1. MAPK/ERK Pathway
  2. JNK
  3. AS601245

AS601245 

Cat. No.: HY-11010 Purity: 98.70%
Handling Instructions

AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.

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

AS601245 Chemical Structure

AS601245 Chemical Structure

CAS No. : 345987-15-7

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Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
50 mg USD 810 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
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Description

AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties[1][2].

IC50 & Target[1]

hJNK1

150 nM (IC50)

hJNK2

220 nM (IC50)

hJNK3

70 nM (IC50)

In Vitro

AS601245, an anti-Inflammatory JNK inhibitor, and Clofibrate have a synergistic effect in inducing cell responses and in affecting the gene expression profile in CaCo-2 colon cancer cells [2].

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

In Vivo

AS601245 (40, 60, and 80 mg/kg; i.p.) provides significant protection against the delayed loss of hippocampal CA1 neurons in a gerbil model of transient global ischemia[1].
AS601245 (0.3-10 mg/kg; p.o.) is a potent inhibitor of LPS-induced TNF-α release in mice[1].

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

Animal Model: C3H/HEN mice[1]
Dosage: 0.3, 1, 3, or 10 mg/kg
Administration: P.o.
Result: Decreased the TNF-α release in a dose-dependent manner.
Molecular Weight

372.45

Formula

C₂₀H₁₆N₆S

CAS No.
SMILES

N#CC(C1=CC=NC(NCCC2=CC=CN=C2)=N1)C3=NC4=CC=CC=C4S3

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 : 10 mg/mL (26.85 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6849 mL 13.4246 mL 26.8492 mL
5 mM 0.5370 mL 2.6849 mL 5.3698 mL
10 mM 0.2685 mL 1.3425 mL 2.6849 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: ≥ 1 mg/mL (2.68 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1 mg/mL (2.68 mM); Clear solution

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

AS601245AS 601245AS-601245JNKc-Jun N-terminal kinaseTNF-αreleaseanti-InflammatorycoloncancercellsneuroprotectiveInhibitorinhibitorinhibit

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AS601245
Cat. No.:
HY-11010
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