Chemical Structure : HPK1 PROTAC 10m
CAS No.:
HPK1 PROTAC 10m
Catalog No.: PC-25213Not For Human Use, Lab Use Only.
HPK1 PROTAC 10m is a potent, selective and orally active HPK1 (MAP4K1) PROTAC degrader with DC50 of 5.0 nM, Dmax ≥ 99% in Jurkat cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
HPK1 PROTAC 10m is a potent, selective and orally active HPK1 (MAP4K1) PROTAC degrader with DC50 of 5.0 nM, Dmax ≥ 99% in Jurkat cells.
HPK1 PROTAC 10m (370 nM) potently degraded HPK1, achieved nearly complete elimination of HPK1.
HPK1 PROTAC 10m is ineffective in reducing the levels of other MAP4K family members, including germinal center kinase (GCK, MAP4K2), GLK and HPK1/GCK-like kinase (HGK, MAP4K4) proteins at 0.12-10 μM.
HPK1 PROTAC 10m is a bona fide CRBN-recruiting HPK1 PROTAC degrader.
HPK1 PROTAC 10m effectively enhanced TCR signal transduction and cytokine secretion in Jurkat cells and PBMCs.
HPK1 PROTAC 10m (0.5-3 mpk, PO, QOD) exhibited in vivo antitumor efficacy in MC38 xenograft mouse model. also improved the antitumor efficacy of anti-PD-1 likely through promoting the infiltration of CD8+ T cells into the TME.
Physicochemical Properties
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M.Wt
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795.91
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Formula
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C43H45N11O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-((4-(1-(((3S)-1-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)pyrrolidin-3-yl)methyl)piperidin-4-yl)phenyl)amino)-6-(1-methyl-1H-benzo[d]imidazole-4-yl)-5-(methylamino)pyrazine-2-carboxamide
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References
1. Tong J, et al. J Med Chem. 2025 Jul 30. doi: 10.1021/acs.jmedchem.5c00970.
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