| DC75800 |
R1487 free base |
R-1487 is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. Pyruvate dehydrogenase (PDH) plays an important role in regulating carbohydrate oxidation in skeletal muscle. PDH is deactivated by a set of PDH kinases (PDK1, PDK2, PDK3, PDK4), with PDK2 and PDK4 being the most predominant isoforms in skeletal muscle. |
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| DC75801 |
Epicatechin gallate |
Epicatechin gallate (ECG) is a flavan-3-ol, a type of flavonoid, present in green tea. It is also reported in buckwheat and in grape. The tea component epicatechin gallate is being researched because in vitro experiments showed it can reverse methicillin resistance in bacteria like Staphylococcus aureus. If confirmed, this means the combined intake of a tea extract containing this component might also enhance the effectiveness of methicillin treatment against some resistant bacteria in vivo. |
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| DC75802 |
GSK3368715 free base |
GSK3368715, aslo known as EPZ019997, is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models. Inhibition of PRMT5, the predominant type II PRMT, produces synergistic cancer cell growth inhibition when combined with GSK3368715. Interestingly, deletion of the methylthioadenosine phosphorylase gene (MTAP) results in accumulation of the metabolite 2-methylthioadenosine, an endogenous inhibitor of PRMT5, and correlates with sensitivity to GSK3368715 in cell lines. |
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| DC75803 |
Danicopan free base |
Danicopan, aslo known as ACH-4471 and ACH-0144471, is a highly potent, orally active Factor D inhibitor. Danicopan selectively block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria and atypical hemolytic uremic syndrome. |
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| DC75804 |
PLX5622 free base |
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor. PLX5622 has been shown to eliminate microglia from the brain, which can be sustained in wild-type and the Alzheimer's disease model mice (3xTg-AD model). In the AD model PLX5622 prevents microglial association with amyloid β plaques and improves cognition. |
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| DC75805 |
BAY-1125976 |
BAY-1125976 is a potent and selective allosteric AKT1/2 inhibitor. BAY-1125976 exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY 1125976 potently and selectively inhibited the activity of full-length AKT1 and AKT2 by binding into an allosteric binding pocket formed by kinase and PH domain. In vitro, BAY 1125976 inhibited cell proliferation in a broad panel of human cancer cell lines. BAY 1125976 exhibited strong in vivo efficacy in both cell line and patient-derived xenograft models such as the KPL4 breast cancer model (PIK3CAH1074R mutant), the MCF7 and HBCx-2 breast cancer models and the AKTE17K mutant driven prostate cancer (LAPC-4) and anal cancer (AXF 984) models. |
|
| DC75806 |
Mobocertinib free base |
Mobocertinib, also known as TAK-788 and AP32788, is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. TAK-788 exhibits antitumor activity in pts with EGFR exon 20 insertions with an AE profile consistent with other EGFR TKIs. |
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| DC75807 |
Vortioxetine HBr |
Vortioxetine, also known as Lu AA21004, is an atypical antidepressant, and was approved in 2013 by the U.S. FDA for the treatment of major depressive disorder (MDD) in adults. Vortioxetine is a so-called "serotonin modulator and stimulator." It has been shown to possess the following pharmacological actions: Serotonin transporter (SERT) blocker (i.e. serotonin reuptake inhibitor (SRI)) — Ki (binding affinity) = 1.6 nM, IC50 = 5.4 nM; Norepinephrine transporter (NET) blocker — Ki = 113 nM; 5-HT1A receptor high-efficacy partial agonist/near-full agonist — Ki = 15 nM, IA = 80%; 5-HT1B receptor partial agonist — Ki = 33 nM; 5-HT1D receptor antagonist — Ki = 54 nM; 5-HT3A receptor antagonist — Ki = 3.7 nM; 5-HT7 receptor antagonist — Ki = 19 nM. |
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| DC75808 |
Cinacalcet |
Cinacalcet (INN) is a drug that acts as a calcimimetic (i.e. it mimics the action of calcium on tissues) by allosteric activation of the calcium-sensing receptor that is expressed in various human organ tissues. It is sold by Amgen under the trade name Sensipar in North America and Australia and as Mimpara in Europe. Cinacalcet is used to treat secondary hyperparathyroidism (elevated parathyroid hormone levels), a consequence of having end-stage renal disease. Cinacalcet is also indicated for the treatment of hypercalcemia in patients with parathyroid carcinoma. |
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| DC75809 |
Tinostamustine free base |
Tinostamustine, also known as EDO-S101, is an alkylatlng histone-deacetylase inhibitor (HDACi) fusion molecule. EDO-S101 is a functional pan-histone-deacetylase inhibitor and is assumed to potentiate the alkylating activity of the compound and/or may help to overcome resistance to other therapeutic agents. |
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| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC75821 |
Dioctyl decanedioate new |
Dioctyl decanedioate is a biochemical. |
|
| DC75822 |
AT-9283 L-lactate |
AT-9283 L-lactate is an aurora kinase inhibitor. |
|
| 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. |
|
| 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. |
|
| 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. |
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