PROTAC HPK1 Degrader-1

PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with DC50 value of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits phosphorylation of the SLP76 protein with IC50 value of 496.1 nM. PROTAC HPK1 Degrader-1 is a bona fide HPK1-PROTAC degrader, which provided a potential tool for further HPK1 investigation in TCR signaling[1].

Product Specifications

CAS Number

[3034182-97-0]

UNSPSC

12352005

Target

MAP4K; PROTACs

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-hpk1-degrader-1.html

Purity

99.70

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCOCCC(N4CCN(C5=CC=C(C6=CN=C(NC=C7C8=CC=C(OC)C(OC)=C8)C7=C6)C=C5)CC4)=O)=O

Molecular Formula

C43H43N7O8

Molecular Weight

785.84

References & Citations

[1]Zeng S, et al. Discovery of highly efficient CRBN-recruiting HPK1-PROTAC as a potential chemical tool for investigation of scaffolding roles in TCR signaling. Bioorg Chem. 2024 Feb;143:107016.