2901806-51-5
Chemical Structure
G-6599
- CAS No.: 2901806-51-5
- Formula:C31H37N7O
- Molecular Weight:523.67
InChIKey: FUAWFGGYXBISCX-UHFFFAOYSA-N
SMILES: OC1=CC=CC=C1C2=CC(N3CC4N(C5=CC(C#CCCN6CCCCCC6)=NC=C5)C(CC4)C3)=C(N)N=N2
Biological Activity: G-6599 is a covalent molecular glue degrader targeting SMARCA2/SMARCA4, with DC50 values of 0.017 nM and 0.057 nM against SMARCA2 and SMARCA4 in SW1573 cells, respectively. G-6599 exhibits proteome selectivity for SMARCA2, SMARCA4, and PBRM1. G-6599 induces the assembly of the SMARCA2-FBXO22 ternary complex, enabling ubiquitination and proteasomal degradation of both proteins via the ubiquitin-proteasome pathway without the need for biotransformation. G-6599 shows antiproliferative effects in relevant cancer cell models. G-6599 can be used for research on androgen-dependent prostate cancer and SMARCA4-mutant non-small cell lung cancer[1].
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G-6599 | 98.30% | G-6599 is a covalent molecular glue degrader targeting SMARCA2/SMARCA4, with DC50 values of 0.017 nM and 0.057 nM against SMARCA2 and SMARCA4 in SW1573 cells, respectively. G-6599 exhibits proteome selectivity for SMARCA2, SMARCA4, and PBRM1. G-6599 induces the assembly of the SMARCA2-FBXO22 ternary complex, enabling ubiquitination and proteasomal degradation of both proteins via the ubiquitin-proteasome pathway without the need for biotransformation. G-6599 shows antiproliferative effects in relevant cancer cell models. G-6599 can be used for research on androgen-dependent prostate cancer and SMARCA4-mutant non-small cell lung cancer. | ||||||||||||||||||||
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