| DC75710 |
TWS-119 |
TWS-119 is a potent and selective inhibitor of glycogen synthase kinase-3β (IC50 = 30 nM). TWS119 could activate Wnt/β-catenin pathway and up-regulate the expression of CD62L in a dose-dependent manner, but it decreased the expression of CD107a. Glycogen synthase kinase (GSK)-3, a constitutively active serine-threonine kinase, acts as a key regulator of major signaling pathways, including the Wnt, Hedgehog, and Notch pathways. |
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| DC75711 |
RA371 |
RA371, a derivative of PTP1B-IN-8 (CAS#919091-61-5), is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor |
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| DC75712 |
UAMC-3203 |
UAMC-3203 is an inhibitor of ferroptosis for inhibition of erastin-induced ferroptosis in IMR-32 neuroblastoma cells. It decreases iron-induced plasma lactate dehydrogenase (LDH) levels in a mouse model of acute iron poisoning when administered at a dose of 20 µmol/kg. It is not toxic to mice following chronic administration of a 20 µmol/kg dose for four weeks. UAMC-3203 has increased solubility and a longer half-life in mouse, rat, and human microsomes and isolated plasma than the ferroptosis inhibitor ferrostatin-1. In an in silico membrane dynamics study, UAMC-3203 was incorporated into a phospholipid bilayer. |
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| DC75713 |
HKI-357 |
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation. |
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| DC75714 |
JAB-3068 free base |
JAB-3068, also known as HMN23485, SHP2-IN-6, is a potent SHP2 inhibitor. JAB-3068 targets, binds to and inhibits the activity of SHP2. This prevents SHP2-mediated signaling, inhibits MAPK signaling and prevents growth of SHP2-expressing tumor cells. SHP2, an oncoprotein overexpressed in a variety of cancer cell types, regulates cell survival, differentiation and proliferation through activation of the Ras-Raf-MEK-ERK signaling pathway. The Ras-MAPK pathway is often hyperactivated in cancer cells due to specific mutations and rearrangements and are dependent on SHP2 for their oncogenic signaling. SHP2 also regulates programmed cell death 1 (PD-1)-mediated signal transduction and is involved in immune checkpoint modulation. |
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| DC75715 |
ASP4132 tosylate |
ASP4132 is an AMPK activator with potential antineoplastic activity. Upon oral administration, ASP4132 affects oxidative phosphorylation in mitochondria of metabolically-active tumor cells, which reduces both energy production and tumor cell proliferation. Mitochondrial oxidative phosphorylation is hyperactivated in tumor cells and plays a key role in the promotion of tumor cell proliferation. |
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| DC75716 |
Danuglipron free acid |
Danuglipron, also known as PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor agonist (GLP-1R). WO 2019148044 (2019). |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| DC75727 |
CIN16645 |
CIN16645, also known as LP-01 lipid, is an ionizable lipid, IT is useful in lipid nanopparticle formulation for DNA and RNA vaccine delivery and Gene editing. CIN16645 was first reported in Novartis patent WO 2015095340A1. 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).. |
|
| 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. |
|
| 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. |
|
| DC75730 |
DT-2216 |
DT2216 is discontinued for commercial reasons. |
|
| 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. |
|
| DC75733 |
2-PMDQ |
2-PMDQ is a potent selective α1 antagonist. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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 |
|
| 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. |
|
| 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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