| 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. |
|
| 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. |
|
| 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. |
|
| DC74708 |
LW3 |
LW3 is a potent antifungal agent. |
|
| DC74709 |
RS5517 |
RS5517 is a specific PDZ1-domain antagonist of NHERF1. |
|
| DC74710 |
Z26395438 |
Z26395438 (compound 1) is a potent Sirtuin-1 inhibitor. |
|
| DC74711 |
Tasurgratinib |
Tasurgratinib, also known as E-7090, is a fibroblast growth factor receptor inhibitor potentially for the treatment of solid tumors. E-7090 is a selective inhibitor of the tyrosine kinase activities of FGFR1, -2, and -3. In kinetic analyses of the interaction between E7090 and FGFR1 tyrosine kinase, E7090 associated more rapidly with FGFR1 than did the type II FGFR1 inhibitor ponatinib, and E7090 dissociated more slowly from FGFR1, with a relatively longer residence time, than did the type I FGFR1 inhibitor AZD4547, suggesting that its kinetics are more similar to the type V inhibitors, such as lenvatinib. |
|
| DC74712 |
CZL55 |
CZL55 is a caspase-1 inhibitor. CZL55 can be used for the research of febrile seizures (FS) |
|
| 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. |
|
| DC74714 |
RIG012 |
RIG012 is a potent RIG-I inhibitor. It inhibits IFN-β and ISG hRsad2 expression. |
|
| 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. |
|
| 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. |
|
| DC74717 |
Eg5-IN-1 |
Eg5-IN-1 (compound 6c) is a potent kinesin family motor protein (Eg5) inhibitor |
|
| DC74718 |
WAY-615145 |
WAY-615145 is a glucokinase activator. |
|
| 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. |
|
| 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. |
|
| DC74721 |
GPAT-IN-1 |
GPAT-IN-1 is a glycerol-3-phosphate acyltransferase (GPAT) inhibitor |
|
| DC74722 |
MAO-B-IN-19 |
MAO-B-IN-19 is a selective MAO-B inhibitor with an IC50 of 0.67 μM. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| DC74726 |
Nintedanib esylate |
Nintedanib, also known as BIBF1120, is a potent inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology. Nintedanib esylate was approved in 2014 for the treatment of idiopathic pulmonary fibrosis (IPF). |
|
| DC74727 |
Nirogacestat free base |
Nirogacestat, also known as PF-03084014, is a potent and selective gamma secretase (GS) inhibitor with potential antitumor activity. PF-03084014 binds to GS, blocking proteolytic activation of Notch receptors. Nirogacestat enhances the Antitumor Effect of Docetaxel in Prostate Cancer. Nirogacestat enhances docetaxel-mediated tumor response and provides a rationale to explore GSIs as adjunct therapy in conjunction with docetaxel for men with CRPC (castration-resistant prostate cancer). |
|
| DC74728 |
Cardiogenol C HCl |
Cardiogenol C is a diaminopyrimidine compound that induces the differentiation of MHC- (myosin heavy chain) positive cardiomyocytes from embryonic stem cells with an EC50 value of 0.1 µM. Cardiogenol C upregulates cardiac markers and induces cardiac functional properties in lineage-committed progenitor cells. Cardiogenol C can induce Mouse Hair Bulge Progenitor Cells to Transdifferentiate into Cardiomyocyte-like Cells. |
|
| DC74729 |
Rezatapopt |
Rezatapopt, also known as PC14586, is p53 Y220C reactivator that binds selectively to p53 Y220C mutant protein and restores the p53 wildtype conformation and transcriptional activity, resulting in potent preclinical antitumor activity. PC14586 was structurally designed to bind tightly to a crevice within the mutant protein (KD~2.5 nM). PC14586 was shown to stabilize the Y220C mutant in the wild type conformation, resulting in reactivation of p53 transcriptional activity and subsequent expression of its target proteins (e.g. p21, MDM2, Bax, PUMA). The reactivation of p53 function is highly selective to Y220C mutant cells and results in arrest of the cell cycle in vitro (IC50 ~0.230-1.8 μM). In nude mice bearing Y220C mutant NUGC3 gastric cancer xenograft tumors, oral administration of PC14586 results in a dose responsive anti-tumor effect. In human xenografts, PC14586 was shown to convert Y220C mutant to the wildtype conformation, resulting in activation of p53 transcription. |
|
| DC74730 |
Pimicotinib |
Pimicotinib, also known as ABSK021, is a tyrosine kinase inhibitor and antineoplastic. It is a small molecule CSF-1R inhibitor that is orally available. Pimicotinib has antitumor activity and a solid white to off-white appearance. Its formula is C22H24N6O3 and its CAS number is 2253123-16-7. |
|
| DC74731 |
Xanthine oxidoreductase-IN-5 |
Xanthine oxidoreductase-IN-5 is an orally active xanthine oxidoreductase (XOR) inhibitor |
|
| DC74732 |
BLK degrader1 |
BLK degrader 1 (compound 9) is a selective degrader of B-lymphoid tyrosine kinase (BLK). |
|
| DC74733 |
Orziloben |
Orziloben is a medium chain fatty acid (MCFA) analogue. |
|
| DC74734 |
Telotristat ethyl |
Telotristat ethyl, also known as LX 1032 or LX 1606, 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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