790245-61-3
Chemical Structure
NCT02
- CAS No.: 790245-61-3
- Formula:C17H16N2O2S
- Molecular Weight:312.39
IUPAC Name: 2-(6,7-dihydro-5H-indeno[5,6-b]furan-3-yl)-N-(5-methylthiazol-2-yl)acetamide
InChIKey: IELCYEUTXLYDOV-UHFFFAOYSA-N
SMILES: O=C(NC1=NC=C(C)S1)CC2=COC3=CC4=C(CCC4)C=C32
Biological Activity: NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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NCT02 | 98.14% | NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models. | ||||||||||||||||||||
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- [1]. Dieter SM, et al. Degradation of CCNK/CDK12 is a druggable vulnerability of colorectal cancer. Cell Rep. 2021;36(3):109394. [Content Brief]
- [2]. Lei P, et al. Current progress and novel strategies that target CDK12 for drug discovery. Eur J Med Chem. 2022 Oct 5;240:114603. [Content Brief]
- [3]. Weagel E G, et al. Molecular glues: enhanced protein-protein interactions and cell proteome editing. Medicinal Chemistry Research, 2022, 31(7): 1068-1087.
Keywords
