Indoleamine 2,3-Dioxygenase (IDO) Degrader
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PROTAC IDO1 Degrader-1
0 ImagesPROTAC IDO1 Degrader-1 is a potent IDO1 (Indoleamine 2,3-dioxygenase 1) PROTAC degrader with a DC50 of 2.84 μM. PROTAC IDO1 Degrader-1 forms a ternary complex with IDO1 and the CRBN E3 ligase, and induces polyubiquitination of IDO1 followed by proteasomal degradation via the ubiquitin-proteasome system. PROTAC IDO1 Degrader-1 is applicable for related research on cancer immunity.
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NU223612
0 ImagesNU223612 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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NU227326
0 ImagesCat. No.: HY-173066CAS No.: 3048196-52-4NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer.
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iDeg-6
0 ImagesCat. No.: HY-177785iDeg-6 is a molecular glue degrader that selectively targets IDO1, with a DC50 of 6.5 nM, an IC50 of 16 nM, and a Kd of 1.46 μM. iDeg-6 competes to bind the heme-binding site of apoprotein IDO1, promoting CRL2KLHDC3-mediated polyubiquitination of IDO1 and neddylation-modification-dependent proteasomal degradation. iDeg-6 reduces kynurenine production, abrogates the non-enzymatic pro-tumor migration function of IDO1, and inhibits tumor growth in immunodeficient mice. iDeg-6 can be used in studies of cancer, infection, and neurological diseases (such as melanoma).
