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Chemical Structure : YJ1206
Catalog No.: PC-23149Not For Human Use, Lab Use Only.
YJ1206 is a selective, orally bioavailable CDK12/13 PROTAC degrader, shows potent degradation effects and inhibits VCaP cell viability (IC50=12.5 nM).
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YJ1206 is a selective, orally bioavailable CDK12/13 PROTAC degrader, shows potent degradation effects and inhibits VCaP cell viability (IC50=12.5 nM).
YJ1206 demonstrated the best PK properties, with a bioavailability over 39% by oral gavage.
YJ1206 treatment significantly increased the transcripts at the TSSs in VCaP cells, while a distinct reduction toward the TESs of the long genes ATM and ATR was observed in a time-dependent manner.
YJ1206 combined with AKT inhibitors (uprosertib, capivasertib, and MK2206) triggers a synergistic effect in vitro, The combination regimen of CDK12/13 degraders with AKT inhibitors suppresses tumor growth in vivo.
| M.Wt | 867.94 | |
| Formula | C47H46FN9O7 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Chang Y, et al. Cell Rep Med. 2024 Sep 21:101752. doi: 10.1016/j.xcrm.2024.101752.
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