| DC75650 |
GSK256066 free base |
GSK256066 is a potent and selective PDE4 inhibitor that can be given by inhalation, minimising the potential for side effects. GSK256066 demonstrated a protective effect on the EAR and LAR. GSK256066 is a slow and tight binding inhibitor of PDE4B (apparent IC(50) 3.2 pM; steady-state IC(50) <0.5 pM), which is more potent than any previously documented compound, for example, roflumilast (IC(50) 390 pM), tofimilast (IC(50) 1.6 nM), and cilomilast (IC(50) 74 nM). Consistent with this, GSK256066 inhibited tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC(50). GSK256066 has been demonstrated to have exceptional potency in vitro and in vivo and is being clinically investigated as a treatment for chronic obstructive pulmonary disease. |
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| DC75651 |
Azilsartan free acid |
Azilsartan is an angiotensin II receptor antagonist used in the treatment of hypertension, developed by Takeda. It is marketed in tablet form under the trade name Edarbi as the prodrug azilsartan medoxomil (INN, codenamed TAK-491). Azilsartan medoxomil lowers blood pressure by blocking the action of angiotensin II, a vasopressor hormone. |
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| DC75652 |
MA-VAL-ALA-PAB-OH |
MA-VAL-ALA-PAB-OH is a usefully ACD-linker, which was reported in JACS 2020, 142, pp12890-12895. |
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| DC75653 |
BXT-51072 |
BXT 51072, also known as ALT-2074, belongs to a class of drugs called "glutathione peroxidase mimics." BXT-51072 works by imitating a substance produced in various tissues in the body, which prevents damage of the heart and blood vessels. The intraocular injection of BXT-51072 protected axotomized neurons at doses in a narrow (tenfold) range. It also reduced the deleterious effects of intraocular tert-butyl hydroperoxide, an inducer of lipid peroxidation, and diminished the excitotoxic degeneration induced by N-methyl-D-aspartate. However, BXT-51072 did not noticeably reduce naturally occurring cell death. |
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| DC75654 |
Ripretinib free base |
Ripretinib, also known as DCC-2618, is a potent, orally active and selective KIT/PDGFR inhibitor with potential antineoplastic activity. DCC-2618 targets and binds to both wild-type and mutant forms of KIT and PDGFRa specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. In May 2020, FDA Approves Qinlock (ripretinib) for the Treatment of Fourth-Line Gastrointestinal Stromal Tumor |
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| DC75655 |
Befiperide HCl |
Befiperide, also known as DU-29325, is a substituted piperazine that has agonist activity at serotonin1 receptors. |
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| DC75656 |
Revumenib |
Revumenib, also known as SNDX-5613, is a potent and specific Menin-MLL inhibitor. It can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). |
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| DC75657 |
Quetiapine |
Quetiapine, marketed as Seroquel, is an atypical antipsychotic approved for the treatment of schizophrenia, bipolar disorder, and along with an antidepressant to treat major depressive disorder. It is also sometimes used as a sleep aid because of its sedating effect but this use is not recommended. Quetiapine is a dopamine, serotonin, and adrenergic antagonist, and a potent antihistamine with clinically negligible anticholinergic properties. Quetiapine binds strongly to serotonin receptors; the drug acts as partial agonist at 5-HT1A receptors. |
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| DC75658 |
Artilide fumarate |
Artilide, also known as U88943 or U88943E, is a drug used for the treatment of cardiac arrhythmias. Artilide is a class III antiarrhythmic which is structurally-related to ibutilide and d,l-sotalol. Artilide had demonstrated inducibe ventricular arrhythmias prior to treatment. This antiarrhythmic action was associated with significant increases in ventricular refractoriness and monophasic action potential duration. Lower doses of artilide tended to reduce the incidence of spontaneous ventricular arrhythmias but these effects were not significant. These results are consistent with the concept that spontaneous and pacing induced ventricular arrhythmias result from different mechanisms, and that class III anti-arrhythmic agents are more effective in suppressing induced ventricular tachycardia due to reentry than spontaneous arrhythmias which result from nonreentrant mechanisms. |
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| DC75659 |
NAD free acid |
NAD is a dinucleotide of adenine and nicotinamide. It has coenzyme activity in redox reactions and also acts as a donor of ADP-ribose moieties. |
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| DC75660 |
Varenicline HCl |
Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine itself does. In this respect it is similar to cytisine and different from the nicotinic antagonist, bupropion, and nicotine replacement therapies (NRTs) like nicotine patches and nicotine gum. Varenicline displays full agonism on α7 nicotinic acetylcholine receptors and is a partial agonist on the α4β2, α3β4, and α6β2 subtypes. In addition, it is a weak agonist on the α3β2 containing receptors. Varenicline's partial agonism on the α4β2 receptors rather than nicotine's full agonism produces less effect of dopamine release than nicotine's. This α4β2 competitive binding reduces the ability of nicotine to bind and stimulate the mesolimbic dopamine system—similar to the method of action of buprenorphine in the treatment of opioid addiction. |
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| DC75661 |
Trilaciclib HCl |
Trilaciclib is a potential first-in-class short-acting CDK4/6 inhibitor in development to preserve hematopoietic stem cells and enhance immune system function during chemotherapy. Trilaciclib may help protect bone marrow cells from damage caused by chemotherapy by inhibiting cyclin-dependent kinase 4/6, a type of enzyme. Trilaciclib is the first therapy in its class and was approved for medical use in the United States in February 2021. |
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| DC75662 |
YCN47284 |
YCN47284 is an aromatic guanylhydrazone compounds with antimalarial activity. YCN47284 was first reported in WO 9621450. YCN47284 inhibited P. falciparum growth with IC50 = 0.075 μM to >10 μM as reported in US 20030186993. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). |
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| DC75663 |
BMS-1001 free base |
BMS-1001 is a potent PD-1/PD-L1 interaction inhibitor. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes. |
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| DC75664 |
Neomycin B sulfate |
Neomycin is an aminoglycoside antibiotic found in many topical medications such as creams, ointments, and eyedrops. Neomycin belongs to aminoglycoside class of antibiotics that contain two or more aminosugars connected by glycosidic bonds. Similar to other aminoglycosides, neomycin has excellent activity against Gram-negative bacteria, and has partial activity against Gram-positive bacteria. It is relatively toxic to humans, and many people have allergic reactions to it. Aminoglycosides such as neomycin are known for their ability to bind to duplex RNA with high affinity. |
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| DC75665 |
SUVN-911 free base |
SUVN-911 is a potent and selective α4β2 nAChR antagonist. SUVN-911 showed excellent ADME properties with no drug-drug interaction liability and robust efficacy in animal models of depression. it is a potent α4β2 receptor ligand with a Ki value of 1.5 nM. It showed >10 μM binding affinity toward the ganglionic α3β4 receptor apart from showing selectivity over 70 other targets. It is orally bioavailable and showed good brain penetration in rats. . |
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| DC75666 |
MN58b bromide |
MN58b bromide, or MN58b, is a selective choline kinase α (CHKα) inhibitor. MN58b is a novel anticancer drug that inhibits choline kinase, resulting in inhibition of phosphocholine synthesis. Inhibition of choline kinase by MN58b resulted in altered phospholipid metabolism both in cultured tumor cells and in vivo. |
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| DC75667 |
Tarloxotinib bromide |
Tarloxotinib bromide, also known TH-4000 or PR-610, is a prodrug designed to selectively release a covalent (irreversible) EGFR tyrosine kinase inhibitor under severe hypoxia, a feature of many solid tumors. Tarloxotinib has the potential to effectively shut down aberrant EGFR signaling in a tumor-selective manner, thus potentially avoiding or reducing the systemic side effects associated with currently available EGFR tyrosine kinase inhibitors. |
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| DC75668 |
Sunitinib free base |
Sunitinib free base is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor. Sunitinib malate salt was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs). The simultaneous inhibition of these targets therefore reduces tumor vascularization and triggers cancer cell apoptosis and thus results in tumor shrinkage. Sunitinib also inhibits CD117 (c-KIT), the receptor tyrosine kinase that (when improperly activated by mutation) drives the majority of gastrointestinal stromal cell tumors. |
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| DC75669 |
Venadaparib |
Venadaparib, also known as IDX-1197, is a potent, selective and orally active PARP inhibitor with IC50s of 1 ~2 nM.. By inhibiting PARP, IDX-1197 stops cancer cells from repairing SSBs and drives the conversion of SSBs into double-strand breaks. IDX-1197 triggers a phenomenon known as synthetic lethality, which is defined by cell death resulting from the simultaneous perturbation of two genes without damaging normal cells. IDX-1197 is primarily aimed at treating homologous recombination deficient (HRD) patients. Notably, IDX-1197 has a particularly strong trapping effect, meaning it is more effective at trapping PARP1 and PARP2 enzymes on damaged DNA. |
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| DC75670 |
Dalpiciclib free base |
Dalpiciclib, also known as SHR-6390, is a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. SHR6390 exhibited potent antiproliferative activity against a wide range of human RB‐positive tumor cells in vitro, and exclusively induced G1 arrest as well as cellular senescence, with a concomitant reduction in the levels of Ser780‐phosphorylated RB protein. Compared with the well‐known CDK4/6 inhibitor palbociclib, orally administered SHR6390 led to equivalent or improved tumor efficacy against a panel of carcinoma xenografts, and produced marked tumor regression in some models, in association with sustained target inhibition in tumor tissues. Furthermore, SHR6390 overcame resistance to endocrine therapy and HER2‐targeting antibody in ER‐positive and HER2‐positive breast cancer, respectively. Moreover, SHR6390 combined with endocrine therapy exerted remarkable synergistic antitumor activity in ER‐positive breast cancer. |
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| DC75671 |
BAY-1251152 racemate |
BAY-1251152 racemate, also known as (±)-BAY-1251152, is a racemic mixture of BAY-1251152. BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins. This may cause cell cycle arrest and induce apoptosis, which may lead to a reduction in tumor cell proliferation. |
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| DC75672 |
JHN07588 |
JHN07588, also known as MMP-2/MMP-9 inhibitor I, is a potent inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9. It acts by binding zinc at the active site of these MMPs. This compound has been used to elucidate the roles of MMP-2 and MMP-9 in diverse systems, including mammary epithelial cell transformation, neuronal dysfunction, lymphocyte recruitment, and progressive hereditary kidney disease. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). |
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| DC75673 |
Senaparib free base |
Senaparib, also known as IMP4297, is s a novel highly potent and selective oral PARP1/2 inhibitor with strong antitumor activity in preclinical studies. Senaparib demonstrated encouraging clinical benefit and a favorable tolerability profile in patients with advanced solid tumour. |
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| DC75674 |
JBJ-04-125-02 R-isomer |
JBJ-04-125-02 is a mutant-selective EGFR allosteric inhibitor with potential anticancer activity. As a single agent, it can inhibit cell proliferation and EGFRL858R/T790M/C797S signaling in vitro and in vivo. The combination of osimertinib and JBJ-04-125-02 results in an increase in apoptosis, a more effective inhibition of cellular growth, and an increased efficacy in vitro and in vivo compared with either single agent alone. |
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| DC75675 |
Bupropion HCl |
Bupropion, also known as amfebutamone and BW 323, is a norepinephrine–dopamine reuptake inhibitor (NDRI) and a nicotinic receptor antagonist. However, its effects on dopamine are weak and clinical significance is contentious. Chemically, bupropion is an aminoketone that belongs to the class of substituted cathinones and more generally that of substituted amphetamines and substituted phenethylamines. |
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| DC75676 |
Butenafine HCl |
Butenafine is a synthetic benzylamine antifungal. It is structurally related to synthetic allylamine antifungals such as terbinafine. Like the allylamine antifungals, butenafine works by inhibiting the synthesis of ergosterol by inhibiting squalene epoxidase, an enzyme responsible for the creation of sterols needed in fungal cell membranes. Lacking ergosterol, the cell membranes increase in permeability, allowing their contents to leak out. Furthermore, inhibition of squalene epoxidase leads to a toxic buildup of squalene. This double action of butenafine (increased membrane permeability and toxic buildup of squalene) makes butenafine fungicidal rather than merely fungistatic. |
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| DC75677 |
LGH447 free base |
PIM447, also known as LGH447, is a potent Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitor. Pan proviral insertion site of Moloney murine leukemia (PIM) 1, 2, and 3 kinase inhibitors have recently begun to be tested in humans to assess whether pan PIM kinase inhibition may provide benefit to cancer patients. PIM447 demonstrates in vivo target modulation (pS6RP), single agent antitumor activity in a KG-1 AML mouse xenograft model, and druglike properties suitable for development. PIM447 advanced into humans in 2012 and is currently being assessed in several phase I trials. |
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| DC75678 |
Dalbavancin HCl |
Dalbavancin is a novel second-generation lipoglycopeptide antibiotic. It belongs to the same class as vancomycin, the most widely used and one of the few treatments available to patients infected with methicillin-resistant Staphylococcus aureus (MRSA). Dalbavancin is a semisynthetic lipoglycopeptide that was designed to improve upon the natural glycopeptides currently available, vancomycin and teicoplanin. It possesses in vitro activity against a variety of Gram-positive pathogens including MRSA and methicillin-resistant Staphylococcus epidermidis (MRSE). |
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| DC75679 |
JNJ-18038683 citrate |
JNJ-18038683 is a 5-HT7 receptor antagonist which has been shown to be effective in models of depression and to increase the latency to rapid eye movement (REM) sleep and decrease REM duration. JNJ-18038683 enhanced serotonin transmission, antidepressant-like behavior, and REM sleep suppression induced by citalopram in rodents. |
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