| DC75810 |
PJ-34 HCl |
PJ-34 is a novel and potent PARP-1 inhibitor with potential anticancer activity. PJ34 has a high affinity for PARP-1 (IC(50) = 20 nM). PJ-34 inhibits PARP-1 expression and ERK phosphorylation in glioma-conditioned brain microvascular endothelial cells. PJ-34 reduces mesenteric vascular injury induced by experimental cardiopulmonary bypass with cardiac arrest. PJ-34 reduce cell inflammation and damage that follow PARP-1 overexpression. PJ-34 negatively modulate proinflammatory commitment of human glioblastoma cells. |
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| DC75811 |
Linperlisib free base |
Linperlisib, also known as YY-20394 and PI3Kδ-IN-2, is a potent and selective PI3Kδ inhibitor. YY-20394 significantly inhibited primary tumor growth in immune-competent mice with 4T1 and CT26 tumors, as well as 4T1 lung metastasis with dose dependency. YY-20394 significantly inhibited T cell differentiation into Treg both in mouse splenocyte and in human primary CD4+ T cells, and was especially potent inhibiting their IL-10 secretion in vitro. |
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| DC75812 |
VHL-7526 TFA |
VHL-7526, also known as Protein degrader 1, is a protein degrader and is a small molecule ligand for VHL |
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| DC75813 |
Vonoprazan Fumarate |
Vonoprazan Fumarate, also known as TAK438, is a new medicine for treating acid-related diseases with a novel mechanism of action called potassium-competitive acid blockers (P-CABs) which competitively inhibits the binding of potassium ions to H+,K+-ATPase (also known as the proton pump) in the final step of gastric acid secretion in gastric parietal cells. TAKECAB provides a strong and sustained acid secretion inhibitory effect. |
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| DC75814 |
Tedizolid phosphate |
Tedizolid phosphate, also know as TR-701FA tedizolid, torezolid (trade name Sivextro), is an oxazolidinone drug being developed by Cubist Pharmaceuticals following acquisition of Trius Therapeutics (originator: Dong-A Pharmaceuticals) for complicated skin and skin-structure infections (cSSSIs), including those caused by methicillin-resistant Staphylococcus aureus (MRSA). Tedizolid has been approved by the FDA on June 20, 2014, for the treatment of MRSA skin infections. |
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| DC75815 |
Avanafil |
Avanafil is a PDE5 inhibitor approved for erectile dysfunction by FDA on April 27, 2012 and by EMA on June 21, 2013. Avanafil is known by the trademark names Stendra and Spedra and was developed by Vivus Inc. Avanafil acts by inhibiting a specific phosphodiesterase type 5 enzyme which is found in various body tissues, but primarily in the corpus cavernosum penis, as well as the retina. |
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| DC75816 |
Nisoxetine |
Nisoxetine is a potent inhibitor for norepinephrine uptake into rat brain synaptosomes and brain. |
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| DC75817 |
Ralmitaront HCl |
Ralmitaront, also known as WHO 11130, RO 6889450 and RG7906, is a neuroleptic. |
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| DC75818 |
TAS-115 mesylate |
TAS-115 is a c-MET Inhibitor. TAS-115 inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. TAS-115 is extremely selective and specific, at least in vitro. In in vivo studies, TAS-115 completely suppressed the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 induced marked tumor shrinkage and prolonged survival in MET-amplified human cancer-bearing mice. TAS-115 is a unique VEGFR/MET-targeted inhibitor with improved antitumor efficacy and decreased toxicity. |
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| DC75819 |
PEAQX sodium |
PEAQX, also known as NVP-AAM077; is a competitive antagonist at the NMDA receptor. Although originally described as 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors, more detailed studies of the Ki of PEAQX revealed it only shows a 5 fold difference in affinity for GluN1/GluN2A vs. GluN1/GluN2B receptors. It is also a potent anticonvulsant in animal tests. |
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| DC75820 |
Hydroxyfasudil HCl |
Hydroxyfasudil, aslo known as HA1100, is a cell-permeable hydroxylated metabolite of HA-1077, is a potent inhibitor of Rho-associated kinase (ROCK) (Ki = 150 nM). Hydroxyfasudil alleviates demyelination through the inhibition of MOG antibody and microglia activation in cuprizone mouse model. |
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| DC75821 |
Dioctyl decanedioate new |
Dioctyl decanedioate is a biochemical. |
|
| DC75822 |
AT-9283 L-lactate |
AT-9283 L-lactate is an aurora kinase inhibitor. |
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| DC75823 |
UNC-669 |
UNC-669 is a L3MBTL domain inhibitor. UNC669 specifically targets lethal 3 malignant brain tumour-like protein (L3MBTL) with an IC50 of 5 μM. |
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| DC75824 |
Simeprevir sodium |
Simeprevir, also known as TMC43, is a drug for the treatment and cure of hepatitis C. In the United States, simeprevir is approved by the Food and Drug Administration for use in combination with peginterferon-alfa and ribavirin for hepatitis C and hepatitis B. Simeprevir has been approved in Japan for the treatment of chronic hepatitis C infection, genotype 1. |
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| DC75825 |
PHA-767491 HCl |
PHA-767491, also known as CAY10572, is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. PHA-767491 in combination with 5-FU exhibited much stronger cytotoxicity and induced significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracted the 5-FU-induced phosphorylation of Chk1, a substrate of Cdc7; and decreased the expression of the anti-apoptotic protein myeloid leukemia cell 1, a downstream target of Cdk9. |
|
| DC75826 |
ZM323881 HCl |
ZM323881 is a potent and selective inhibitor of VEGF-R2 tyrosine kinase in vitro (IC(50) < 2 nM), compared with other receptor tyrosine kinases, including VEGF-R1 (IC(50) > 50 microM). ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC(50) = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro. |
|
| DC75827 |
Idalopirdine HCl |
Idalopirdine, also known as Lu AE58054 or Iladopirdine, is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia. It is in phase III clinical trials. Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. Lu AE58054 demonstrated >50-fold selectivity for more than 70 targets examined. Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. Lu AE58054 may be useful for the pharmacotherapy of cognitive dysfunction in disease states such as schizophrenia and Alzheimer's disease. |
|
| DC75828 |
SRT-1720 free base |
SRT-1720, also known as CAY10559 and is a drug developed by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in the body to the known SIRT1 activator resveratrol, but is 1000x more potent. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function. A study of SRT1720 conducted by the National Institute on Aging found that the drug may extend the lifespan of obese mice by 44% . |
|
| DC75829 |
Cefuroxime axetil |
Cefuroxime axetil is a second generation cephalosporin antibiotic with a broad spectrum activity against Gram positive and Gram negative bacteria. |
|
| DC75830 |
Brepocitinib free base |
Brepocitinib, also known as PF-06700841, is an inhibitor of JAK1 and TYK2 kinases for potential treatment of systemic lupus erythematosus and plaque psoriasis. PF-06700841 potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (HWB IC50 = 65 and 120 nM, respectively). PF-06700841 improves clinical symptoms of chronic plaque psoriasis by inhibition of proinflammatory cytokines that require TYK2 and Janus kinase 1 for signal transduction. |
|
| DC75831 |
Otenabant HCl |
Otenabant, also known as CP-945,598, is a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the treatment of obesity, but development for this application has been discontinued following the problems seen during clinical use of the similar drug rimonabant. (source: http://en.wikipedia.org/wiki/Otenabant). |
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| DC75832 |
Rilpivirine free base |
Rilpivirine is a pharmaceutical drug, developed by Tibotec, for the treatment of HIV infection. It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz. Rilpivirine entered phase III clinical trials in April 2008, and was approved for use in the United States in May 2011. A fixed-dose drug combining rilpivirine with emtricitabine and tenofovir, was approved by the U.S. Food and Drug Administration in August 2011 under the brand name Complera. |
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| DC75833 |
AGG-523 |
AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury. |
|
| DC75834 |
Topocecan free base |
Topotecan is a topoisomerase inhibitor. It is a synthetic, water-soluble analog of the natural chemical compound camptothecin. In physiological environments, topotecan is in equilibrium with its inactive carboxylate form. Topotecan's active lactone form intercalates between DNA bases in the topoisomerase-I cleavage complex. The binding of topotecan in the cleavage complex prevents topoisomerase-I from religating the nicked DNA strand after relieving the strain. This intercalation therefore traps the topoisomerase-I in the cleavage complex bound to the DNA. When the replication-fork collides with the trapped topoisomerase-I, DNA damage occurs. This disruption prevents DNA replication and ultimately leads to cell death. |
|
| DC75835 |
SB505124 |
SB505124: SB505124 is a selective inhibitor of transforming growth factor-β type I receptor (ALK5, ALK4 and ALK7) with potential anticancer activity. SB505124 selectively inhibits signaling from TGF-β and activin; does not inhibit other ALK family members. SB-505124 selectively and concentration-dependently inhibits ALK4-, ALK5-, and ALK 7-dependent activation of downstream cytoplasmic signal transducers, Smad2 and Smad3, and of TGF-beta-induced mitogen-activated protein kinase pathway components but does not alter ALK1, ALK2, ALK3 or ALK6-induced Smad signaling. |
|
| DC75836 |
Grazoprevir (MK5172) |
Grazoprevir, also known as MK5172, is a drug approved for the treatment of hepatitis C. It was developed by Merck and completed Phase III trials, following promising results in Phase II when used in combination with the NS5A replication complex inhibitor elbasvir, either with or without ribavirin.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. |
|
| DC75837 |
Salinomycin |
Salinomycin is an antibacterial and coccidiostat ionophore agent. Salinomycin suppresses T24 cells by regulating KDM1A and the unfolded protein response pathway. Salinomycin alleviates osteoarthritis progression via inhibiting Wnt/β-catenin signaling. Vitamin D3 and Salinomycin synergy in MCF-7 cells cause cell death via endoplasmic reticulum stress in monolayer and 3D cell culture. Salinomycin induces cell cycle arrest and apoptosis and modulates hepatic cytochrome P450 mRNA expression in HepG2/C3a cells. Salinomycin inhibits proliferation and induces apoptosis of human hepatocellular carcinoma cells in vitro and in vivo, |
|
| DC75838 |
CT-1812 free base |
CT-1812 is a first-in-class, orally available sigma-2/PGRMC1 antagonist (alpha beta oligomer receptor antagonist), is being developed by Cognition. sCT-1812 is a novel therapeutic candidate for Alzheimer's disease. |
|
| DC75839 |
Tenovin-6 HCl |
Tenovin-6, also known as Tnv-6, is a bioactive small molecule SIRT2 inhibitor with anti-neoplastic activity. Inhibition of the Sirtuin class of protein deacetylases with activation of p53 function is associated with the pro-apoptotic effects of Tnv-6 in many tumors. Tnv-6 causes non-genotoxic cytotoxicity, without adversely affecting human clonogenic hematopoietic progenitors in vitro, or murine hematopoiesis. Mechanistically, exposure of CLL cells to Tnv-6 did not induce cellular apoptosis or p53-pathway activity. Transcriptomic profiling identified a gene program influenced by Tnv-6 that included autophagy-lysosomal pathway genes. |
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