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SP600125

Cat. No. M2076
SP600125 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 45  USD45 In stock
10mg USD 40  USD40 In stock
25mg USD 50  USD50 In stock
50mg USD 60  USD60 In stock
100mg USD 90  USD90 In stock
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Quality Control
Biological Activity

SP600125 is a selective, ATP-competitive JNK inhibitor. SP600125 reversibly inhibits JNK1, 2 and 3 (IC50 = 40 - 90 nM) with negligible activity at ERK2, p38β and a range of enzymes (IC50 > 10 μM). SP600125 potently decreased renal epithelial tubular cell apoptosis induced by renal ischemia/reperfusion via suppression of the extrinsic pathway. In cells, SP600125 dose dependently inhibited the phosphorylation of c-Jun, the expression of inflammatory genes COX-2, IL-2, IFN-gamma, TNF-alpha, and prevented the activation and differentiation of primary human CD4 cell cultures. In mice, SP600125 (15 mg/kg or 30 mg/kg) blocked lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4(+) CD8(+) thymocytes.

Product Citations
Customer Product Validations & Biological Datas
Source Molecules and Cells (2017). Figure 5. SP600125 (Abmole Bioscience, USA)
Method Wound healing assay
Cell Lines EGI-1 cells
Concentrations 10 µM
Incubation Time
Results The JNK inhibitor significantly decreased cell migration and invasion, as well as JNK phosphorylation (Figs. 5A-5C), but not cell proliferation (Fig. 5D).
Protocol
Cell Experiment
Cell lines A549 cells
Preparation method Cell viability assay.
Cell viability was evaluated using the Cell Counting kit (CCK)-8 assay (AbMole). In brief, the cells were seeded into 96-well plates at a density of 3×103 cells/well and left to adhere overnight. The cells were then incubated with or without 0–40 nM SP600125. Then, 100 μl CCK-8 was added and incubated in the dark at 37°C for 3 h. The absorbance was determined using the MRX II microplate reader (Dynex, Chantilly, VA, USA) at a wavelength of 450 nm.
Concentrations 0~40 nM
Incubation time 24 h
Animal Experiment
Animal models Female CD-1 mice
Formulation 30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline
Dosages 0, 12, 24, and 36 h, 15 mg/kg
Administration s.c.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 220.23
Formula C14H8N2O
CAS Number 129-56-6
Purity 99.73%
Solubility DMSO 16 mg/mL
Storage at -20°C
References

[1] Zheng Y, et al. Exp Ther Med. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation of claudin-4.

[2] Wang Y, et al. Life Sci. SP600125, a selective JNK inhibitor, protects ischemic renal injury via suppressing the extrinsic pathways of apoptosis.

[3] Bennett BL, et al. Proc Natl Acad Sci U S A. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase.

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Keywords: SP600125 supplier, JNK, inhibitors

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