| DC74801 |
Niraparib free base |
Niraparib, also known as MK4827, is an orally active, potent and selective poly(ADP-Ribose) polymerase (PARP) inhibitor that radiosensitizes human lung and breast cancer cells. Niraparib inhibits PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM respectively. Niraparib is currently in Phase 3 clinical trials for ovarian cancer and BRCA+ breast cancer. |
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| DC74802 |
Tucidinostat free base |
Tucidinostat (also known as HBI-8000, Chidamide, and CS-055) is a benzamide type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Tucidinostat selectively binds to and inhibits HDAC leading to an increase of acetylation levels of histone protein H3. This agent also inhibits the expression of signaling kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. |
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| DC74803 |
Vicriviroc maleate |
Vicriviroc, also known as SCH 417690, MK-7690 and SCH-D, is a potent, orally active and selective CCR5 entry inhibitor of HIV-1 (IC50 = 0.91 nM). Vicriviroc effectively inhibits the initial stages of the virus life cycle. Vicriviroc demonstrated synergistic anti-HIV activity in combination with drugs from all other classes of approved antiretrovirals. Vicriviroc binds with higher affinity to CCR5 than SCH-C. Functional assays, including inhibition of calcium flux, guanosine 5'-[35S]triphosphate exchange, and chemotaxis, confirmed that vicriviroc acts as a receptor antagonist by inhibiting signaling of CCR5 by chemokines. Vicriviroc demonstrated diminished affinity for the human ether a-go-go related gene transcript ion channel compared to SCH-C, suggesting a reduced potential for cardiac effects. Vicriviroc represents a promising new candidate for the treatment of HIV-1 infection. |
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| DC74804 |
4-PPBP maleate |
4-PPBP is a σ ligand and selective non-competitive antagonist at recombinant NR1a/2B NMDA receptors expressed in Xenopus oocytes. 4-PPBP protects against newborn excitotoxic brain injury by stabilizing the mitochondrial membrane potential in vitro and inhibiting microglial activation in vivo. 4-PPBP modulates neuronal nitric oxide synthase/postsynaptic density-95 coupling mechanisms and protects against neonatal ischemic degeneration of striatal neurons. |
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| DC74805 |
X-376 |
X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer. Caution: Many vendora are mistakenly selling X-376 as Ensartinib (X396, X-396, X 396). The structure is slightly different (see Cat#206013) |
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| DC74806 |
Clemizole HCl |
Clemizole, also known as AL 20, P 48, or Reactrol, is a potent inhibitor of transient receptor potential channel TRPC5. Clemizole efficiently blocks TRPC5 currents and Ca(2+) entry in the low micromolar range (IC50 = 1.0-1.3 µM). Clemizole blocks TRPC5 currents irrespectively of the mode of activation. Based on fluorometric [Ca(2+)]i measurements, clemizole exhibits a sixfold selectivity for TRPC5 over TRPC4β (IC50 = 6.4 µM). Clemizole was not only effective in blocking heterologously expressed TRPC5 homomers but also TRPC1:TRPC5 heteromers as well as native TRPC5-like currents in the U-87 glioblastoma cell line. |
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| DC74807 |
AZD-8529 free base |
AZD-8529 is a a positive allosteric modulator at the mGluR2 receptor. AZD8529 decreases Nicotine Self-Administration and Relapse in Squirrel Monkeys. AZD8529 potentiated agonist-induced activation of mGluR2 in the membrane-binding assay and in primate cortex, hippocampus, and striatum. In monkeys, AZD8529 decreased nicotine self-administration at doses (.3-3 mg/kg) that did not affect food self-administration. AZD8529 also reduced nicotine priming- and cue-induced reinstatement of nicotine seeking after extinction of the drug-reinforced responding. In rats, AZD8529 decreased nicotine-induced accumbens dopamine release. The positive allosteric modulators of metabotropic glutamate receptor 2 should be considered for relapse prevention. |
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| DC74808 |
Timapiprant |
Timapiprant, also known as OC000459, is a potent, selective and orally active CRTH2 antagonist. OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. OC000459 inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. OC000459 treatment inhibited LAR and post-allergen increase in sputum eosinophils. OC000459 appears to inhibit allergic inflammation in asthma. |
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| DC74809 |
PKUMDL-LC-101-D04 |
PKUMDL-LC-101-D04 is an allosteric activator of glutathione peroxidase 4 (GPX4). |
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| DC74810 |
PF-543 free base |
PF-543 is a novel selective SK-1 inhibitor which inhibited SK-1 activity in a competitive manner with sphingosine. PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 was effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. PF-543 is the most potent inhibitor of SphK1 described to date and it will be useful for dissecting specific roles of SphK1-driven S1P signalling. |
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| DC74811 |
NNC 55-0396 HCl |
NNC 55-0396 is a T-type calcium channel blocker. NNC 55-0396 inhibits angiogenesis via suppression of hypoxia-inducible factor-1α signal transduction. NNC 55-0396 suppressed mitochondrial reactive oxygen species-mediated HIF-1α expression as well as stabilization by inhibiting protein synthesis in a dose-dependent manner. NNC 55-0396 inhibited tumor-induced angiogenesis in vitro and in vivo by suppressing HIF-1α stability. NNC 55-0396 could be a potential therapeutic drug candidate for cancer treatment. |
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| DC74812 |
Ciproxifan maleate |
Ciproxifan, also known as FUB-359, is an extremely potent histamine H3 inverse agonist/antagonist. Ciproxifan produces wakefulness and attentiveness in animal studies, and produced cognitive enhancing effects without prominent stimulant effects at relatively low levels of receptor occupancy, and pronounced wakefulness at higher doses. It has therefore been proposed as a potential treatment for sleep disorders such as narcolepsy and to improve vigilance in old age, particularly in the treatment of conditions such as Alzheimer's disease. It also potentiated the effects of antipsychotic drugs, and has been suggested as an adjuvant treatment for schizophrenia. |
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| DC74813 |
N-piperidine Ibrutinib HCl |
N-piperidine Ibrutinib hydrochloride, a reversible Ibrutinib derivative, is a potent BTK inhibitor. |
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| DC74814 |
CYP1B1-IN-4 |
CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition. |
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| DC74815 |
ML024 |
SID-852843 is a WNV NS2B-NS3 proteinase inhibitor. |
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| DC74816 |
Navoximod free base |
Navoximod, also known as IDO-IN-7 and NLG-1488, is an indoleamine 2,3-dioxygenase (IDO) inhibitor. It is also used as an immunomodulator and an antineoplastic. |
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| DC74817 |
Ro60-0175 free base |
Ro60-0175 is a potent and selective SR-2 agonist. It shows selectivity for the 5-HT2C subtype (pKi values are 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively). Ro60-0175 acts as a potent and selective agonist for both the 5-HT2B and 5-HT2C serotonin receptor subtypes, with good selectivity over the closely related 5-HT2A subtype, and little or no affinity at other receptors. |
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| DC74818 |
α-Glucosidase-IN-22 |
α-Glucosidase-IN-22 (compound 7i), a benzimidazole, is a potent α-glucosidase inhibitor. |
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| DC74819 |
RG-6080 |
Nacubactam, also known as RG-6080, FPI-1459, and OP-0595, is a beta-lactamase inhibitor used for treating bacterial infections. |
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| DC74820 |
Ponatinib HCl |
Ponatinib, also known as AP24534 is an oral drug for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome–positive (Ph+) acute lymphoblastic leukemia (ALL). It is a multi-targeted tyrosine-kinase inhibitor. Some forms of CML, those that have the T315I mutation, are resistant to current therapies such as imatinib. Ponatinib has been designed to be effective against these types of tumors. Ponatinib was approved in 2012. |
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| DC74821 |
DRI-C21041 |
DRI-C21041 is a CD40/CD40L interaction inhibitor |
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| DC74822 |
TRK-IN-22 |
TRK-IN-22 (compound 11) is a TRK inhibitor. |
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| DC74823 |
Azelnidipine |
Azelnidipine, also known as CS 905 and CCRIS 8650, is a dihydropyridine calcium channel blocker. It is sold in Japan by Daiichi-Sankyo pharmaceuticals, Inc. Unlike nicardipine, it has a gradual onset and has a long-lasting hypotensive effect, with little increase in heart rate. |
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| DC74824 |
CWI1-2 HCl |
CWI1-2 is an IGF2BP2 inhibitor. CWI1-2) shows promising anti-leukemia effects in vitro and in vivo. CWI1-2 preferentially binds to IGF2BP2 and inhibits its interaction with m6A-modified target transcripts. Targeting IGF2BP2 with CWI1-2 alone, or in combination with other agents, such as daunorubicin (DNR) or homoharringtonine (HHT), shows promising therapeutic efficacy in treating AML. CWI1-2 treatment significantly delayed leukemia onset and prolonged the survival of BMT recipient mice. Importantly, monitoring of body weight from the day of drug treatment for 12-18 days did not show any reduction of body weight upon CWI1-2 treatment. CWI1-2 is an effective and largely safe leading compound targeting IGF2BP2 for AML treatment. |
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| DC74825 |
Higenamine hydrochloride |
Higenamine, also known as norcoclaurine, is a β-adrenoceptor partial agonist potentially for the treatment of coronary heart disease. Higenamine is a chemical compound found in a variety of plants including Nandina domestica (fruit), Aconitum carmichaelii (root), Asarum heterotropioides, Galium divaricatum (stem and vine), Annona squamosa, and Nelumbo nucifera (lotus seeds). Higenamine, also known as norcoclaurine HCl, is legal to use within food supplements in the UK, EU, the USA and Canada. |
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| DC74826 |
MK-212 HCl |
MK-212 is a 5HT2C-receptor agonist. A dose-dependent the effect of 5HT2C-receptor agonist MK-212 on mouse behavior was demonstrated. Intraperitoneal injection of MK-212 in high doses (0.5 and 1.0 mg/kg) increased blood level of corticosterone in mice and reduced their motor activity. In low doses of 0.1 and 0.2 mg/kg, the agonist reduced anxiety, but had no effect on motor activity. It is hypothesized that low doses of MK-212 exhibited anxiolytic activity in mice. |
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| DC74827 |
Peramivir hydrate |
Peramivir, also known as BCX1812 and RWJ 270201, is an antiviral drug for the treatment of influenza. Peramivir is a neuraminidase inhibitor, acting as a transition-state analogue inhibitor of influenza neuraminidase and thereby preventing new viruses from emerging from infected cells. Peramivir was approved to treat influenza infection in adults. |
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| DC74828 |
KSK94 |
KSK94 is a high-affinity histamine H3 receptor antagonist. |
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| DC74829 |
KSK68 |
KSK68 is a Histamine H3 and Sigma‑1 Receptor Ligand, which may be useful in the Treatment of Nociceptive and Neuropathic Pain |
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| DC74830 |
PNU282987 HCl |
PNU282987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors. In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget. |
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