About 32 results found for searched term "CK2-IN-3" (0.093 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M45297 | CK2-IN-3 | Casein Kinase |
| CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM) with IC50 values of 1.51 μM (CK2α), 7.64 μM (CK2α') and can be used in cancer-related studies. | ||
| M45303 | CK2 inhibitor 3 | Casein Kinase |
| CK2 inhibitor 3 is a potent CK2 inhibitor with an IC50 of 280 nM that significantly affects tumor cell viability and exhibits significant selectivity for a panel of 320 kinases. | ||
| M1817 | Y-27632 dihydrochloride | ROCK |
| Y27632; Y-27632 2HCl | ||
| Y-27632 is a potent, selective inhibitor of Rho-associated protein kinases (ROCK) with IC50 values of 140-220 nM for ROCK1 and ROCK2. In addition, Y-27632 inhibited LPA-induced entosis. | ||
| M2523 | CK-636 | Actin-Related Protein |
| CK-0944636 | ||
| CK-636 is an Arp2/3 complex inhibitor with IC50 of 4 μM, 24 μM and 32 μM for inhibition of actin polymerization induced by human, fission yeast and bovine Arp2/3 complex, respectively. | ||
| M3486 | NPS-2143 | Calcium-sensing Receptor |
| SB262470 | ||
| NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. | ||
| M4138 | Deucravacitinib (BMS-986165) | JAK |
| BMS986165 | ||
| Deucravacitinib (BMS-986165) is a first-in-class, selective, orally bioavailable inhibitor of TYK2 transitions.Deucravacitinib selectively binds the TYK2 pseudokinase (JH2) structural domain with an IC50 of 1.0 nM and a Ki value of 0.02 nM. Deucravacitinib (BMS-986165) blocks receptor-mediated Tyk2 activation by stably regulating the JH2 structural domain. deucravacitinib also inhibits the IL-12/23 and type I IFN pathways. deucravacitinib may be used in psoriasis research. | ||
| M5123 | Y-39983 dihydrochloride | ROCK |
| Y-33075 dihydrochloride | ||
| Y-39983 (Y-33075) dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM, derived from Y-27632, inhibited ROCK more potently than Y-27632. | ||
| M5156 | CCT241533 hydrochloride | Checkpoint |
| CCT241533 HCl | ||
| CCT241533 hydrochloride is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM. | ||
| M6611 | CK 666 | Actin-Related Protein |
| Ck-666 is a cell-permeable inhibitor (IC50=12 μM) of the Arp2/3 complex, which binds to the Arp2/3 complex and stabilizes the inactive state of the complex, preventing the movement of Arp2 and Arp3 subunits into the active filamentous conformation. | ||
| M6970 | ML171 | NADPH Oxidase |
| 2-Acetylphenothiazine; 2-APT | ||
| ML171 is a potent and selective inhibitor of NADPH-oxidase with IC50s of 0.25 μM, 5 μM, 3μM, 5 μM and 5.5 μM for NOX1, NOX2, NOX3, NOX4 and xanthine oxidase, respectively. ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay. | ||
| M7327 | Lintitript | Cholecystokinin Receptor |
| SR 27897 | ||
| Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC50 of 6 nM and a Ki of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC50 value of 200 nM). | ||
| M7725 | CK-548 | Others |
| CK-548 inhibits the activity of actin-related protein (Arp)2/3 complex by inserting into the hydrophobic core of Arp3 and altering its conformation: inhibits. | ||
| M7790 | Emodin | Casein Kinase |
| Frangula emodin | ||
| Emodin is an anti-SARS-CoV compound that blocks the interaction between the SARS-coronavirus spike protein and angiotensin converting enzyme 2 (ACE2). Emodin inhibited casein kinase 2 (CK2) and 11β-HSD1. Emodin can also induce necrotic apoptosis of glioma U251 cells and inhibit U251 cell proliferation by targeting the TNF/RIPK1/RIPK3 signaling pathway. | ||
| M8090 | PF-04965842 | JAK |
| Abrocitinib | ||
| Abrocitinib is an orally active and selective JAK1 inhibitor with an IC50 value of 29 nM. Abrocitinib reversibly inhibits JAK1 kinase by blocking its ATP-binding site. Abrocitinib (PF-04965842) inhibited TYK2 activity (IC50, 1.253 μM) and phosphorylation of STAT1, STAT3, and STAT5 after stimulation. It can be used in the study of autoimmune diseases. | ||
| M8121 | PD-85639 | Others |
| PD-85639 (PD85,639) is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1. | ||
| M8747 | Synta66 | Calcium Channel |
| Synta66 (S66) is a CRAC (Ca2+ release-activated Ca2+) channel inhibitor that blocks SOCE (store-operated Ca2+ entry) upon Ca2+ depletion from intracellular stores by thapsigargin in human vascular smooth muscle cells (VSMCs) with high potency (IC50 = 26 nM & 43 nM based on maximum Ca2+ level & rate of increase, respectly). | ||
| M9298 | AX-024 hydrochloride | Immunology/Inflammation |
| AX-024 HCl | ||
| Ax-024 Hydrochloride is orally available, the first tCR-NCK interaction inhibitor that selectively inhibits TCR-induced T cell activation with an IC50 value of 1 nM. Ax-024 Hydrochloride regulates cellular signaling by targeting the SH3 domain. Ax-024 Hydrochloride has the characteristics of low toxicity, high efficiency and high selectivity. | ||
| M10654 | Ajmalicine (Raubasine) | Adrenergic Receptor |
| Raubasine | ||
| Ajmalicine (Raubasine) is an adrenolytic agent which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor. Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM. | ||
| M10781 | Alrizomadlin | Mdm2 |
| APG-115; AA-115 | ||
| Alrizomadlin (APG-115) is an oral active small molecule MDM2 protein inhibitor that binds to MDM2 protein.IC50 value and Ki The values are 3.8 nM and 1 nM, respectively. Alrizomadlin blocks MDM2 interaction with p53 and induces cell cycle arrest and apoptosis in a p53-dependent manner. | ||
| M10782 | APG-1387 | IAP |
| APG-1387 is a divalent SMAC mimetic that is an IAP antagonist that blocks the activity of the IAP family of proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins as well as caspase-3 activation and PARP lysis, leading to apoptosis. APG-1387 can be used for the study of hepatocellular carcinoma, ovarian cancer and nasopharyngeal carcinoma. | ||
| M10878 | Reldesemtiv | Others |
| CK-2127107 | ||
| Reldesemtiv (CK-2127107) is a selective, orally active next-generation rapid skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates rapid skeletal muscle fibrils, EC50Is 3.4 μM. | ||
| M21033 | CK1-IN-1 | Casein Kinase |
| PUN51207, Compound 1C | ||
| CK1-IN-1 (PUN51207, Compound 1C) is an inhibitor of casein kinase 1 (CK1) with IC50 of 15 nM, 16 nM and 73 nM for CK1δ, CK1ε and p38α MAPK, respectively. | ||
| M21591 | RLX-33 | RXFP |
| RLX-33 is a potent and selective blood-brain barrier permeable relaxin family peptide 3 (RXFP3) antagonist that also blocks relaxin 3 (Relaxin 3) -induced ERK1/2 phosphorylation. The IC50 phosphorylated RXFP3, ERK1 and ERK2 were 2.36μM, 7.82μM and 13.86μM, respectively. RLX-33 can block the increase of food intake in rats induced by RXFP3 selective agonist R3/I5. RLX-33 can be used in the study of metabolic syndrome. | ||
| M21647 | MB710 | Mdm2 |
| MB-710 | ||
| MB710 is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM. MB710 shows anticancer activity in p53-Y220C cell lines. | ||
| M22519 | Prostaglandin A2 | Metabolite/Endogenous Metabolite |
| PGA2; Medullin | ||
| Prostaglandin A2 (PGA2) is a endogenous metabolite derived from arachidonic acid, it plays a vital role in the induction of apoptosis. Prostaglandin A2 blocks the cell cycle progression of NIH 3T3 cells at the G1 and G2/M phase. Prostaglandin A2 induces p53-dependent apoptosis. | ||
| M28240 | AZD4320 | Bcl-2 |
| AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively. | ||
| M28750 | CD532 | Aurora Kinase |
| CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer. | ||
| M28890 | WCK-4234 | Antibiotic |
| WCK-4234 is a potent β-lactamase inhibitor. WCK-4234 inhibits class A, C, and D β-lactamases activity. WCK-4234 lacks direct antibacterial activity. WCK-4234 potentiates imipenem and meropenem against Enterobacteriaceae with OXA-48/OXA-181 or KPC enzymes, or with combinations of impermeability and AmpC or ESBL activity. WCK-4234 distinctively overcomes resistance mediated by OXA-type carbapenemases. | ||
| M28960 | CPUY201112 | HSP |
| CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research. | ||
| M29195 | Nastorazepide | Cholecystokinin Receptor |
| Z-360 | ||
| Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Target：CCK-2 in vitro: Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. Check for active clinical trials or closed clinical trials using this agent. in vivo: Z-360 is a novel orally active CCK-2/gastrin receptor antagonist, significantly inhibits the growth of subcutaneous xenografts of human pancreatic tumor cells in mice, and that Z-360 combined with gemcitabine prolonged survival in a pancreatic carcinoma orthotopic xenograft mice. | ||
| M29455 | DDO-7263 | Keap1-Nrf2 |
| DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD). | ||
| M29943 | T-2 Triol | Metabolite/Endogenous Metabolite |
| T-2 Triol is a trichothecene mycotoxin derived by the metabolism of T-2 toxin. It is less toxic than T-2 toxin. T-2 Triol major metabolites are evaluated in broiler chickens with Half-lives (t1/2λz), Peak plasma concentrations (Cmax) and Tmax values of 9.6 mins, 563 ng/ml , 2.5 mins, respectively. | ||
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