| DC74795 |
ML-9 HCl |
ML-9 HCl a is myosin light chain kinase (MLCK) inhibitor. ML-9 enhances the anticancer activity of docetaxel, suggesting its potential application as an adjuvant to existing anticancer chemotherapy. The complex effect of ML-9 on autophagy and indentified ML-9 as an attractive tool for targeting autophagy in cancer therapy through dual inhibition of both the Akt pathway and the autophagy. |
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| DC74796 |
AlPcS4 |
AlPcS4 , also known as aluminum phthalocyanine tetrasulfonate Chloroaluminum tetrasulfophthalocyanine; or AlS4Pc, AlPcS4(a), is a potent photosensitizer, and is potentially useful in cancer sonodynamic therapy and cancer photodynamic therapy. Aluminum phthalocyanine disulfonate is a mixture of regional isomers, in which sulfonate group can be in 3- or 4- position in phenyl ring. Aluminum phthalocyanine disulfonate is also a Coloring Agent; Dermatologic Agent; Fluorescent Dye; Indicators and Reagent; Luminescent Agent; Photosensitizing Agent; Radiation-Sensitizing Agent. |
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| DC74797 |
Etifoxine HCl |
Etifoxine, also known as HOE 36801 and etafenoxine, is an anxiolytic and anticonvulsant drug developed by Hoechst in the 1960s. Unlike benzodiazepines, etifoxine appears to produce its anxiolytic effects by binding to β2 and β3 subunits of the GABAA receptor complex, and so is acting at a different target site to benzodiazepines, although the physiological effect that is produced is similar to that of benzodiazepines. |
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| DC74798 |
JNJ-10191584 |
JNJ-10191584 is a drug which acts as a potent and selective antagonist at the histamine H4 receptor. It has antiinflammatory and analgesic effects in animal studies of acute inflammation. JNJ-10191584 binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). |
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| DC74799 |
NSC243928 |
NSC243928 binds to LY6K in cancer cells expressing LY6K, leading to cell death. NSC243928 is an anticancer agent. |
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| DC74800 |
PXS-5505 HCl |
PXS-5505 is a Pan-Lysyl Oxidase Inhibitor that has been found to ameliorate multiple-organ fibrosis by inhibiting collagen crosslinks in rodent models in systemic sclerosis. PXS-5505 inhibited lysyl oxidase activity in the skin and LOXL2 activity in the lung. PXS-5505 exhibited anti-fibrotic effects in the SSc skin mouse model, reducing dermal thickness and α-smooth muscle actin. Similarly, in the bleomycin-induced mouse lung model, PXS-5505 reduced pulmonary fibrosis toward normal levels, mediated by its ability to normalise collagen/elastin crosslink formation. PXS-5505 also reduced fibrotic extent in models of the ischaemia-reperfusion heart, the unilateral ureteral obstruction kidney, and the CCl4-induced fibrotic liver. |
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| 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. |
|
| 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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