, is a potent and selective inhibitor of receptor interacting protein-2 (RIP2) kinase. |
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