| DC75150 |
Hexamide |
Hexamide is a protein inhibitor. |
|
| DC75151 |
KG-5 |
KG-5 is an orally available PDGFRß and B-Raf allosteric inhibitor. |
|
| DC75152 |
Pexmetinib |
Pexmetinib, also known as ARRY-614, is an orally bioavailable small-molecule inhibitor of p38 and Tie2 kinases with potential antineoplastic, anti-inflammatory and antiangiogenic activities. p38/Tie2 kinase inhibitor Arry-614 binds to and inhibits the activities of p38 and Tie2 kinases, which may inhibit the production of proinflammatory cytokines and may decrease tumor angiogenesis and tumor cell growth and survival. p38 is a MAP kinase that is often upregulated in cancer cells, playing a crucial part in the production of a variety of cytokines involved in inflammation and cellular proliferation such as tumor necrosis factor (TNF) and interleukin (IL)-1 and -6. Tie2 is an endothelial cell specific receptor that is activated by angiopoietins, growth factors required for angiogenesis. |
|
| DC75153 |
Givinostat free base |
Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis.ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro. ITF2357 decreases surface CXCR4 and CCR5 expression on CD4(+) T-cells and monocytes and is superior to valproic acid for latent HIV-1 expression in vitro. |
|
| DC75154 |
Cenupatide TFA |
Cenupatide is an urokinase plasminogen activator receptor (uPAR) inhibitor drug candidate. Cenupatide inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of streptozotocin (STZ)-induced diabetes. Cenupatide was found to revert STZ-induced up-regulation of uPA levels and activity, while uPAR on podocytes and (s)uPAR were unaffected. In glomeruli, Cenupatide inhibited FPR2 expression suggesting that the drug may act downstream uPAR, and recovered the increased activity of the αvβ3 integrin/Rac-1 pathway indicating a major role of uPAR in regulating podocyte function. |
|
| DC75155 |
Enzastaurin free base |
Enzastaurin, also known as DB-102 and LY317615, is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden. |
|
| DC75156 |
Miransertib free base |
Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 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. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma. |
|
| DC75157 |
BMS-955176 free base |
GSK3532795, also known as BMS-955176, is a potent, orally active, second-generation HIV-1 maturation inhibitor (MI) that advanced through phase IIb clinical trials. GSK3532795 combines broad coverage of polymorphic viruses (EC50 <15 nM toward a panel of common polymorphisms representative of 96.5% HIV-1 subtype B virus) with a favorable pharmacokinetic profile in preclinical species. |
|
| DC75158 |
Abivertinib |
Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. Abivertinib may be a promising novel agent for AML, with potential for combination treatment with HHT. |
|
| DC75159 |
Aroplatin |
Aroplatin is a synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotoxicity. Because DNA mismatch-repair (MMR) complexes do not recognize DACH–platinum adducts, DNA repair mechanisms are inhibited, overcoming limitations observed with other platinum-based agents. In addition, the liposomal encapsulation improves the bioavailability of NDDP and reduces its toxicity profile. |
|
| DC75160 |
Sivelestat Sodium hydrate |
Sivelestat Sodium is an inhibitor of human neutrophil elastase. |
|
| DC75161 |
EP6 |
EP6 is a 5-lipoxygenase (5-LO) inhibitor. 5-LO is a crucial enzyme of the arachidonic acid (AA) cascade and catalyzes the formation of bioactive leukotrienes (LTs) which are involved in inflammatory diseases and allergic reactions. |
|
| DC75162 |
Bromazine HCl |
Bromazine (trade names Ambodryl, Ambrodil and others), also known as bromodiphenhydramine, is an antihistamine and anticholinergic. It is a brominated form of diphenhydramine. |
|
| DC75163 |
Carotegrast methyl free base |
Carotegrast methyl, also known as AJM300 and PTC-100, is an orally-active small molecule that antagonises the α4 integrin receptor. AJM300 reduces inflammation by blocking leucocyte trafficking. Oral treatment with AJM300 dose-dependently inhibited lymphocyte homing to Peyer's patches and increased the peripheral lymphocyte count in the same dose range. AJM300 dose-dependently prevented the development of experimental colitis in mice. |
|
| DC75164 |
Anaxirone |
Anaxirone is a synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis. This agent has been shown to exhibit a broad spectrum of antineoplastic activity against experimental tumors, including those resistant to other alkylating agents. |
|
| DC75165 |
Anlotinib HCl |
Anlotinib, also known as AL3818 and Catequentinib, is a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth. |
|
| DC75166 |
Berberine chloride |
Berberine chloride is a regulator of HuR in LPS-induced macrophages. It acts by decreasing iNOS mRNA stability, and is an antineoplastic, radiosensitizing, anti-inflammatory, anti-lipidemic and antidiabetic agent. |
|
| DC75167 |
Avatrombopag free base |
Avatrombopag, also known as AKR-501, YM477, AS 1670542 or E5501, is a novel orally-active thrombopoietin (TPO) receptor agonist. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and maturation of megakaryocytes just as rhTPO did. AKR-501 may be useful in the treatment of patients with thrombocytopenia. Avatrombopag was first approved in 2018. |
|
| DC75168 |
Nazartinib |
Nazartinib, also known as EGF816 and NVS-816, is an orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. EGF816 covalently binds to and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGF816 preferentially inhibits mutated forms of EGFR including T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase inhibitors. |
|
| DC75169 |
Afatinib free base |
Afatinib, also know as BIBW 2992, is an orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. EGFR/HER2 tyrosine kinase inhibitor BIBW 2992 irreversibly binds to and inhibits human epidermal growth factor receptors 1 and 2 (EGFR-1; HER2), which may result in the inhibition of tumor growth and angiogenesis. EGFR/HER2 are RTKs that belong to the EGFR superfamily; both play major roles in tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types. Afatinib is approved in much of the world (including the United States, Canada, the United Kingdom and Australia) for the treatment of metastatic non-small cell lung carcinoma (NSCLC), developed by Boehringer Ingelheim. It acts as an angiokinase inhibitor. |
|
| DC75170 |
Eflornithine free base |
Eflornithine, also known as Difluoromethylornithine, is a difluoromethylated ornithine compound with antineoplastic activity. Eflornithine irreversibly inhibits ornithine decarboxylase, an enzyme required for polyamine biosynthesis, thereby inhibiting the formation and proliferation of tumor cells. Polyamines are involved in nucleosome oligomerization and DNA conformation, creating a chromatin environment that stimulates neoplastic transformation of cells. This agent has been shown to induce apoptosis in leiomyoma cells. |
|
| DC75171 |
Laninamivir free base |
Laninamivir, also known as CS-8958, is a neuraminidase inhibitor that is a drug used for the treatment and prophylaxis of Influenzavirus A and Influenzavirus B. It is a long-acting neuraminidase inhibitor administered by nasal inhalation. Laninamivir was approved for influenza treatment in Japan in 2010 and for prophylaxis in 2013 |
|
| DC75172 |
AC430 |
AC430 is a potent and specific small molecule inhibitor of janus kinase 2 (JAK2), which has been implicated as a target for therapy in both oncology and autoimmune disease. AC430 is currently being developed by Ambit. In preclinical studies, AC430 has exhibited potency against JAK2 and V617F mutated JAK2 in cell-based models that is at least equivalent to, and in most cases superior to, competing JAK2 inhibitors. In preclinical oncology and autoimmune models, AC430 is well tolerated and has significant efficacy at oral doses as low as 10 mg/kg/day. |
|
| DC75173 |
Navitoclax |
Navitoclax, also known as ABT-263, is an orally bioavailable, synthetic small-molecule antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. ABT-263 selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w and prevents their binding to the apoptotic effectors Bax and Bak proteins, which may trigger apoptosis in tumor cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. |
|
| DC75174 |
GSK-J4 free base |
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). |
|
| DC75175 |
Difetarsone |
Difetarsone is an antiprotozoal agent. Various studies have shown it to be particularly effective against Trichuris trichiura, commonly known as the whipworm. It has also been used to treat Entamoeba histolytica infections. Prior to the drugs use in the early 1970s, there were few effective treatments for this infection. Difetarsone often has minor side effects, which include rashes, nausea and vomiting. It has also resulted in angioedema in at least one known case. |
|
| DC75176 |
ML120B free base |
ML120B is a selective inhibitor of IKKbeta, which is essential for inflammatory cytokine-induced activation of nuclear factor kappaB (NF-kappaB). NF-kappaB plays a pivotal role in the function of major cell types that contribute to the pathophysiological process of rheumatoid arthritis (RA). |
|
| DC75177 |
Dilmapimod |
Dilmapimod, also known as SB-681323 and GW-681323 , is p38 MAPK inhibitor. SB-681323 inhibited the p38 MAPK pathway to a greater degree than prednisolone did. SB-681323 inhibited TNF-alpha production. SB-681323 is a potent p38 MAPK inhibitor that potentially suppresses inflammation in COPD. The treatment with SB-681832 is a safe and effective means of reducing hsCRP in patients undergoing elective PCI. |
|
| DC75178 |
Hydroxychloroquine sulfate |
Hydroxychloroquine is an autophagy inhibitor. It acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR9. Hydroxychloroquine (HCQ) is a medication used to prevent and treat malaria in areas where malaria remains sensitive to chloroquine. Other uses include treatment of rheumatoid arthritis, lupus, and porphyria cutanea tarda. It is taken by mouth. It is also being studied as an experimental treatment for coronavirus disease 2019 (COVID-19). |
|
| DC75179 |
Rosmanol |
Rosmanol is a natural polyphenol from the herb rosemary (Rosmarinus officinalis L.) with high antioxidant activity. |
|
