GNE-1858

SKU: orb1309623

Description

GNE-1858 is a potent and selective ATP-competitive inhibitor of hematopoietic progenitor kinase 1 (HPK1), demonstrating low nanomolar IC50 values against the wild-type and active mimetic mutant forms. This small molecule is a valuable research tool for investigating HPK1's role in immune cell signaling and T-cell function in both cellular and animal models of oncology and immunotherapy.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2680616-96-8
• MW: 428.48
• Purity: 98.70% (May vary between batches)
• Formula: C₂₁H₂₆F₂N₈
• SMILES: CC(C)n1ncc2cnc(Nc3cc(nc(n3)N3CCC(F)(F)C3)C3CCNC3)cc12
• Target: MAPK
• Solubility: DMSO:4.29 mg/mL (10.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.33 mM)

Bioactivity

• Target IC50:
  HPK1: 1.9 nM
• In Vitro:
  HPK1 is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function.Hematopoietic progenitor kinase-1 (HPK1), a serine/threonine Ste20-related protein kinase whose expression is restricted to the hematopoietic compartment (e.g., T cells, B cells, and dendritic cells), is one such kinase.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GNE 1858, GNE1858, GNE-1858, Inhibitor, hematopoietic, MAP4K, MAPK Kinase Kinase Kinase, HPK1, inhibit, negative-feedback, regulator, proliferation, progenitor, signaling, receptor, T-cell

Compound Identifiers

PubChem CID

146026186