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Chemical Structure : KH-103
Catalog No.: PC-21533Not For Human Use, Lab Use Only.
KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PROTAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggering and crosstalk inhibition.
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KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PROTAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggering and crosstalk inhibition.
KH-103 (1 uM) led to efficient and rapid degradation of GR cells within less than an hour in HEK293 cells.
KH-103 shows highly efficient degradation at 10 nM, reaching almost full depletion at 100 nM.
KH-103 shows efficient reversible degradation in various in-vitro models across tissue origins and species.
KH-103 induces nuclear translocation without triggering GR-mediated gene activation.
KH-103 blocks dexamethasone (DEX) effects with increased efficiency compared to other inhibitors.
KH-103 treatment alone has no nonspecific transcriptional effects.
KH-103 effectively depletes GR in the pituitary in vivo and impacts corticosterone levels.
| M.Wt | 833.01 | |
| Formula | C46H61FN4O9 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Gazorpak M, et al. Nat Commun. 2023 Dec 9;14(1):8177.
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