3031840-36-2
Chemical Structure
NEP162
- CAS No.: 3031840-36-2
- Formula:C50H56ClN11O3S
- Molecular Weight:926.57
IUPAC Name: 2-(((1H-indol-2-yl)methyl)amino)-N-((1s,4s)-4-(6-(3-(4-(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetyl)piperazin-1-yl)propoxy)-1H-benzo[d]imidazol-2-yl)cyclohexyl)acetamide
InChIKey: WIURLZYDRMMHFO-BPKRYYIFSA-N
SMILES: O=C(N[C@@H]1CC[C@H](C2=NC(C=CC(OCCCN3CCN(C(C[C@H]4C5=NN=C(C)N5C(SC(C)=C6C)=C6C(C7=CC=C(Cl)C=C7)=N4)=O)CC3)=C8)=C8N2)CC1)CNCC(N9)=CC%10=C9C=CC=C%10
Biological Activity: NEP162 is a BRD4 PROTAC degrader based on the E3 ubiquitin ligase GID4, with DC50 values of 1.2 μM and 1.6 μM in SW480 and U2OS cells, respectively, and a Kd value of 0.13 µM for GID4. NEP162 bridges the E3 ligase GID4 and BRD4 to form a ternary complex, promotes polyubiquitination and subsequent degradation of BRD4 via the ubiquitin-proteasome system, reduces the proliferation capacity of tumor cells and induces apoptosis. NEP162 can be used for research on cancers such as osteosarcoma, colorectal cancer and non-small cell lung cancer[1].
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NEP162 | NEP162 is a BRD4 PROTAC degrader based on the E3 ubiquitin ligase GID4, with DC50 values of 1.2 μM and 1.6 μM in SW480 and U2OS cells, respectively, and a Kd value of 0.13 µM for GID4. NEP162 bridges the E3 ligase GID4 and BRD4 to form a ternary complex, promotes polyubiquitination and subsequent degradation of BRD4 via the ubiquitin-proteasome system, reduces the proliferation capacity of tumor cells and induces apoptosis. NEP162 can be used for research on cancers such as osteosarcoma, colorectal cancer and non-small cell lung cancer. | |||||||||||||||||||||
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Keywords
