395074-72-3
395074-72-3
Chemical Structure
GSK-3/CDK5/CDK2-IN-1
- CAS No.: 395074-72-3
- Formula:C21H22N4O2
- Molecular Weight:362.42
IUPAC Name: N-(1-((1s,3s)-3-acetamidocyclobutyl)-1H-imidazol-4-yl)-2-(naphthalen-2-yl)acetamide
InChIKey: XJRCZTVFSOVAQW-KDURUIRLSA-N
SMILES: O=C(NC1=CN([C@H]2C[C@@H](NC(C)=O)C2)C=N1)CC3=CC=C4C=CC=CC4=C3
Biological Activity: GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases[1].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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GSK-3/CDK5/CDK2-IN-1 | GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases. | |||||||||||||||||||||
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PNU-292137 | 99.95% | PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model. | ||||||||||||||||||||
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CDK5 inhibitor 20-223 | 99.62% | CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent. | ||||||||||||||||||||
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HDAC6-IN-9 | HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC50 values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities. | |||||||||||||||||||||
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RIOK2-IN-1 | RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression. | |||||||||||||||||||||
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hRIO2 kinase ligand-1 | 99.95% | hRIO2 kinase ligand-1 (compound 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM. | ||||||||||||||||||||
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Nafimidone | Nafimidone is a stable and brain-penetrant antiepileptic compound Nafimidone shows effective anticonvulsant effects in kindled amygdaloid seizure model. However, The effective window of Nafimidone is narrow, and has obvious epileptogenic effects at high doses. Nafimidone can be used for the study of epilepsy. | |||||||||||||||||||||
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Nafimidone hydrochloride | Nafimidone is a stable and brain-penetrant antiepileptic compound. Nafimidone shows effective anticonvulsant effects in kindled amygdaloid seizure model. Nafimidone exhibits the narrow effective window, and has obvious epileptogenic effects at high doses. Nafimidone can be used for the study of epilepsy. | |||||||||||||||||||||
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BAS-118 | BAS-118 is a benzamide derivative with antibacterial activity. The MIC50, MIC90 and MIC ranges of BAS-118 for 100 randomly selected isolates of Helicobacter pylori are ≤0.003, 0.013 and ≤0.003-0.025 mg/L, respectively. BAS-118 is promising for research of anti-H. pylori agent. | |||||||||||||||||||||
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E-2101 | E-2101 is a novel antispastic agent. E-2101 is a competitive CYP2C19 and CYP2D6 inhibitor with Ki values of 15 and 48 μM, respectively. E-2101 is metabolized by Cytochromes P450 to form monohydroxylated (M1 and M2), dihydroxylated (M3), and N-dealkylated metabolites (M4). E-2101 can be used in the research of skeletal muscle spasm. | |||||||||||||||||||||
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Gly-Phe-β-naphthylamide | 99.97% | Gly-Phe-β-naphthylamide is a substrate of Cathepsin C (HY-P2922) and belongs to the lysosomal agonist. Gly-Phe-β-naphthylamide can freely pass through the cell membrane and organelle membrane. Gly-Phe-β-naphthylamide will be specifically hydrolyzed by Cathepsin C, ultimately leading to a permeability lysis when it enters the acidic compartment. Gly-Phe-β-naphthylamide can be used to study lysosomal hydrolysis, lysosomal membrane permeability, and the function of cathepsin C. | ||||||||||||||||||||
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