| DC75530 |
Givinostat HCl |
Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis.ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro. ITF2357 decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro. |
|
| DC75531 |
BAY-K-8644 |
BAY-K-8644, also known as BAYK 8644 andBAY-K-8644, is a L-type Ca2+ channel activator (EC50 = 17.3 nM). BAYK 8644 has positive inotropic, vasoconstrictive and behavioral effects in vivo. |
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| DC75532 |
PMPA free acid |
PMPA is a NAALADase inhibitor. PMPA increases threshold for electroconvulsions and enhances the antiseizure action of valproate against maximal electroshock-induced seizures in mice. Inhibition of NAALADase by 2-PMPA attenuates cocaine-induced relapse in rats: a NAAG-mGluR2/3-mediated mechanism. PMPA attenuates magnetic resonance BOLD signals in brain of anesthetized mice: evidence of a link between neuron NAAG release and hyperemia. |
|
| DC75533 |
AZD8542 |
AZD8542 is an antagonist of Smoothened (SMO), with potential as an oncology therapeutic. It is a novel Hedgehog (Hh) pathway antagonist on tumor progression with an emphasis on the role of the stroma compartment. |
|
| DC75534 |
AZD6703 free base |
AZD6703 is a potent, selective and reversible orally bioavailable inhibitor of p38 mitogen-activated protein kinase 14 (MAPK14). |
|
| DC75535 |
Importazole HCl |
Importazole is a small molecule inhibitor of the transport receptor importin-β. Importazole specifically inhibits the function of importin-β, likely by altering its interaction with RanGTP. Importazole is a valuable tool to evaluate the function of the importin-β/RanGTP pathway at specific stages during the cell cycle. |
|
| DC75536 |
Pibrentasvir |
Pibrentasvir, also known as ABT-530, is a protease inhibitor potentially for the treatment of HCV infection. |
|
| DC75537 |
AZD-1386 |
AZD1386 is an orally available antagonist of the transient receptor potential channel TRPV1. Note: Structure of this product was from NIH/NCATS web page: https://drugs.ncats.io/drug/210323T9CP and drugbank web page: https://go.drugbank.com/drugs/DB15333. |
|
| DC75538 |
LY2365109 HCl |
LY2365109 is a Potent and selective glycine transporter 1 (GlyT1) inhibitor (IC50 values are 15.8 and > 30 000 nM at GlyT1 and GlyT2 respectively). LY2365109 increased cerebrospinal fluid levels of glycine and potentiated NMDA-induced increases in dialysate levels of neurotransmitters in the prefrontal cortex (PFC) and the striatum. GlyT1 overexpression in the epileptic brain constitutes a new target for therapeutic intervention, and that GlyT1 inhibitors constitute a new class of antiictogenic drugs. |
|
| DC75539 |
AZD6538 |
AZD6538 is a novel mGluR5 negative allosteric modulators selected for clinical development. |
|
| DC75540 |
Exatecan mesylate |
Exatecan, also known as DX 8951, is semisynthetic, water-soluble camptothecin derivative with antineoplastic activity. Exatecan mesylate inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA and inhibiting religation of DNA breaks, thereby inhibiting DNA replication and triggering apoptotic cell death. This agent does not require enzymatic activation and exhibits greater potency than camptothecin and other camptothecin analogues |
|
| 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. |
|
| DC75542 |
LP-471756 |
LP-471756 is antagonist of GPR139. |
|
| 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. |
|
| 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. |
|
| DC75545 |
Pyruvate sodium |
Sodium pyruvate is an antioxidant potentially for the treatment of chronic obstructive pulmonary disease. |
|
| DC75546 |
KN-92 phosphate |
KN-92 is an inactive analog of the CaM kinase II inhibitor KN 93. |
|
| DC75547 |
Dexamethasone phosphate disodium |
Dexamethasone phosphate disodium is a water-soluble form of the synthetic glucocorticoid dexamethasone. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
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