HPK1-IN-64

HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer[1].

Product Specifications

CAS Number

[3034320-17-4]

UNSPSC

12352005

Target

Interleukin Related; MAP4K

Related Pathways

Immunology/Inflammation; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C1C(C2=C(C=C3C4=CN=C5N4CCC[C@H]5OC)C(C)(C6=CC(N7CCOCC7)=CC=C6N2)C)=C3CN1

Molecular Formula

C29H33N5O3

Molecular Weight

499.60

References & Citations

[1]Xi B, et al. Pocket-based molecule generation with an SE (3) -equivariant language model leads to a potent and selective HPK1 inhibitor with in vivo efficacy[J]. bioRxiv, 2025: 2025.09. 23.678079.