About 33 results found for searched term "CK1-IN-1" (0.08 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| 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. | ||
| M43468 | Ack1 inhibitor 1 | ALK |
| Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. | ||
| M45300 | CK2/PIM1-IN-1 | Casein Kinase |
| CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1 with IC50 values of 3.787 μM and 4.327 μM for the effects of CK2 and PIM1, respectively.CAS 번호410483-84-5 | ||
| 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. | ||
| 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. | ||
| M2255 | Genistein | EGFR/HER2 |
| NPI 031L | ||
| Genistein is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM. | ||
| 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 | ||
| 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. | ||
| M4960 | RKI-1313 | ROCK |
| Inhibition of ROCK in human H1299 cells assessed as decrease in phosphorylation of MYPT-1 after 1 hr by Western immunoblotting assay. | ||
| 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. | ||
| 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). | ||
| M6625 | CP 339818 hydrochloride | Potassium Channel |
| CP 339818 hcl | ||
| CP 339818 hydrochloride is a non-peptide, potent KV1.3 channel blocker. CP 339818 hydrochloride potently blocks the C-type inactivated conformation of Kv1.3 and suppresses T cell activation. | ||
| 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. | ||
| M7123 | PF 5006739 | Casein Kinase |
| PF 5006739 is a potent, selective CK1δ/ε inhibitor with IC50s of 3.9 nM and 17.0 nM, respectively, and possesses low nanomolar CK1δ/ε potency in vitro and high kinome selectivity. In addition, PF-5006739 improves glucose tolerance in diet-induced obesity (DIO) and genetic (ob/ob) mouse models. It can be used in studies of psychiatric disorders. | ||
| 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). | ||
| M7603 | AP-18 | TRP Channel |
| AP18 | ||
| AP-18 is a selective TRPA1 channel blocker. AP-18 blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. | ||
| M7683 | CKI-7 dihydrochloride | Casein Kinase |
| CKI-7 is a CK1 inhibitor; also inhibits SGK, S6K1 and MSK1. | ||
| 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. | ||
| M8947 | PF-01247324 | Sodium Channel |
| PF-01247324 is a novel selective and orally bioavailable Nav 1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel. | ||
| M9355 | UNC2541 | Others |
| UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM). | ||
| 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. | ||
| M9416 | Durvalumab | PD-1/PD-L1 |
| MEDI 4736 | ||
| Durvalumab (MEDI 4736) is an humanized anti-PD-L1 monoclonal antibody, it completely blocks the binding of PD-L1 to both PD-1 and CD80, with IC50s of 0.1 and 0.04 nM, respectively. Durvalumab was inactive against the mPD-L1. | ||
| M9897 | GB1107 | Galectin |
| GB-1107 | ||
| GB1107 is a potent, selective, orally active galectin-3 inhibitor with Kd of 37 nM. GB1107 inhibits lung adenocarcinoma growth and augments response to PD-L1 blockade. GB1107 potentiates the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules. | ||
| M10129 | CCT245737 | Checkpoint |
| SRA737; PNT-737 | ||
| CCT245737 is a potent, selective and orally active checkpoint kinase 1 (CHK1) inhibitor, with IC50 values of 1.3 nM, 2440 nM and 30 nM for CHK1, CHK2 and G2 check point abrogation, respectively. | ||
| M10183 | Difopein TFA | Peptides |
| Difopein TFA is a specific and competitive inhibitor of 14-3-3 protein, blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. | ||
| M10561 | IMP-1088 | DNA/RNA Synthesis |
| IMP1088 | ||
| IMP-1088 is a novel potent and selective blocker of N-myristoylation in cells. IMP-1088 is also a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC50s of <1 nM for HsNMT1 and HsNMT2. | ||
| M10583 | RRX-001 | NLR |
| ABDNAZ | ||
| Rrx-001 is a hypoxic selective epigenetic factor that has been used as a radiation or chemotherapy sensitizer to induce apoptosis. Rrx-001 is an immune checkpoint inhibitor that down-regulates CD47 and SIRP-α. Rrx-001 is also an effective inhibitor of G6PD with strong antimalarial activity. Rrx-001 inhibits the expression of CD47 in tumor cells by inhibiting c-myC, a positive regulator of CD47. | ||
| M10707 | FIT-039 | CDK |
| FIT-039 is a selective, ATP-competitive, orally active CDK9 inhibitor against CKD9/cyclin T1 IC50 Is 5.8 μM. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits HSV-1 (IC50 is 0.69 μM), HSV-2, human adenovirus, and human CMV replication. FIT-039 is a promising antiviral agent that can be used to suppress resistant HSV and other DNA viruses. | ||
| 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. | ||
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