| DC75541 |
Ulixertinib HCl |
Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase. Downmodulation of ERK protein kinase activity inhibits VEGF secretion by human myeloma cells and myeloma-induced angiogenesis. Upon oral administration, BVD-523 inhibits both ERK 1 and 2, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is often upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival. |
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| DC75542 |
LP-471756 |
LP-471756 is antagonist of GPR139. |
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| DC75543 |
Mozavaptan free base |
Mozavaptan, also known as OPC 31260, is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors. |
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| DC75544 |
OTS514 HCl |
OTS514 is a potent TOPK (T-LAK cell-originated protein kinase) inhibitor. OTS514 exhibits growth suppressive effect on small cell lung cancer. TS514 effectively suppressed growth of SCLC cell lines (IC50 ; 0.4 ~ 42.6 nM) and led to their apoptotic cell death. Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity, which was involved in stemness of CSC. Furthermore, OTS514 treatment reduced CD90-positive SCLC cells and showed higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells. |
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| DC75545 |
Pyruvate sodium |
Sodium pyruvate is an antioxidant potentially for the treatment of chronic obstructive pulmonary disease. |
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| DC75546 |
KN-92 phosphate |
KN-92 is an inactive analog of the CaM kinase II inhibitor KN 93. |
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| DC75547 |
Dexamethasone phosphate disodium |
Dexamethasone phosphate disodium is a water-soluble form of the synthetic glucocorticoid dexamethasone. |
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| DC75548 |
H-89 Dihydrochloride |
H-89 is a specific adenylyl cyclase inhibitor (DDA) and a cyclic AMP-dependent protein kinase inhibitor. H-89 blocks the action of equine growth hormone on in vitro maturation of equine oocytes. H-89 decreases the gain of excitation-contraction coupling and attenuates calcium sparks in the absence of beta-adrenergic stimulation. H-89 potentiates adipogenesis in 3T3-L1 cells by activating insulin signaling independently of protein kinase A. |
|
| DC75549 |
KN-93 free base |
KN-93 free base is a CaMKII inhibitor. KN-93 suppresses ventricular arrhythmia induced by LQT2 without decreasing TDR. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. KN-93 ameliorates levodopa-induced dyskinesia in a rat model of Parkinson's disease. KN-93 protects rat cerebral cortical neurons from N-methyl-D-aspartic acid-induced injury. |
|
| DC75550 |
Siramesine free base |
Siramesine, also known as Lu-28-179, is a potent sigma-2 receptor agonist. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Siramesine involves lysosomal leakage and oxidative stress. |
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| DC75551 |
AR-M1000390 HCl |
AR-M1000390, also known as ARM-390, is a nonpeptidic δ receptor selective agonist. |
|
| DC75552 |
Topovale |
Topovale, also known as ARC-111, is a potent topoisomerase I inhibitor. ARC-111 inhibits hypoxia-mediated hypoxia-inducible factor-1alpha accumulation. ,ARC-111 exhibited low nM cytotoxicity against a panel of cancer cells. ARC-111 cytotoxicity as well as ARC-111-induced apoptosis was reduced >100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells. |
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| DC75553 |
NSC-632839 hydrochloride |
NSC 632839 is an Inhibitor of ubiquitin isopeptidase activity. |
|
| DC75554 |
HOE 33342 trihydrochlorde |
HOE 33342, also known as Hoechst 33342, HO342, is a Benzimidazole fluorescent dye and a Cell permeable fluorescent DNA stain; binds minor groove of AT-rich regions. HOE 33342 trihydrochlorde is used to quantify DNA in viable cells. |
|
| DC75555 |
Orteronel (racemic) |
Orteronel (racemic) is a mixture of S-Orteronel and R-Orteronel isomers. Orteronel, aslo known as TAK-700, is an orally bioavailable non-steroidal androgen synthesis inhibitor of steroid 17alpha-monooxygenase (17,20 lyase) with potential antiandrogen activity. TAK-700 binds to and inhibits the steroid 17alpha-monooxygenase in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells. |
|
| DC75556 |
Tebanicline HCl |
Tebanicline, also known as ABT-594 and Ebanicline, a potent synthetic nicotinic (non-opioid) analgesic drug developed by Abbott. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine, which is some 200x stronger than morphine as an analgesic but produces extremely dangerous toxic side effects. Like epibatidine, tebanicline showed potent analgesic activity against neuropathic pain in both animal and human trials, but with far less toxicity than its parent compound. It acts as a partial agonist at neuronal nicotinic acetylcholine receptors, binding to both the α3β4 and the α4β2 subtypes. |
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| DC75557 |
Bisbenzimide HCl |
Bisbenzimide, also known as Pibenzimol, Hoechst 33258, is a cell-permeable, benzimidazole dye that binds to the minor groove of double stranded DNA with preference for adenine and thymine-rich sequences. |
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| DC75558 |
AH6809 |
AH6809 is a DP/EP prostanoid receptor antagonist. |
|
| DC75559 |
Tinoridine HCl |
Tinoridine, also known as Y-3642, is a non-steroidal anti-inflammatory drug. Tinoridine, at concentrations from 5 microM up to 100 microM, produced a concentration-dependent inhibition on the simultaneous increases in lipid peroxide formation and renin release induced by 50 microM ascorbic acid in the renin granule fraction. On the other hand, indomethacin, hydrocortisone and prednisolone, which had no ability to inhibit the lipid peroxidation in the renin granule fraction, did not influence the release of renin from the granules. These results suggest that tinoridine suppresses renin release by inhibiting the oxidative disintegration of membranes of renin granules. |
|
| DC75560 |
AC-90179 HCl |
AC-90179 is a high selective 5-hydroxytryptamine2A receptor inverse agonist. It is an atypical antipsychotic pharmaceutical. It has been shown to alleviate hallucinogen-induced vasocontriction and possible other harmful physical symptoms. |
|
| DC75561 |
Pirmenol |
Pirmenol is an antiarrhythmic agent. Pirmenol inhibits muscarinic acetylcholine receptor-operated K+ current in the guinea pig heart. Pirmenol is active in a variety of experimental arrhythmic models of diverse etiology and has a favorable therapeutic index compared with other class I agents. Pirmenol is highly efficacious whether the arrhythmias were atrial or ventricular in origin, chemically, mechanically or electrically induced or of the automaticity or reentrant types. |
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| DC75562 |
P552-02 free base |
P552-02, also known as KM-003, PS 552-02, or 552-02, is a sodium channel blocker potentially for the treatment of cystic fibrosis. |
|
| DC75563 |
Sulopenem |
Sulopenem, also known as CP-70429, is a potent beta-lactamase inhibitor.Sulopenem showed potent antibacterial activity against gram-positive and gram-negative bacteria except Pseudomonas aeruginosa and Xanthomonas maltophilia. CP-70,429 was stable to various types of beta-lactamases except for the enzyme from X. maltophilia and was 16- to 128-fold more active than the other compounds against beta-lactamase-producing strains of Enterobacter cloacae and Citrobacter freundii. |
|
| DC75564 |
Lys05 trihydrochloride |
Lys05, or Lys01 trihydrochloride, is a potent, water soluble lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ. Lys05 produced more potent antitumor activity as a single agent both in vitro and in vivo in multiple human cancer cell lines and xenograft models compared with HCQ. Lys05 is therefore a new lysosomal autophagy inhibitor that has potential to be developed further into a drug for cancer and other medical applications. |
|
| DC75565 |
STO-609 free base |
STO-609 is a specific inhibitor of the Ca(2+)/calmodulin-dependent protein kinase kinase. STO-609 inhibits the activities of recombinant CaM-KK alpha and CaM-KK beta isoforms, with K(i) values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 is highly selective for CaM-KK without any significant effect on the downstream CaM kinases (CaM-KI and -IV), and the IC(50) value of the compound against CaM-KII is approximately 10 microg/ml. STO-609 is a selective and cell-permeable inhibitor of CaM-KK and that it may be a useful tool for evaluating the physiological significance of the CaM-KK-mediated pathway in vivo as well as in vitro. |
|
| DC75566 |
Vonoprazan free base |
Vonoprazan is a novel potassium-competitive acid blocker. Vonoprazan is a first-in-class potassium-competitive acid blocker. It was approved in the Japanese market in February 2015. Vonoprazan can be used for the treatment of gastroduodenal ulcer (including some drug-induced peptic ulcers) and reflux esophagitis, and can be combined with antibiotics for the eradication of Helicobacter pylori. |
|
| DC75567 |
Nifenalol HCl |
Nifenalol, also known as INPEA, is a new beta-adrenergic receptor antagonist. |
|
| DC75568 |
Pipequaline HCl |
Pipequaline, also known as PK-8165, is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic. Pipequaline acts as a non-selective GABAA receptor partial agonist. While its profile of anxiolytic effects without sedation would appear to have potential medical applications, pipequaline has never been developed for medical use and is currently only used in scientific research. |
|
| DC75569 |
NVP-VID-400 |
NVP-VID-400, also known as SDZ285-428, is CYP24A1 inhibitor. |
|
| DC75570 |
Piperoxan HCl |
Piperoxan, also known as benodaine, is a drug which was the very first antihistamine to be discovered. This compound, derived from benzodioxan, was prepared in the early 1930s by Daniel Bovet and Ernest Fourneau at the Pasteur Institute in France. Formerly investigated by Fourneau as an α-adrenergic-blocking agent, they demonstrated that it also antagonized histamine-induced bronchospasm in guinea pigs. |
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