DC74695 |
AFN-1252 |
AFN-1252, also known as AFN-12520000; API-1252; Debio-1452, is FASII Inhibitor which is potentially for the treatment of acute bacterial skin. AFN-1252 exhibits typical MIC(90) values of ≤0·015 μg/ml against diverse clinical isolates of S. aureus, oral absorption, long elimination half-live and efficacy in animal models. AFN-1252 efficiently blocked daptomycin-induced phospholipid decoy production, even in the case of isolates resistant to AFN-1252, which prevented the inactivation of daptomycin and resulted in sustained bacterial killing. In turn, daptomycin prevented the fatty acid-dependent emergence of AFN-1252-resistant isolates in vitro |
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DC74696 |
Bisaramil HCl |
Bisaramil, also known as NK-1556 and RGH-2957, is a calcium channel antagonist and sodium channel antagonist potentially for the treatment of arrhythmia. |
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DC74697 |
Ribociclib HCl |
Ribociclib hydrochloride is an potent and orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. Ribociclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. 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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DC74698 |
RGB-286638 free base |
RGB-286638 is a multitargeted cyclin-dependent kinase inhibitor. RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. GB-286638 treatment resulted in MM cytotoxicity in vitro associated with inhibition of MM tumor growth and prolonged survival in vivo. RGB-286638 displayed caspase-dependent apoptosis in both wt-p53 and mutant-p53 cells that was closely associated with the downregulation of RNA polymerase II phosphorylation and inhibition of transcription. RGB-286638 triggered p53 accumulation via nucleolar stress and loss of Mdm2, accompanied by induction of p53 DNA-binding activity. |
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DC74699 |
Olodanrigan free acid |
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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DC74700 |
Valomaciclovir stearate |
Valomaciclovir stearate (A-174606.0; ABT-606; EPB-348; MIV-606; RP-606) is a DNA polymerase inhibitor potentially for treatment of acute herpes zoster and EB virus infection. Valomaciclovir stearate is an orally available and a prodrug of Valomaciclovir with broad-spectrum antiviral activity against a variety of important herpesviruses, including Epstein-Barr virus, or EBV (the first virus to be directly associated with human cancer), varicella zoster virus, or herpes zoster (cause of shingles), and herpes simplex virus 1 and 2. |
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DC74701 |
Doripenem Monohydrate |
Doripenem Monohydrate, also known as S-4661 and Finibax, is a beta-lactam class drug used for bacterial infections with ultra-broad antibiotic spectrum. Doripenem Monohydrate is used commonly for the treatment of complicated intra-abdominal infections and complicated urinary tract infections. |
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DC74702 |
Tyramide alkyne |
Tyramide alkyne is an alternative labeling substrate that can be coupled to detection or enrichment moieties via a Copper-catalyzed Azide/Alkyne Cycloaddition (CuAAC) “click” reaction. |
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DC74703 |
SCH 23390 HCl |
SCH 23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). SCH 23390 is also an agonist at 5-HT1C and 5-HT2C receptors in vitro (Ki values are 6.3 nM and 9.3 nM respectively). |
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DC74704 |
MSNBA |
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. |
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DC74705 |
MK-0941 mesylate |
MK-0941 mesylate is a glucokinase activator (GKA) potentially for the treatment of type 2 diabetes. MK-0941 led to improvements in glycemic control that were not sustained. MK-0941 was associated with an increased incidence of hypoglycemia and elevations in triglycerides and blood. |
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DC74706 |
Trans-crocetin sodium |
Trans-crocetin sodium, also known as Transcrocetinate sodium or Sodium crocetinate, is potentially for the treatment of glioblastoma. Trans-crocetin improves amyloid-β degradation in monocytes from Alzheimer's Disease patients. trans-crocetin inhibit glutamatergic synaptic transmission in rat cortical brain slices. Crocetin inhibits invasiveness of MDA-MB-231 breast cancer cells via downregulation of matrix metalloproteinases. |
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DC74707 |
BI-135585 |
BI-135585 is a potent and selective 11β-HSD1 inhibitor. BI 135585 was safe and well tolerated over 14 days and can be dosed once daily. |
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DC74708 |
LW3 |
LW3 is a potent antifungal agent. |
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DC74709 |
RS5517 |
RS5517 is a specific PDZ1-domain antagonist of NHERF1. |
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DC74710 |
Z26395438 |
Z26395438 (compound 1) is a potent Sirtuin-1 inhibitor. |
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DC74712 |
CZL55 |
CZL55 is a caspase-1 inhibitor. CZL55 can be used for the research of febrile seizures (FS) |
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DC74713 |
Brepocitinib tosylate |
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. |
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DC74714 |
RIG012 |
RIG012 is a potent RIG-I inhibitor. It inhibits IFN-β and ISG hRsad2 expression. |
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DC74715 |
Ajmaline |
Ajmaline, also known as Gilurytmal and Ritmos, is a sodium channel blocker used to treat arrhythmia. Ajmaline is also often used to bring out typical findings of ST elevations in patients suspected of having Brugada syndrome. |
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DC74716 |
Defactinib HCl |
Defactinib, also known as VS-6063 and PF04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. Defactinib inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including those involving RAS/MEK/ERK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation, survival, and tumor angiogenesis. |
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DC74717 |
Eg5-IN-1 |
Eg5-IN-1 (compound 6c) is a potent kinesin family motor protein (Eg5) inhibitor |
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DC74718 |
WAY-615145 |
WAY-615145 is a glucokinase activator. |
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DC74719 |
Bifemelane HCl |
Bifemelane, also known as MCI-2016, is Antidepressant MAO inhibitor used to treat cerebral infarction and Alzheimer's disease. At concentrations of 10 - 30 microM, Bifemelane induced a slow onset and small increase in the [Ca2+]i, while at higher concentrations (100 - 300 microM), it induced a rapid transient increase in the [Ca2+]i during administration and a second large increase was seen during drug washout. |
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DC74720 |
Carfecillin Sodium |
Carfecillin Sodium, also known as Carbenicillin Phenyl Sodium and BRL-3475, is the phenyl ester of Carbenicillin that, upon oral administration, is broken down in the intestinal mucosa to the active antibacterial. It is used for urinary tract infections. |
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DC74721 |
GPAT-IN-1 |
GPAT-IN-1 is a glycerol-3-phosphate acyltransferase (GPAT) inhibitor |
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DC74722 |
MAO-B-IN-19 |
MAO-B-IN-19 is a selective MAO-B inhibitor with an IC50 of 0.67 μM. |
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DC74723 |
PNU-282987 free base |
PNU-282987 is a highly selective α7 nAChR agonist (Ki = 26 nM) displaying negligible blockade of α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM). PNU-282987 is inactive against a panel of 32 receptors at 1 μM, except 5-HT3 receptors (Ki = 930 nM). |
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DC74724 |
Ruboxistaurin HCl |
Ruboxistaurin, also known as LY-333531, is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt. |
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DC74725 |
Metformin HCl |
Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. Metformin exerts an anorexiant effect, decreasing caloric intake. Metformin decreases gluconeogenesis (glucose production) in the liver. Metformin inhibits basal secretion from the pituitary gland of growth hormone, adrenocorticotropic hormone, follicle stimulating hormone, and expression of proopiomelanocortin, which in part accounts for its insulin-sensitizing effect with multiple actions on tissues including the liver, skeletal muscle, endothelium, adipose tissue, and the ovaries. |
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