2759420-43-2
Chemical Structure
NU223612
- CAS No.: 2759420-43-2
- Formula:C49H55FN6O9
- Molecular Weight:890.99
IUPAC Name: toluene-3-d
InChIKey: PLYOHMQINGIYDN-MXPGEODHSA-N
SMILES: O=C([C@H](C)[C@@]1([H])CC[C@](C2=CC=NC3=CC=C(F)C=C23)([H])CC1)NC4=CC=C(OC5CCN(C(CCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)CC5)C=C4
Biological Activity: NU223612 is a cereblon (CRBN)-recruiting IDO1 PROTAC degrader, with a DC50 value of 0.329-0.5438 μM against human IDO1, and it is capable of penetrating the blood-brain barrier. NU223612 directly binds to IDO1, mediates the degradation of both wild-type and catalytically inactive mutant IDO1 proteins, and does not degrade TDO2. NU223612 inhibits IDO1-mediated enzymatic activity. NU223612 directly binds to CRBN and promotes the formation of a cooperative ternary complex with IDO1. NU223612 induces ubiquitin-dependent proteasomal degradation of the IDO1 protein. NU223612 suppresses IDO1-mediated non-enzymatic phosphorylation of NF-κB p65 and the DNA-binding activity of downstream transcription factors. NU223612 can be used in studies of glioblastoma (malignant glioma)[1].
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NU223612 | 99.41% | NU223612 is a cereblon (CRBN)-recruiting IDO1 PROTAC degrader, with a DC50 value of 0.329-0.5438 μM against human IDO1, and it is capable of penetrating the blood-brain barrier. NU223612 directly binds to IDO1, mediates the degradation of both wild-type and catalytically inactive mutant IDO1 proteins, and does not degrade TDO2. NU223612 inhibits IDO1-mediated enzymatic activity. NU223612 directly binds to CRBN and promotes the formation of a cooperative ternary complex with IDO1. NU223612 induces ubiquitin-dependent proteasomal degradation of the IDO1 protein. NU223612 suppresses IDO1-mediated non-enzymatic phosphorylation of NF-κB p65 and the DNA-binding activity of downstream transcription factors. NU223612 can be used in studies of glioblastoma (malignant glioma). | ||||||||||||||||||||
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