| 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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| DC75680 |
Atorvastatin calcium trihydrate |
Atorvastatin is used primarily for lowering blood cholesterol and for prevention of events associated with cardiovascular disease. Like all statins, atorvastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.Atorvastatin is also used for the treatment of dyslipidemia. |
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| DC75681 |
AZD-5904 |
AZD5904 is a potent orally bioavailable MPO inhibitor. In preclinical studies, AZD5904 inhibited the isolated MPO enzyme with an IC50 of 140 nM and was approximately equipotent in assays of rat and mouse MPO enzyme activity. Cross over to other species has not been investigated. AZD5904 was > 10-fold selective for the related peroxide enzymes lactoperoxidase (LPO) and thyroid peroxidase (TPO) and > 70-fold selective against a panel of other targets. AZD5904 dose dependently reduced MPO activity in a rat peritonitis model with an estimated plasma IC50 of 5 μmol/L (~1.3 μg/mL) and elicited protective effects at comparable plasma exposures in a mouse Experimental Autoimmune Encephalomyelitis (EAE) model, although effects were not consistently reproduced. AZD5904 was in development for multiple sclerosis and COPD and has been evaluated in single and multiple dose studies in healthy volunteers. |
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| DC75682 |
Palbociclib free base |
Palbociclib, also known as PD-0332991, is an orally available cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. Palbociclib selectively inhibits cyclin-dependent kinase 4 (CDK4) and 6 (CDK6), thereby inhibiting retinoblastoma (Rb) protein phosphorylation early in the G1 phase leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of cell cycle progression. Palbociclib, was approved on February 3, 2015 as a treatment (in combination with letrozole) for patients with estrogen receptor-positive advanced breast cancer. |
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| DC75683 |
TC-I-2000 |
TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells |
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| DC75684 |
Bepridil HCl |
Bepridil Hydrochloride is the hydrochloride salt form of bepridil, a calcium antagonist and class IV anti-arrhythmic agent. Bepridil hydrochloride blocks calcium entry through membranous calcium channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This drug is used to treat chronic stable and variant angina pectoris. Bepridil hydrochloride has antihypertensive and selective anti-arrhythmia activities and acts as a calmodulin antagonist. |
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| DC75685 |
ICI-204448 HCl |
ICI-204448 is a potent and peripherally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching effects. It is used in research to distinguish centrally from peripherally mediated kappa opioid receptor effects. |
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| DC75686 |
Quipazine dimaleate |
Quipazine dimaleate is a selective 5-HT3 receptor agonist that also displays antagonist activity at peripheral 5-HT3 receptors. [3H]-Quipazine labels 5-HT3 sites in the cortical membranes. |
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| DC75687 |
Lenacapavir |
Lenacapavir, also known as GS-6207, is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs). Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history. |
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| DC75688 |
Pardoprunox HCl |
Pardoprunox, also known as SLV-308; DU-126891; SME-308, is dopamine D2/5-HT1A receptor agonist potentially for the treatment of Parkinson's disease. It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned. Pardoprunox acts as a D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%). It also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. |
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| DC75689 |
Remodelin HBr |
Remodelin is a cell-permeable, potent, and stable analog of CPTH2. Remodelin inhibits acetyl-transferase NAT10, a nucleolar N-acetyltransferase involved in stabilization of microtubules. Remodelin is a cell-permeable, potent, and stable analog of CPTH2. Remodelin was found to correct cell defects associated with progeria, restoring and improving nuclear shape and reducing the DNA damage believed to be associated with mutations in the gene for laminin A. |
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| DC75690 |
Obeticholic Acid |
Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo rat model of cholestasis. It inhibits vascular smooth muscle cell inflammation and migration as well as promotes adipocyte differentiation and regulates adipose cell function in vivo. |
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| DC75691 |
Mitoglitazone |
Mitoglitazone, also known as CAY10415, is a novel peroxisome proliferator-activated receptor (PPAR)γ ligand. CAY10415 induced cell death and ROS generation in a PPARγ-independent manner. CAY10415 enhanced γ-radiation-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage in vitro. The combined CAY10415 / γ-radiation treatment triggered caspase-8 activation, and this initiator caspase played an important role in the combination-induced apoptosis. The combined treatment of CAY10415 and γ-radiation synergistically induced DNA damage and apoptosis, which was regulated by ROS. |
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| DC75692 |
PYR-5084 |
PYR-5084, CAS#59435-08-4, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
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| DC75693 |
Mycophenolate mofetil free acid |
Mycophenolate mofetil, also known as MMF or CellCept, is a prodrug of mycophenolic acid, and classified as a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). It is an immunosuppressant combined with drugs such as Cyclosporine and corticosteroids to prevent organ rejection after hepatic, renal, and cardiac transplants. |
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| DC75694 |
NB-598 free base |
NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). NB-598 suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. NB-598 reduced basolaterally secreted radioactivity in cholesterol, cholesterol ester, PL and TG. Furthermore, NB-598 suppressed the basolateral secretion of apolipoprotein (apo) B. When microsomes prepared from control Caco-2 cells were incubated with 10 microM NB-598, acyl CoA:cholesterol acyltransferase (ACAT) activity was inhibited slightly. |
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