| DC74679 |
Sephin1 |
Sephin1 is a selective inhibitor of a holophosphatase. Sephin1 safely and selectively inhibited a regulatory subunit of protein phosphatase 1 in vivo. Sephin1 selectively bound and inhibited the stress-induced PPP1R15A, but not the related and constitutive PPP1R15B, to prolong the benefit of an adaptive phospho-signaling pathway, protecting cells from otherwise lethal protein misfolding stress. In vivo, Sephin1 safely prevented the motor, morphological, and molecular defects of two otherwise unrelated protein-misfolding diseases in mice, Charcot-Marie-Tooth 1B, and amyotrophic lateral sclerosis. Sephin1may have potential to safely prevent two protein misfolding diseases. |
|
| DC74680 |
trans-ISRIB |
trans-ISRIB is an Integrated Stress Response Inhibitor. trans-ISRIB inhibits the eIF2α phosphorylation-mediated unfolded protein response following induction of ER stress (IC50 = 5 nM in a cell-reporter assay). ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly. ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly |
|
| DC74681 |
MRT68921 free base |
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively). |
|
| DC74682 |
Z16078526 |
Z16078526 induces endogenous Ucp1 expression, promotes p38 MAPK phosphorylation and lipolysis. |
|
| DC74683 |
KPT-9274 |
Padnarsertib, also known as KPT-9274 and PAK4-IN-1, is a potent, selective and dual PAK4/NAMPT inhibitor. KPT-9274 interferences with PAK4/NAMPT signaling pathways, which results in reduction of G2-M transit as well as induction of apoptosis and decrease in cell invasion and migration in several human RCC cell lines. Mechanistic studies demonstrate that inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc. KPT-9274 demonstrated the expected on-target effects in this mouse model. KPT-9274 is being evaluated in a phase I human clinical trial in solid tumors and lymphomas, which will allow this data to be rapidly translated into the clinic for the treatment of RCC. |
|
| DC74684 |
ZH8667 |
ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist. |
|
| DC74685 |
HFY-4A |
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. |
|
| DC74686 |
GW0193 |
GW0193 is also named as 7-(2-(oxiran-2-yl)ethoxy)-2H-chromen-2-one. It is a coumarin derivative. |
|
| DC74688 |
Foslinanib sodium |
Foslinanib, also known as TRX-818, CVM-1118, is an orally bioavailable agent with potential antineoplastic and anti-vasculogenic mimicry (VM) activities. Although the exact multiple mechanisms of action through which this agent exerts its effects have yet to be fully elucidated, TRX-818, upon oral administration appears to induce cancer cell apoptosis and inhibits cancer cell proliferation. This agent also prevents tumor cell VM by blocking the formation of vasculogenic-like tubular structures through an as of yet undetermined mechanism of action. |
|
| DC74689 |
Ubenimex |
Ubenimex, also known as NK 421 and Bestatin, is a CD13 inhibitor. Ubenimex attenuates acquired sorafenib resistance in renal cell carcinoma by inhibiting Akt signaling in a lipophagy associated mechanism. Ubenimex synergistically enhances the effects of anticancer drugs in hepatocellular carcinoma. Ubenimex inhibits cell proliferation, migration and invasion by inhibiting the expression of APN and inducing autophagic cell death in prostate cancer cells. |
|
| DC74690 |
WAY-278705 |
WAY-278705 is a phosphoinositide 3-kinase (PI3 kinase) modulator. |
|
| DC74691 |
WAY-354896 |
WAY-354896 is a Dual activator of Protein Kinase R (PKR) and Protein Kinase R-Like Kinase (PERK). |
|
| DC74692 |
Nafamostat mesylate |
Nafamostat, also known as FUT-175, is a serine protease inhibitor and an anticoagulant. Nafamostat promotes endothelium-dependent vasorelaxation via the Akt-eNOS dependent pathway. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat Attenuates Ischemia-Reperfusion-Induced Renal Injury. Nafamostat protects against acute cerebral ischemia via blood-brain barrier protection. Nafamostat Inhibits TNF-α-Induced Vascular Endothelial Cell Dysfunction by Inhibiting Reactive Oxygen Species Production. Researchers have identified the drug as a potential therapy for COVID-19,[ with clinical trials in Japan possibly set to begin in March 2020. |
|
| DC74693 |
WAY-301464 |
WAY-301464 is a Pim-1 inhibitor. |
|
| DC74694 |
BIT225 |
BIT-225 is a NCp7 zinc finger inhibitor potentially for the treatment of HCV infection and HIV infection. BIT225 inhibits HIV-1 replication in myeloid dendritic cells. BIT225, inhibits bovine viral diarrhea virus in vitro and shows synergism with recombinant interferon-alpha-2b and nucleoside analogues. BIT225 against HIV-1 release from human macrophages. |
|
| 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 |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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). |
|
| DC74704 |
MSNBA |
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. |
|
| 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. |
|
