| DC75702 |
AG-045572 |
AG-045572 is a selective gonadotropin-releasing hormone (GnRH) receptor antagonist that suppresses testosterone and luteinising hormone (LH) levels in vivo. |
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| DC75703 |
Minocycline HCl |
Minocycline (INN) is a broad-spectrum tetracycline antibiotic, and has a broader spectrum than the other members of the group. It is a bacteriostatic antibiotic, classified as a long-acting type. As a result of its long half-life it generally has serum levels 2–4 times that of the simple water-soluble tetracyclines (150 mg giving 16 times the activity levels compared with 1 g of tetracycline at 24–48 hours). Minocycline is the most lipid-soluble of the tetracycline-class antibiotics, giving it the greatest penetration into the prostate and brain. Minocycline is not a naturally-occurring antibiotic, but was synthesized semi-synthetically from natural tetracycline antibiotics by Lederle Laboratories in 1966. (https://en.wikipedia.org/wiki/Minocycline) ) |
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| DC75704 |
P7C3A20-analog |
P7C3A20-analog, as known as defluoro-P7C3-A20, is a structural analogue of P7C3-A20. Compared to P7C3-A20 structure, P7C3-A20 analog has no fluorine atom in the 1,3-diaminopropane-bridge. P7C3-A20 analog was synthesized by mistake during a process to make P7C3-A20. The bioactivity of P7C3-A20 analog is unknown. P7C3-A20 analog may be used for research to compare with P7C3-A20. P7C3-A20 is a proneurogenic, neuroprotective agent. P7C3-A20 displayed increased activity and an improved toxicity profile compared to P7C3. P7C3-A20 demonstrated greater proneurogenic efficacy than a wide spectrum of currently marketed antidepressant drugs. P7C3-A20 showed neuroprotective properties in rodent models of Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury and age-related cognitive decline. |
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| DC75705 |
ANR-94 |
ANR-94 is an adenosine A2A receptor (AA2AR) antagonist that displays activity in the treatment of Parkinson's disease in vivo, improves parkinsonian motor deficits and tremors, and exhibits neuroprotective and anti-inflammatory effects. |
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| DC75706 |
CCRP2 |
CCRP2, also known as TLX agonist 1 and SUN23314, is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity. CCRP2 was reported in PLoS One . 2014 Jun 17;9(6):e99440. |
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| DC75707 |
(±)-AC 7954 hydrochloride |
(±)-AC 7954 hydrochloride is a selective nonpeptidic druglike urotensin-II receptor agonist. |
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| DC75708 |
NG-25 HCl |
NG-25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer. |
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| DC75709 |
IKK-16 (free base) |
IKK-16 is a potent and slective inhibitor of IκB kinase (IKK) (IC50 values are 40, 70 and 200 nM for IKKβ, IKK complex and IKKα respectively). KK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. |
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| 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). |
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| 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. |
|
| 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).. |
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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. |
|
| 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. |
|
| DC75731 |
EPZ-025654 |
EPZ-025654 is a potent and selective arginine methyltransferase CARM1 inhibitor. |
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