| DC75717 |
GSK-J4 HCl |
GSK-J4 is a cell permeable, potent and selective histone demethylase. GSK-J4 is a prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). |
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| DC75718 |
Roxadustat |
Roxadustat, also known as ASP1517 and FG-4592, is an HIF α prolyl hydroxylase inhibitor in a cell-free assay. It stabilizes HIF-2 and induces EPO production and stimulates erythropoiesis. Roxadustat transiently and moderately increased endogenous erythropoietin and reduced hepcidin. |
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| DC75719 |
KB-R7943 mesylate |
KB-R7943 is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 μM). KB-R7943 does not modify secondary pathology in the thalamus following focal cerebral stroke in rats. KB-R7943 blocks opening of the mitochondrial permeability transition pore. KB-R7943 restores endothelium-dependent relaxation induced by advanced glycosylation end products in rat aorta. KB-R7943 inhibits high glucose-induced endothelial ICAM-1 expression and monocyte-endothelial adhesion. |
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| DC75720 |
ZX-29 |
ZX-29 is a potent and selective ALK inhibitor for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect. |
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| DC75721 |
CL2A-SN38 DCA |
CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. . |
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| DC75722 |
Cefteram |
Cefteram is a cephalosporin antibiotic. Its prodrug is Cefteram Pivoxil, which is used in the treatment of infections caused by bacteria. It works by killing bacteria or preventing their growth. Cefditoren pivoxil is also used to treat some throat and lung infections, including bronchitis and tonsillitis. It is also used to treat some skin infections. |
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| DC75723 |
Mavorixafor free base |
Mavorixafor, also known as AMD11070, AMD070, X4P-001, is an orally bioavailable and potent CXCR4 inhibitor. AMD11070 is an antagonist of SDF-1α ligand binding (IC50 = 12.5 ± 1.3 nM), inhibits SDF-1 mediated calcium flux (IC50 = 9.0 ± 2.0 nM) and SDF-1α mediated activation of the CXCR4 receptor as measured by a Eu-GTP binding assay (IC50 =39.8 ± 2.5 nM) or a [(35)S]-GTPγS binding assay (IC50 =19.0 ± 4.1 nM), and inhibits SDF-1α stimulated chemotaxis (IC50 =19.0 ± 4.0 nM). AMD11070 abrogates melanoma cell migration and is significantly more effective than AMD3100. AMD11070 represents a novel therapeutic strategy for both B-RAF wild-type and mutated melanomas. |
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| DC75724 |
AZD-2858 |
AZD2858 is a potent and GSK-3 inhibitor with an IC50 of 68 nM. AZD-2858 inhibits tau phosphorylation at the S396 site, and it activates Wnt signaling pathway. AZD2858 has a substantial impact on fracture healing. The fractures healed with a bony callus without an obvious endochondral component, suggesting that AZD2858 drives mesenchymal cells into the osteoblastic pathway. |
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| DC75725 |
NBQX free acid |
NBQX, also known as FG9202, is an AMPA receptor antagonist. NBQX blocks AMPA receptors in micromolar concentrations (~10–20 µM) and also blocks kainate receptors. In experiments, it is used to counter glutamate excitotoxicity. NBQX was found to have anticonvulsant activity in rodent seizure models. As the disodium salt, NBQX is soluble in water at high concentrations (at least up to 100 mM). |
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| DC75726 |
Tranilast |
Tranilast is an analog of a tryptophan metabolite. Initially, tranilast was identified as an anti-allergic agent, and used in the treatment of inflammatory diseases, such as bronchial asthma, atypical dermatitis, allergic conjunctivitis, keloids and hypertrophic scars. Subsequently, the results showed that it could be also effective in the management of a wide range of conditions. The beneficial effects of tranilast have also been seen in a variety of disease states, such as fibrosis, proliferative disorders, cancer, cardiovascular problems, autoimmune disorders, ocular diseases, diabetes and renal diseases. |
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| DC75728 |
Ansamitocin P-3' |
Ansamitocin P3' is an isomer of Ansamitocin P-3 or iso-Ansamitocin P-3 , is a natural product. Ansamitocin P-3' showed potential antineoplastic and antimitotic activity. Ansamitocin -' binds to tubulin and inhibits vinblastine-induced spiral formation. |
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| DC75729 |
Molybdenum phosphide |
Molybdenum Phosphide has been investigated as a highly efficient electrocatalyst for various applications such as hydrogen evolution and CO2 reduction. Molybdenum phosphide exhibits high activity towards the hydrogen evolution reaction (HER) in both acid and alkaline media even in bulk form. Comparative analysis of Mo, Mo3P and MoP as catalysts for HER clearly indicates that phosphorization can potentially modify the properties of the metal and different degrees of phosphorization lead to distinct activities and stabilities. |
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| DC75730 |
DT-2216 |
DT2216 is discontinued for commercial reasons. |
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| DC75731 |
EPZ-025654 |
EPZ-025654 is a potent and selective arginine methyltransferase CARM1 inhibitor. |
|
| DC75732 |
RA190 HCl |
RA190 is a potent Rpn13 inhibitor and ADRM1 inhibitor, suppressing intrahepatic cholangiocarcinoma by inducing NF-kappaB-mediated cell apoptosis. |
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| DC75733 |
2-PMDQ |
2-PMDQ is a potent selective α1 antagonist. |
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| DC75734 |
Clobenpropit HBr |
Clobenpropit, also known as VUF 9153, is a highly potent H3 antagonist and H4 partial agonist. Clobenpropit has been shown to protect NMDA-induced neuronal necrosis in cortical neuronal cell culture from rats. Clobenpropit promises neuroprotection against LPS-induced cognitive deficits by meliorating neuroinflammation and restoring the MRCC enzymes in mice. Clobenpropit protects propofol-induced apoptosis of hippocampal neurons through PI3K/AKT pathway. |
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| DC75735 |
Ochratoxin-A |
Ochratoxin A (OTA) is a mycotoxin produced by several fungal species including Aspergillus ochraceus, A. carbonarius, A. niger and Penicillium verrucosum. OTA causes nephrotoxicity and renal tumors in a variety of animal species; however, human health effects are less well-characterized. Various studies have linked OTA exposure with the human diseases Balkan endemic nephropathy (BEN) and chronic interstitial nephropathy (CIN), as well as other renal diseases. |
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| DC75736 |
Selonsertib free base |
Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation. |
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| DC75737 |
ML109 |
ML-109, also known as CID-25246343 and (S)-(+)-NCGC00161870, is a potent and full thyroid stimulating hormone receptor (TSHR) agonist. ML109 is the first selective and orally available small-molecule TSHR agonist, and the probe will be a useful pharmacological tool to study TSHR biology in thyroidal and extrathyroidal tissues |
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| DC75738 |
Ibrutinib Interm 0441 |
Ibrutinib Interm 0441 is a piperidine derivative with an amine protecting group. It may be used in the preparation of biologically active compounds such as antagonists of the human P2X7 receptor and selective irreversible inhibitors for brutons tyrosine kinase. |
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| DC75739 |
Ipatasertib dihydrochloride |
Ipatasertib, also known as GDC-0068, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. |
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| DC75740 |
Elamipretide |
Elamipretide, also known as MTP 131, is a mitochondria-targeted peptide antioxidant. Elamipretide decreases inflammation and protect against a variety of neurological illnesses. Elamipretide (SS-31) improves mitochondrial dysfunction, synaptic and memory impairment induced by lipopolysaccharide in mice. Elamipretide Promotes Mitophagosome Formation and Prevents Its Reduction Induced by Nutrient Excess in INS1 β-cells. |
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| DC75741 |
J147 |
J147 is a potent neuroprotective and neurotrophic compound. J147 protects against neurotoxicity in cortical neurons in vitro (EC50 = 25 - 200 nM). J147. J147 reverses cognitive impairment in aged Alzheimer's disease mice. J147 is an exciting new compound that is extremely potent, safe in animal studies and orally active. J147 is a potential AD therapeutic due to its ability to provide immediate cognition benefits, and it also has the potential to halt and perhaps reverse disease progression in symptomatic animals as demonstrated in these studies. |
|
| DC75742 |
Bexagliflozin |
Bexagliflozin, also known as EGT1442, is a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. The IC(50) values for EGT1442 against human SGLT1 and SGLT2 are 5.6μM and 2nM, respectively. In normal rats and dogs a saturable urinary glucose excretion was produced with an ED(50) of 0.38 and 0.09mg/kg, respectively. EGT1442 showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients. |
|
| DC75743 |
Isavuconazonium sulfate |
Isavuconazole (BAL4815; trade name Cresemba) is a triazole antifungal drug. Its prodrug, isavuconazonium sulfate (BAL8557), was granted approval by the U.S. Food and Drug Administration (FDA) on March 6, 2015. Isavuconazole has been approved for treatment of invasive aspergillosis and invasive mucormycosis in adults ages 18 years and older. Both infections are caused by mold and fungi common to the environment, and occur in individuals who are immunosuppressed or have other complicating conditions, such as diabetes or lung disease. |
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| DC75744 |
Vesatolimod |
Vesatolimod, also known as GS-9620, is a potent and oral agonist of Toll-like receptor-7 developed for finite treatment of chronic hepatitis B viral (HBV) infection, with the goal of inducing a liver-targeted antiviral effect without inducing the adverse effects associated with current systemic interferon-α (IFN-α) therapies. GS-9620 demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses. GS-9620 can induce a sustained antiviral response in the woodchuck model of CHB. |
|
| DC75745 |
Mitoxantrone free base |
Mitoxantrone is an anthraquinone that intercalates in DNA and inhibits topoisomerase II (IC50 = 5.3 μM), thus inhibiting cell proliferation. It also inhibits HIV-1 integrase (IC50 = 3.8 μM). Mitoxantrone is exported from cells in an ATP- and glutathione-dependent manner by multidrug resistance protein-1.4 Formulations containing mitoxantrone have been used in the treatment of cancer and multiple sclerosis. |
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| DC75746 |
Epirubicin free base |
Epirubicin is an anthracycline drug used for chemotherapy. It can be used in combination with other medications to treat breast cancer in patients who have had surgery to remove the tumor. Similarly to other anthracyclines, epirubicin acts by intercalating DNA strands. Intercalation results in complex formation which inhibits DNA and RNA synthesis. It also triggers DNA cleavage by topoisomerase II, resulting in mechanisms that lead to cell death. Binding to cell membranes and plasma proteins may be involved in the compound's cytotoxic effects. Epirubicin also generates free radicals that cause cell and DNA damage. |
|
| DC75747 |
Siponimod |
Siponimod, also known as BAF-312, is a a potent and orally selective S1P Receptor Modulator with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively. Development of sphingosine-1-phosphate receptor 1 (S1P1) modulators to dampen inflammation and its sequelae is becoming increasingly promising for treating medical conditions characterized by significant immunopathology. |
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