| DC75485 |
RX821002 HCl |
RX821002 is a potent, selective α2-adrenoceptor antagonist with very low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively). |
|
| DC75486 |
Importazole free base |
Importazole is a small molecule inhibitor of the transport receptor importin-β. Importazole specifically inhibits the function of importin-β, likely by altering its interaction with RanGTP. Importazole is a valuable tool to evaluate the function of the importin-β/RanGTP pathway at specific stages during the cell cycle. |
|
| DC75487 |
GDC0575 monohydrochloride |
GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis. |
|
| DC75488 |
RS 67333 HCl |
RS 67333 is a potent and highly selective 5-HT4 partial agonist, with pKi values of 8.7 at 5-HT4 sites in guinea pig striatum and > 6 at various other receptors, including 5-HT1A, 1D, 2A, 2C, D1, D2 and M1-3. RS 67333 HCl is active in vivo, with an intrinsic activity relative to 5-HT of 0.5. |
|
| DC75489 |
NLX-101 |
NLX-101, also known as F-15,599, is a novel compound that activates serotonin 5-HT1A receptors with exceptional selectivity, having over 1000-fold higher affinity for this target over other receptors. In addition, NLX-101 is a 'biased agonist' at 5-HT1A receptors, preferentially activating 5-HT1A receptors in those brain regions that control mood and cognition. |
|
| DC75490 |
NKY80 |
NKY80 is a inhibitor of adenylyl cyclase (AC). NKY80 exhibits greater affinity for AC5 over AC3 and AC2 (IC50 values are 8.3 μM, 132 μM and 1.7 mM respectively). |
|
| DC75491 |
RS 100329 HCl |
RS 100329 is a subtype-selective α1A-adrenoceptor antagonist (pKi = 9.6 for human cloned α1A receptors). RS 100329 displays 126- and 50-fold selectivity over human α1B and α1D receptors respectively. |
|
| DC75492 |
Rimonabant free base |
Rimonabant, also known as SR141716 and A 281, is an anorectic anti-obesity drug. It is an inverse agonist for the cannabinoid receptor CB1. Its main avenue of effect is reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States. |
|
| DC75493 |
E4031 HCl |
E4031 selectively blocks hERG K+ channels. E4031 inhibits the rapid delayed-rectifier K+ current (IKr) and reversibly prolongs action potential duration in guinea pig papillary muscle and isolated ventricular myocytes, without affecting Na+ or Ca2+ inward currents. E4031 is a class III antiarrhythmic agent. |
|
| DC75494 |
SKF89976A free base |
SKF89976A is a potent GABA uptake inhibitor, which is selective for GAT-1 (IC50 values are 0.13, 550, 944 and 7210 μM for hGAT-1, rGAT-2, hGAT-3 and hBGT-1 respectively). SKF89976A inhibits transport current competitively (Ki = 7 μM) and transmitter-gated current non-competitively (Ki = 0.03 nM). It is able to pass the blood-brain barrier after systemic administration and is active in vivo. |
|
| DC75495 |
Olodaterol HCl |
Olodaterol, also known as BI 1744, is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim. Olodaterol was approved by FDA in 2014 for the treatment of chronic obstructive pulmonary disease. |
|
| DC75496 |
Imatinib free base |
Imatinib is a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Imatinib was approved for medical use in the United States in 2001. |
|
| DC75497 |
SB-258585 HCl |
SB-258585 HCl is a potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53). It displays over 100-fold selectivity for 5-HT6 over other 5-HT, dopamine, and α-adrenergic receptors. |
|
| DC75498 |
Tenapanor free base |
Tenapanor, also known as AZD-1722 and RDX 5791, is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney. Tenapanor possesses an excellent preclinical safety profile and, as of now, there are no serious concerns about its side effects. Tenapanor is currently in clinical trials. |
|
| DC75499 |
Nilotinib free base |
Nilotinib, also known as AMN107, is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia. Structurally related to imatinib, it was developed based on the structure of the Abl-imatinib complex to address imatinib intolerance and resistance. Nilotinib is a selective Bcr-Abl kinase inhibitor that is 10-30 fold more potent than imatinib in inhibiting Bcr-Abl tyrosine kinase activity and proliferation of Bcr-Abl expressing cells. Nolitinib was developed by Novartis and is sold under the trade name Tasigna. |
|
| DC75500 |
Tofacitinib citrate |
Tofacitinib, also known as tasocitinib, CP-690550, is a Janus kinase (JAK) inhibitor. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the in vitro activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC50 of 406, 56, and 1377 nM, respectively. |
|
| DC75501 |
MLN120B HCl |
MLN-120B is a potent and effective inhibitor of IκB kinase beta subunit (IKKβ) with IC50 value of 20 μM. MLN-120B blocks multiple myeloma cell growth in vitro and in vivo. |
|
| DC75502 |
1400W HCl |
1400W is a highly selective inducible nitric oxide synthase inhibitor and is a potential disease modifier in the rat kainate model of temporal lobe epilepsy. 1400W reduces ischemia reperfusion injury in an ex-vivo porcine model of the donation after circulatory death kidney donor. 1400W ameliorates acute hypobaric hypoxia/reoxygenation-induced cognitive deficits by suppressing the induction of inducible nitric oxide synthase in rat cerebral cortex microglia. 1400W blocks death pathway of LPS-induced activated-microglia to preOLs. |
|
| DC75503 |
Inarigivir soproxil |
Inarigivir soproxil, also known as SB 9200, is an antiviral agent. SB 9200 is also a novel agonist of innate immunity, which shows potent antiviral activity against resistant HCV variants. SB 9200 has broad-spectrum antiviral activity against RNA viruses including hepatitis C virus (HCV), norovirus, respiratory syncytial virus, and influenza and has demonstrated activity against hepatitis B virus (HBV) in vitro and in vivo. In phase I clinical trials in chronically infected HCV patients, SB 9200 has been shown to reduce HCV RNA by up to 1.9 log10 . |
|
| DC75504 |
Ribociclib succinate |
Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. |
|
| DC75505 |
CHIR99021 HCl |
CHIR99021, also known as CT99021, is a glycogen synthase kinase 3β (GSK3β) inhibitor that has antiproliferative activity in vitro and in vivo. CHIR-99021 inhibits GSK-3 with IC50 at 7 nM. In a series of carcinoma cell lines, the IC50 of CHIR99021 for proliferation is about 10μM. CHIR99021 promotes self-renewal of mouse embryonic stem cells by modulation of protein-encoding gene and long intergenic non-coding RNA expression. |
|
| DC75506 |
ML355 free base |
ML355 is a potent and selective inhibitor of human 12-lipoxygenase. |
|
| DC75507 |
Ilginatinib maleate |
Ilginatinib, also known as NS-018, is a selective JAK2 inhibitor. Ilginatinib preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. NS-018 suppressed the phosphorylation of STAT3 in colony-forming cells from MDS patients. NS-018 reduces myeloma cell proliferation and suppresses osteolysis through inhibition of the JAK2 and Src signaling pathways. |
|
| DC75508 |
BAY-1895344 HCl |
Elimusertib, also known as BAY-1895344, is a potent and selective ATM inhibitor. BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride. |
|
| DC75509 |
9-Hydroxyellipticin free base |
9-hydroxyellipticine, also known as IGIG 929 and LS133324, is a potent cytotoxic and antitumor agent. Structurally, 9-hydroxyellipticine is a 9-hydroxy derivative of ellipticine. The hydroxy group in 9-hydroxyellipticines increases the apparent affinity for DNA, stabilisation of toposiomerase II-DNA cleavable complex, oxidation to reactive quinone-imine intermediates, phosphorylation of p53 suppressor proteins and cytotoxicity relative to the parent ellipticines. |
|
| DC75510 |
Acecainide HCl |
Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. |
|
| DC75511 |
LY-3214996 |
LY-3214996, also known as Temuterkib, is a potent and selective, orally available inhibitor of extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity. Upon oral administration, LY3214996 inhibits both ERK 1 and 2, thereby preventing the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. |
|
| DC75512 |
WST-8 sodium |
WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity. At neutral pH and in the presence of the intermediate electron acceptor. |
|
| DC75513 |
OTSSP167 free base |
OTSSP167, also known as OTS167, is an orally available inhibitor of maternal embryonic leucine zipper kinase (MELK) with potential antineoplastic activity. Upon administration, OTS167 binds to MELK, which prevents both MELK phosphorylation and activation; thus inhibiting the phosphorylation of downstream MELK substrates. This may lead to an inhibition of both cell proliferation and survival in MELK-expressing tumor cells. |
|
| DC75514 |
GSK-3326595 |
Pemrametostat, also known as GSK-3326595 and EPZ015938, is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) that potently inhibits tumor growth in vitro and in vivo in animal models.GSK-3326595 halts proliferation and induces apoptosis in numerous solid and hematologic tumor cell lines. It has been shown to have potent anti-tumor activity in vivo in animal models. |
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