1. MAPK/ERK Pathway
    Apoptosis
  2. MAP3K
    Apoptosis
  3. GS-444217

GS-444217 

Cat. No.: HY-100844 Purity: 99.80%
Handling Instructions

GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.

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

GS-444217 Chemical Structure

GS-444217 Chemical Structure

CAS No. : 1262041-49-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 380 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM[1].

IC50 & Target[1]

ASK1

2.87 nM (IC50)

In Vitro

Treatment with GS-444217 reduces ASK1 phosphorylation and prevents the phosphorylation of MKK3/6, MKK4, p38, and JNK at concentrations of 0.3 μM and above with full suppression of ASK1 activity at 1 μM. GS-444217 (1 μM) reduces ASK1 activity within 5 minutes of addition to the cultures, reaching a maximum level of inhibition by 30 minutes. Removal of GS-444217 from the cultures results in reactivation of ASK1 autophosphorylation within 10 minutes and near-complete recovery 2 hours after drug washout[1].

In Vivo

GS-444217 reduces oxidative stress (OS)-induced ASK1 signaling in kidney and inhibits acute renal tubular injury in rats. GS-444217 (30 mg/kg) inhibits activation of ASK1, p38, and JNK in rat kidney. GS-444217 has an in vivo EC50 of approximately 1.6 μM for inhibiting the ASK1 pathway in rodent kidney[1].

Molecular Weight

411.46

Formula

C₂₃H₂₁N₇O

CAS No.

1262041-49-5

SMILES

O=C(C1=NC=CC(N2C=C(C3CC3)N=C2)=C1)NC4=CC=CC(C5=NN=CN5C6CC6)=C4

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 : 15.5 mg/mL (37.67 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4304 mL 12.1518 mL 24.3037 mL
5 mM 0.4861 mL 2.4304 mL 4.8607 mL
10 mM 0.2430 mL 1.2152 mL 2.4304 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: ≥ 2.5 mg/mL (6.08 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.08 mM); Clear solution

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

GS-444217GS444217GS 444217MAP3KApoptosisMAP kinase kinase kinase, MEKK, MAPKKKInhibitorinhibitorinhibit

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Product Name:
GS-444217
Cat. No.:
HY-100844
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