| DC74780 |
Lefamulin free base |
Lefamulin is an antibiotic medication used it to treat adults with community-acquired bacterial pneumonia. It is a pleuromutilin antibiotic that inhibits the large subunit of bacterial ribosomes Lefamulin is used to treat adults with community-acquired bacterial pneumonia. It was also investigated for treatment of acute bacterial skin and skin-structure infections (ABSSSI). Lefamulin has in vitro activity against Streptococcus viridans, Moraxella catarrhalis, Enterococcus faecium, methicillin-resistant Staphylococcus aureus (MRSA), among other bacteria. . Lefamulin was approved in 2019. |
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| DC74781 |
PDCD4-IN-1 |
PDCD4-IN-1(compound 20031600) is a PDCD4 inhibitor. |
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| DC74782 |
CDK8-IN-12 |
CDK8-IN-12 is an orally active, potent CDK8 inhibitor. |
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| DC74783 |
Raxatrigine HCl |
Raxatrigine, also known as vixotrigine, GSK1014802, and CNV1014802, is a small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor. |
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| DC74784 |
Beloxepin |
Beloxepin, also known as ADL-6906; ORG-4428, is an oral dual selective serotonin and norepinephrine uptake inhibitor. |
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| DC74785 |
PARP-1-IN-4 |
PARP-1-IN-4 is a PARP-1 inhibitor. |
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| DC74786 |
Physostigmine salicylate |
Physostigmine salicylate is a reversible cholinesterase inhibitor, a parasympathomimetic alkaloid. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. |
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| DC74787 |
LY 235959 new |
LY 235959 is a competitive NMDA receptor antagonist. |
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| DC74788 |
PF-670462 HCl |
PF-670462 is a potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC50 = 7.7 and 14 nM, respectively), with applications towards treatment of bladder cancer. Inhibition of CKIepsilon yields a perturbation of oscillator function that forestalls light as a zeitgeber, and they demonstrate that pharmacological tools such as PF-670462 may yield valuable insight into clock function. Casein kinase Iepsilon (CKIepsilon) is an essential component of the biological clock, phosphorylating PER proteins, and in doing so regulating their turnover and nuclear entry in oscillator cells of the suprachiasmatic nucleus (SCN). |
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| DC74789 |
CAY10462 HCl |
CAY10462 is the hydrochloride salt of CAY10434 and selective inhibitor of the 20-HETE synthase CYP4A11 exhibiting an IC50 of 8.8 nM when tested in human renal microsomes.4 CAY10434 is nearly 200 times less potent as an inhibitor of 1A, 1C, and 3A CYP450. |
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| DC74790 |
PROTAC MDM2 Degrader-2 |
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. |
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| DC74791 |
Oxantel Pamoate |
Oxantel Pamoate is an anthelmintic used to treat Trichuris trichiura infection. |
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| DC74792 |
KN62 |
KN62 is a P2X7R antagonist (hP2X7 IC50 = 51 nM) and Ca2+/calmodulin-dependent protein kinase II inhibitor. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca(2+)-channels. The effect of KN62 on Ca(2+)-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool. |
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| DC74793 |
PF-5274857 freebase |
PF-5274857 is a potent, orally active and selective hedgehog (Hh) signaling pathway inhibitor with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway. |
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| DC74794 |
Otenabant free base |
Otenabant Hydrochloride is the salt of Otenabant, also known as CP-945,598, a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the treatment of obesity, but development for this application has been discontinued following the problems seen during clinical use of the similar drug rimonabant. |
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| 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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