1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
    MAPK/ERK Pathway
  2. ROCK
    Ribosomal S6 Kinase (RSK)
  3. GSK-25

GSK-25 

Cat. No.: HY-14362 Purity: 99.68%
Handling Instructions

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).

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

GSK-25 Chemical Structure

GSK-25 Chemical Structure

CAS No. : 874119-56-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 105 In-stock
Estimated Time of Arrival: December 31
10 mg USD 178 In-stock
Estimated Time of Arrival: December 31
25 mg USD 255 In-stock
Estimated Time of Arrival: December 31
50 mg USD 390 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively)[1].

IC50 & Target[1]

ROCK1

7 nM (IC50)

RSK1

398 nM (IC50)

p70S6K

1000 nM (IC50)

In Vivo

GSK-25 (Rat aorta IC50=256 nM) is profiled in a spontaneously hypertensive rat (SHR) model of hypertension. At 30 mg/kg (p.o.), GSK-25 induces a 25 mmHg (t=3 hours) drop in blood pressure[1].
GSK-25 has promising oral bioavailability (49% in male Sprague-Dawley rats and 19% in monkey), good half-life (1.8 hours in rat and 2.2 hours in monkey)[1].

Molecular Weight

513.33

Formula

C₂₄H₁₆Cl₂F₂N₆O

CAS No.

874119-56-9

SMILES

ClC1=CC(C2=NC(C3=C(F)C=C(Cl)C=C3)C(C(NC4=C(F)C=C(NN=C5)C5=C4)=O)=C(C)N2)=CC=N1

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 : 100 mg/mL (194.81 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9481 mL 9.7403 mL 19.4806 mL
5 mM 0.3896 mL 1.9481 mL 3.8961 mL
10 mM 0.1948 mL 0.9740 mL 1.9481 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: ≥ 2.75 mg/mL (5.36 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.75 mg/mL (5.36 mM); Clear solution

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

GSK-25GSK25GSK 25ROCKRibosomal S6 Kinase (RSK)Rho-associated protein kinaseRho-associated kinaseRho-kinaseROKS6Kselectiveorallybioavailablep70S6KP450bloodpressureInhibitorinhibitorinhibit

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Product name:
GSK-25
Cat. No.:
HY-14362
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