About 32 results found for searched term "CK1-IN-2" (0.068 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M41415 | CK1-IN-2 | Casein Kinase |
| CK1-IN-2 is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively. | ||
| M49883 | Nickel,dibromo[1,2-ethanediylbis[diphenylphosphine-kP]]-, (SP-4-2)- (9CI) | Others |
| Nickel,dibromo[1,2-ethanediylbis[diphenylphosphine-kP]]-, (SP-4-2)- (9CI) | ||
| M1764 | PF-477736 | Checkpoint |
| PF-0044736 | ||
| PF-477736 is a selective checkpoint kinase 1 (Chk1) inhibitor with Ki values of 0.49 nM and 47 nM for CHK1 and CHK2 respectively. | ||
| 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. | ||
| M1923 | Lonidamine | CFTR |
| AF 1890；Diclondazolic Acid; DICA | ||
| Lonidamine (AF-1890) is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki=2.5 μM). | ||
| M2071 | ONX-0914 | Proteasome |
| PR-957 | ||
| Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation. | ||
| M2087 | HC-030031 | TRP Channel |
| HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 = 6.2 and 5.3 μM, respectively). | ||
| M2954 | PPADS Tetrasodium | P2 Receptor |
| PPADS tetrasodium salt is a non-selective P2 purinergic antagonist blocking recombinant P2X1, P2X2, P2X3, P2X5 with IC50 of 1-2.6 μM, native P2Y2-like with IC50 of ~ 0.9 mM, and recombinant P2Y4 receptors with IC50 of ~ 15 mM | ||
| M45283 | BTX161 | Casein Kinase |
| BTX161 is a Thalidomide analog and potent CKIα degrader.BTX161 mediates the degradation of CKIα better than Lenalidomide and activates the DNA damage response (DDR) and p53 while stabilizing the p53 antagonist MDM2 in human AML cells. | ||
| M4079 | (R)Ginsenoside-Rh2 | MMP |
| 20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as an anti-proliferative agent in cells. It has anticancer effects by blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis and has anti-inflammatory and antioxidant activities. 20(R)-Ginsenoside Rh2 inhibited the replication and proliferation of mouse and human γ herpevirus 68 (MHV-68) with an IC50 of 2.77 μM against mouse MHV-68. | ||
| M4090 | Ginsenoside-Rg5 | IGF-1R |
| Ginsenoside Rg5 is the main ingredient of red ginseng. Ginsenoside Rg5 blocks the binding of IGF-1 to its receptor with an IC50 of about 90 nM. Ginsenoside Rg5 also inhibited COX-2 mRNA expression by inhibiting DNA binding activity of NF-κB P65. | ||
| M4244 | Schizandrin-A | Cytochrome P450 (e.g. CYP17) |
| Schizandrin-A; Wuweizisu-A; Deoxyschizandrin | ||
| Schizandrin-A, a lignan from Schisandra chinensis, is also a novel heat shock factor 1 (HSF1) inhibitor that effectively inhibits the induction of HSF1 target proteins such as heat shock protein 70 (HSP70) and HSP27. In addition, Schizandrin-A also regulates lipid metabolism and oxidative stress and possesses neuroprotective activity. | ||
| M5144 | BMS202 | PD-1/PD-L1 |
| PD-1/PD-L1 inhibitor 2 | ||
| Bms-202 is an effective non-peptide PD-1/PD-L complex inhibitor with IC50 of 18 nM and KD of 8 μM. Bms-202 directly binds to PD-L1 and blocks the human PD-1/PD-L interaction. Bms-202 has antitumor activity. | ||
| M5168 | GSK269962A | ROCK |
| GSK 269962 | ||
| GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. | ||
| M5268 | Umbralisib | PI3K |
| TGR-1202; RP5264 | ||
| Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. | ||
| M5341 | TBB | Casein Kinase |
| NSC 231634; TBB (enzyme inhibitor) | ||
| TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively). | ||
| M5923 | Rebamipide | COX |
| OPC-12759 | ||
| Rebamipide (OPC12759) is a cholecystokinin-1 (CCK1) receptor inhibitor that inhibits [125I]BH-CCK-8S with an IC50 of 37.7 μM. Rebamipide is an orally effective gastroprotective agent. Rebamipide enhances the production of endogenous PGs (particularly intragastric PGE2) by inducing COX-2 expression, thereby protecting the gastric mucosa from injury. Rebamipide also has anti-proliferative activity against gastric cancer cells. | ||
| M6102 | Pembrolizumab | PD-1/PD-L1 |
| Lambrolizumab; MK-3475 | ||
| Pembrolizumab (pembrolizumab) is a humanized anti-PD-1 monoclonal antibody that blocks the interaction between PD-1 and its ligands PD-L1 and PD-L2. It has immune checkpoint inhibitory activity and antitumor activity. MW: 146.286 KD.(Pembrolizumab does not recognize murine PD-1 protein, humanized mice or mice expressing human PD-1 gene are required). | ||
| M6291 | 5-Iodotubercidin | PKA |
| NSC 113939, 5-ITu | ||
| 5-IOdotubercidin (NSC 113939), an ATP analogue, is a potent inhibitor of adenosine kinase with an IC50 value of 26 nM. 5-IOdotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by activating phosphorylase and glycogen synthase. 5-IOdotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin inhibitors. | ||
| M6420 | AIM-100 | Others |
| AIM100 | ||
| AIM-100 is a potent and selective Ack1 (TNK2) inhibitor (IC50 = 22 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. | ||
| M7041 | NPPB | Chloride Channel |
| Hoechst 144; HOE 144 | ||
| NPPB is a blocker of the outwardly rectifying chloride channel (ORCC) with IC50 of 80 nM. NPPB has been shown to activate the GPR35-Gαi/o and GPR35-Gα16 pathways in HEK293 cells, inducing intracellular calcium mobilization. | ||
| 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). | ||
| M7569 | AMG-47a | Src-bcr-Abl |
| AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice. | ||
| 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. | ||
| 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. | ||
| M8125 | Quinalizarin | Casein Kinase |
| Quinalizarin is a potent (IC50 = 110 nM), ATP-competitive, and highly selective (IC50 > 1 μM for CK1 and 72 other kinases) inhibitor of casein kinase II (CK2), with a Ki value of approximately 50 nM and an IC50 of 110 nM.Quinalizarin induces apoptosis in some cancer cells. Quinalizarin can induce apoptosis in some cancer cells.) | ||
| M8815 | Tyrphostin AG 1112 | Casein Kinase |
| Tyrphostin AG 1112 is a potent CK II inhibitor. In addition, Tyrphostin AG 1112 inhibited p210bcr-abl tyrosine kinase with IC50 values of 2 μM, 15 μM, and 20 μM against p210bcr-abl, EGFR, and PDGFR kinases, respectively, in cells. | ||
| M8903 | SR-3029 | Casein Kinase |
| SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively. | ||
| 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. | ||
| M9359 | BAY-293 | Ras |
| BAY293 | ||
| BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1), blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. | ||
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