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HPK inhibitor compound 1

Chemical Structure : HPK inhibitor compound 1

CAS No.: 1214561-09-7

HPK inhibitor compound 1

Catalog No.: PC-38665Not For Human Use, Lab Use Only.

HPK inhibitor compound 1 is an allosteric, inactive conformation-selective HPK1 inhibitor, binds to unphosphorylated HPK1 and >24-fold more potently than active HPK1.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

HPK inhibitor compound 1 is an allosteric, inactive conformation-selective HPK1 inhibitor, binds to unphosphorylated HPK1 and >24-fold more potently than active HPK1.
HPK inhibitor compound 1 is not competitive with ATP, and is highly selective against kinases critical for T cell signaling.
HPK inhibitor compound 1 does not bind to the isolated HPK1 kinase domain alone but requires other domains, attenuates kinase autophosphorylation by binding to a pocket consisting of residues within and outside of the kinase domain.

Physicochemical Properties

M.Wt 412.443
Formula C19H17FN6O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(3,7-dimethyl-5-oxo-5,8-dihydro-[1,2,4]triazolo[4,3-a]pyrimidin-6-yl)-N-(5-(3-fluorobenzyl)thiazol-2-yl)acetamide

References

1. Weixue Wang, et al. Biochemistry. 2021 Oct 19;60(41):3114-3124.

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