1. MAPK/ERK Pathway
  2. MAP4K
  3. GNE-1858

GNE-1858 

Cat. No.: HY-135892 Purity: 99.0%
Handling Instructions

GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.

For research use only. We do not sell to patients.

GNE-1858 Chemical Structure

GNE-1858 Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively[1].

In Vitro

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. HPK1 is a negative-feedback regulator of T cell receptor signaling, which dampens T cell proliferation and effector function[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

428.48

Formula

C₂₁H₂₆F₂N₈

SMILES

FC1(CCN(C2=NC(C3CCNC3)=CC(NC4=CC5=C(C=N4)C=NN5C(C)C)=N2)C1)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (46.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3338 mL 11.6692 mL 23.3383 mL
5 mM 0.4668 mL 2.3338 mL 4.6677 mL
10 mM 0.2334 mL 1.1669 mL 2.3338 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2 mg/mL (4.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (4.67 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (4.67 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GNE-1858GNE1858GNE 1858MAP4KMAPK Kinase Kinase Kinasehematopoieticprogenitornegative-feedbackregulatorT-cellreceptorsignalingproliferationInhibitorinhibitorinhibit

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Product Name:
GNE-1858
Cat. No.:
HY-135892
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