| DC74661 |
HEC96719 |
HEC96719 is a tricyclic farnesoid X receptor agonist (FXR agonist) for treatment of non-alcoholic steatohepatitis. HEC96719 exhibits excellent potency superior to GW4064 and obeticholic acid in in vitro and in vivo assays of FXR activation. It also shows higher FXR selectivity and more favorable tissue distribution dominantly in liver and intestine. Preclinical data on pharmacokinetic properties, efficacy, and safety profiles overall indicate that HEC96719 is a promising drug candidate for NASH treatment. |
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| DC74662 |
CHK1-IN-3 |
CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM. |
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| DC74663 |
DOTA |
DOTA is an azamacrocyle in which four nitrogen atoms at positions 1, 4, 7 and 10 of a twelve-membered ring are each substituted with a carboxymethyl group. It has a role as a chelator and a copper chelator. It derives from a hydride of a 1,4,7,10-tetraazacyclododecane. It is a a metal chelate in use in medical diagnostics. |
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| DC74664 |
BAL-0028 |
BAL-0028 (Compound 3) is a NLRP3 activation inhibitor with a IC50 value of 25 nM. |
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| DC74665 |
Protoporphyrin IX |
Protoporphyrin IX is an organic compound, classified as a porphyrin, that plays an important role in living organisms as a precursor to other critical compounds like heme (hemoglobin) and chlorophyll. It is a deeply colored solid that is not soluble in water. The name is often abbreviated as PPIX. Protoporphyrin IX florescence from 5-ALA administration is used in fluorescent-guided surgery of glioblastoma. Protoporphyrin IX is an important precursor for synthesis of verteporfin, an approved photosensitizer. |
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| DC74666 |
WJ-39 |
WJ-39 is an orally active aldose reductase (AR) inhibitor. |
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| DC74667 |
Hispolon |
Hispolon is a phenol originally isolated from I. hispidus that has diverse biological activities. |
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| DC74668 |
LMP744 free base |
LMP744, also known as Mj-III-65 and NSC-706744, is a DNA intercalator and topoisomerase inhibitor with antitumor activity. LMP744 produces persistent topoisomerase I cleavage complexes and overcome multidrug resistance. Consistent with Top1 poisoning, protein-linked DNA breaks were detected in cells treated with LMP744 at nanomolar concentrations. Studies in human cells in culture found LMP744 to be cytotoxic. Furthermore, limited cross-resistance was observed in camptothecin-resistant cell lines. LMP744 also exhibits antitumor activity in mouse tumor xenografts. |
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| DC74669 |
Rilpivirine HCl |
Rilpivirine, also known as TMC278, 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 was approved for use in the United States in May 2011. |
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| DC74670 |
JTE-607 HCl |
JTE-607, also known as TO-207, is a cytokine production inhibitor potentially for the treatment of systemic inflammatory response, and induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. |
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| DC74671 |
CTP518 |
CTP518 is a HIV protease inhibitor and a deuterated Atazanivir derivative. |
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| DC74672 |
ZK-756326 dihydrochloride |
ZK-756326 is a potent, selective and non-peptide CCR8 chemokine receptor agonist. ZK 756326 inhibited the binding of the CCR8 ligand I-309 (CCL1), with an IC(50) value of 1.8 muM. ZK 756326 was a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. |
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| DC74673 |
PRE-084 HCl |
PRE 084 is a high affinity selective sigma 1 agonist. |
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| DC74674 |
PF-05089771 |
PF-05089771 is a Selective Nav1.7 Inhibitor (IC50 = 11 nM) that interacts with the voltage-sensor domain (VSD) of domain IV. PF-05089771 exhibits a slow onset of block that is depolarization and concentration dependent, with a similarly slow recovery from block. Human hereditary gain- or loss-of-pain disorders have demonstrated an essential role of Nav1.7 sodium channels in the sensation of pain, thus making this channel an attractive target for new pain therapies. |
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| DC74675 |
Eliglustat tartrate |
Eliglustat, also known as Genz-112638, is is a potent and selective glucosylceramide synthase inhibitor. Eliglustat was approved for Gaucher's disease. Commonly used as the tartrate salt, the compound is believed to work by inhibition of glucosylceramide synthase. According to an article in Journal of the American Medical Association the oral substrate reduction therapy resulted in "significant improvements in spleen volume, hemoglobin level, liver volume, and platelet count" in untreated adults with Gaucher disease Type 1. |
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| DC74676 |
PD153035 HCl |
PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2). |
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| DC74677 |
Pardoprunox free base |
Pardoprunox, also known as SLV-308; DU-126891; SME-308, is dopamine D2/5-HT1A receptor agonist potentially for the treatment of Parkinson's disease. It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned. Pardoprunox acts as a D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%). It also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. |
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| DC74678 |
AR-R17779 HCl |
AR-R17779 is a selective alpha7 nicotinic agonist (Ki values are 190 and 16000 nM for rat α7 and α4β2 receptors respectively). AR-R17779 improves learning and memory in rats. Treatment with AR-R17779 significantly reduced atherosclerotic plaque area and improved survival of mice. Treatment with AR-R17779 also suppressed abdominal aortic aneurysm formation. Quantitative RT-PCR of the aorta revealed that mRNA expression levels of interleukin-1β, interleukin-6 and NOX2 were significantly decreased in AR-R17779-treated mice compared with Ang II+HFD mice. AR-R17779 treatment also reduced blood pressure and serum lipid levels. |
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| 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. |
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| 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 |
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| DC74681 |
MRT68921 free base |
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively). |
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| DC74682 |
Z16078526 |
Z16078526 induces endogenous Ucp1 expression, promotes p38 MAPK phosphorylation and lipolysis. |
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| 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. |
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| DC74684 |
ZH8667 |
ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist. |
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| DC74685 |
HFY-4A |
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. |
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| DC74686 |
GW0193 |
GW0193 is also named as 7-(2-(oxiran-2-yl)ethoxy)-2H-chromen-2-one. It is a coumarin derivative. |
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| DC74687 |
ND-011992 |
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. |
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| 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. |
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| 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. |
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| DC74690 |
WAY-278705 |
WAY-278705 is a phosphoinositide 3-kinase (PI3 kinase) modulator. |
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