| DC75582 |
Taletrectinib adipate |
Taletrectinib, also known as DS-6051B, is an orally available inhibitor of the receptor tyrosine kinases C-ros oncogene 1 (ROS1) and the neurotrophic tyrosine receptor kinase (NTRK) types 1, 2 and 3, with potential antineoplastic activity. Upon oral administration, DS-6051b binds to and inhibits ROS1 and the NTRK family members. This inhibition leads to a disruption of ROS1- and NTRK-mediated signaling and eventually inhibits the growth of tumor cells that are overexpressing ROS1 and/or NTRKs. ROS1, overexpressed in certain cancer cells, plays a key role in cell growth and survival of cancer cells. NTRK mutations or rearrangements play a key role in cancer progression. |
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| DC75583 |
Empesertib |
Empesertib, also known as BAY1161909, is an orally bioavailable, selective inhibitor of the serine/threonine monopolar spindle 1 (Mps1) kinase, with potential antineoplastic activity. Upon administration, the Mps1 kinase inhibitor BAY1161909 binds to and inhibits the activity of Mps1. This causes inactivation of the spindle assembly checkpoint (SAC), accelerated mitosis, chromosomal misalignment, chromosomal missegregation, mitotic checkpoint complex destabilization, and increased aneuploidy. This leads to the induction of cell death in cancer cells overexpressing Mps1. |
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| DC75584 |
Gefapixant citrate |
Gefapixant citrate is a P2X3 antagonist currently studied for use in the treatment of disorders associated with purinergic receptor activation. |
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| DC75585 |
Roblitinib |
Roblitinib, also known as FGF401, is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4) with potential antineoplastic activity. Upon administration, FGF401 binds to and inhibits the activity of FGFR4, which leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cell proliferation, differentiation, angiogenesis, and survival. |
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| DC75586 |
CPI-169 |
CPI-169 is a potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of <1nM for polycomb repressive complex 2 (PRC2). CPI-169 was shown to inhibit tumor growth in a NHL xenograft model, reducing global H3K27me3.1 It has also been shown to synergize with the B-cell lymphoma inhibitor, ABT-199, to suppress the growth of NHL cell lines. Note: CPI-169 is a racemic mixture. |
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| DC75587 |
DOPS sodium |
DOPS is a lipid reagent. DOPS liposomes are used to encapsulate quantum dots, to form “lipodot”, which facilitated the study of lipdot-cell-interactions. DOPS is an anionic phospholipid that is frequently used to prepare negatively charged liposomes. Liposomes containing DOPS have been used to entrap cisplatin with high efficiency and substantially higher anticancer efficiency. DOPS containing anionic liposomes have been used widely for the interactions between polymers with opposite charges, such as cationic charge polypeptides in the event of membrane fusion. |
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| DC75588 |
Epetraborole HCl |
Epetraborole, also known as GSK2251052 and AN3365, is a potent and selective leucyl-tRNA synthetase inhibitor. Epetraborole was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens. GSK2251052 is a novel boron-containing antibiotic that inhibits bacterial leucyl tRNA synthetase. All Clostridium perfringens strains had GSK2251052 MICs of >32 μg/ml. |
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| DC75589 |
Cariprazine free base |
Cariprazine, also known as RGH-188 and MP-214, is an antipsychotic drug received FDA approval on September 17, 2015. Cariprazine acts as a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor. Action on the dopaminergic systems makes it also potentially useful as an add-on therapy in major depressive disorder. Cariprazine is approved for schizophrenia and bipolar disorder. It has also been investigated as a potential adjunct in treatment-resistant major depressive disorder. |
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| DC75590 |
Hydromethylthionine HBr |
Hydromethylthionine, also known as LMTM and Leucomethylene Blue, is a apotent tau aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. Hydromethylthionine showed pharmacological activity on brain structure and function as both monotherapy and as an add-on to symptomatic treatment in certain patients with Alzheimer’s disease. |
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| DC75591 |
FR-179642 |
FR-179642 is a cyclic peptide and an important intermediate in producing micafungin. |
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| DC75592 |
Moxidectin |
Moxidectin is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms. Moxidectin is a semisynthetic derivative of nemadectin which is produced by fermentation by Streptomyces cyano-griseus. This Streptomyces species was discovered in a soil sample from Australia in the late 1980s collected by an agronomist working for the American Cyanamid company. |
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| DC75593 |
SRI-37330 HCl |
SRI-37330 is an orally bioavailable, non-toxic small molecule TXNIP inhibitor. SRI-37330 effectively rescued mice from streptozotocin- and obesity-induced (db/db) diabetes. SRI-37330 inhibited expression and signaling of thioredoxin-interacting protein, SRI-37330 treatment inhibited glucagon secretion and function, reduced hepatic glucose production, and reversed hepatic steatosis. Rescue assays confirmed that the impact of FTO on the TXNIP/NLRP3 pathway was significantly reversed by the TXNIP inhibitor SRI-37330. |
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| DC75594 |
OUN67600 |
OUN67600, is a Novel Transient Receptor Potential Vanilloid 4 (TRPV4) Agonist as Regulators of Chondrogenic Differentiation. OUN67600 was first reported by Atobe et al (compound 36 in J Med Chem. 2019 Feb 14;62(3):1468-1483). 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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| DC75595 |
LM11A-31 HCl |
LM11A-31 is a small-molecule p75NTR modulator and proNGF antagonist, in preventing diabetes-induced BRB breakdown. Targeting p75NTR signalling using LM11A-31, an orally bioavailable receptor modulator, may offer an effective, safe and non-invasive therapeutic strategy for treating macular oedema, a major cause of blindness in diabetes. |
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| DC75596 |
Eleclazine free base |
Eleclazine, also known as GS-6615, is a selective late sodium current inhibitor. Eleclazine is potentially useful for treatment of coronary vasodilators, antiarrhythmics and vasodilators. Eleclazin showed a shortening of the QTc interval (the time interval between the start of the Q-wave and end of the T-wave in the heart’s electrical cycle) in patients with long QT-3 (LQT3) syndrome. LQT3 is a genetic disorder that prolongs the heart’s QTc interval and can cause life-threatening cardiac arrhythmias (abnormal heartbeats). |
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| DC75597 |
Ibiglustat |
Venglustat, also known as Ibiglustat, GZ402671, GZ-452; Genz-682452 and SAR402671, is a potent and selective Glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor. Ibiglustat blocks the formation of glucosylceramide (GL-1), a key intermediate in the synthesis of GL-3. Ibiglustat is potentially useful for treating Fabry disease. Fabry disease is a rare lysosomal storage disorder, which results in abnormal tissue deposits of a particular fatty substance called globotriaosylceramide (GL-3 or Gb3) throughout the body. |
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| DC75598 |
Rineterkib free base |
Rineterkib, also known as LTT-462 or ERK-IN-1, is a ERK1/2 inhibitor which has demonstrated preclinical activity in multiple MAPK activated cancer cells and xenograft models. LTT462 binds to and inhibits ERK, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in numerous tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival. |
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| DC75599 |
Argatroban hydrate |
Argatroban is an anticoagulant that is a direct thrombin inhibitor. Argatroban was approved in 2000 for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). Argatroban is a direct thrombin inhibitor that reversibly binds to the thrombin active site. Argatroban exerts its anticoagulant effects by inhibiting thrombin-catalyzed or -induced reactions, including fibrin formation; activation of coagulation factors V, VIII, and XIII; activation of protein C; and platelet aggregation. Argatroban inhibits thrombin with an inhibition constant (Ki) of 0.04 μM. |
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| DC75600 |
Riamilovir sodium hydrate |
Riamilovir, also known as Triazavirin, is an antiviral. Riamilovir has antiviral activity against influenza strains (such as H5N1), tick-borne encephalitis virus, and forest-spring encephalitis virus. It is being investigated for activity against Lassa fever, Ebola virus disease, and SARS-CoV-2. |
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| DC75601 |
AN-2898 |
AN-2898 ia a potent and selective PDE4 inhibitor potentially for the treatment of fungal infection. AN2898 inhibited phosphodiesterase 4 (PDE4) enzyme activity (IC50 0.060 μM) and the release of multiple cytokines including TNF-α (IC50 0.16 μM) from peripheral blood mononuclear cells (hPBMCs) stimulated by lipopolysaccharide (LPS) or phytohemag- glutinin. |
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| DC75602 |
MTDIA HCl |
MTDIA, also known as MT-DADMe-ImmA, and Methylthio-DADMe-Immucillin A, is a MTAP inhibitor. Human 5'-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5'-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage. Transition-state (TS) analogues of MTAP are in development as anticancer candidates. TS analogues of MTAP incorporate a cationic nitrogen and a protonated 9-deazaadenine leaving group, which are mimics of the ribocation transition state. MT-ImmA and MT-DADMe-ImmA are two examples of these TS analogues. |
|
| DC75603 |
VUN65671 |
VUN65671is a Potent Entry Inhibitor of Ebola and Marburg Virus Infections. VUN65671 was reported in Journal of Medicinal Chemistry (2020), 63(13), 7211-7225. 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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| DC75604 |
Cerdulatinib HCl |
Cerdulatinib, also known as PRT2070 and PRT062070, is a n ovel, oral, dual spleen tyrosine kinase (Syk) and janus kinase (JAK) inhibitor. Cerdulatinib preferentially inhibited JAK1 and JAK3 dependent cytokine mediated signaling and functional responses in various cell types. IL2 mediated STAT5 Y694 was inhibited with an IC50 of 0.27μM, while IL4 mediated signaling to STAT6 Y641 and functional responses in B cells and monocytes, namely CD69, CD25, and CD23 up-regulation, were inhibited with IC50Â’s within the range of 0.11μM to 0.57μM. It is currently being studied in patients with genetically-defined hematologic cancers, as well as for patients who have failed therapy due to relapse or acquired mutations. |
|
| DC75605 |
Isuzinaxib |
APX-115, also known as EWHA-18278, is a potent, orally active pan NADPH oxidase (Nox) inhibitor. APX-115 protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. APX-115 might be a promising therapeutic agent for the treatment of DN because of its pan-NOX inhibitory activity, including its NOX5 inhibitory activity, and also owing to its anti-inflammatory effect. |
|
| DC75606 |
Fluoxetine |
Fluoxetine is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder. |
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| DC75607 |
BMS-P5 free base |
BMS-P5 is a Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor with pIC50 values in the range of 5-7.5. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays appearance of symptoms and disease progression Targeting PAD4 may be beneficial for treatment of multiple myeloma. |
|
| DC75608 |
Verubecestat TFA |
Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients. |
|
| DC75609 |
Amiselimod HCl |
Amiselimod, also known as MT1303, is a potent and selective immunosuppressant and sphingosine 1 phosphate receptor modulator. Amiselimod may be potentially useful for treatment of multiple sclerosis; inflammatory diseases; autoimmune diseases; psoriasis and inflammatory bowel diseases. Amiselimod is currently being developed by Mitsubishi Tanabe Pharma Corporation. |
|
| DC75610 |
Emavusertib |
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. |
|
| DC75611 |
Fadraciclib free base |
Fadraciclib, also known as CYC065, is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities. CYC065 selectively binds to and inhibits the activity of CDK2, 5 and 9, which leads to inhibition of CDK2, 5 and 9-dependent cellular pathways, downregulation of genes involved in the pro-survival pathway, prevention of the activation of DNA double-strand break repair pathways, and induction of both cell cycle arrest and apoptosis. This inhibits the proliferation of CDK2/5/9-overexpressing tumor cells. In addition, CYC065 protects hematopoietic stem and progenitor cells (HSPCs), prevents myelosuppression, and preserves the function of the bone marrow. |
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