Comparison

SP600125 European Partner

Item no. S1460-1000
Manufacturer Selleckchem
CASRN 129-56-6
Amount 1 g
Quantity options 10 mg 1 g 10 g 100 mg 10 mM/1 mL 200 mg 25 mg 50 mg 5 g
Category
Type Inhibitors
Specific against other
Smiles C1=CC=C2C(=C1)C3=NNC4=CC=CC(=C43)C2=O
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Alias Nsc75890
Similar products SP600125
Available
Manufacturer - Targets
FLT3
Storage Conditions
2 years -80 in solvent
Molecular Weight
220, 23
Administration
Administered via intravenous injection or orally
Animal Models
Mouse LPS/TNF model (female CD-1)
Cell lines
HCT116, A2780, and U2OS cells
Concentrations
0–5 uM, dissolved in 0.1% DMSO
Dosages
15 or 30 mg/kg
Formulation
Dissolved in PPCES (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline)
IC50
40 nM, 40 nM, 40 nM, 40 nM, 40 nM, 40 nM
In vitro
SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 uM to 10 uM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-gamma, and TNF-alpha, with IC50 of 5 uM to 12 uM. [1] However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) [2], Mps1 [3], and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA [4]. In a mouse beta cells MIN6, SP600125 (20 uM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. [5] In HCT116 cells, SP600125 (20 uM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1. [6]
In vivo
In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-alpha expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. [1]
Incubation Time
72 hours
Kinase Assay
[4], In Vitro Kinase Assays, The potency of SP600125 towards kinases, including MPS1, JNK, and Aurora kinase A, is determined based on the specific measurement of radioactive phosphotransfer to the substrate. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·alphaKm) and [substrate] (5·Km) concentrations. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 uM NaVO3, 2 mM beta-glycerophosphate, 0.2 mg/mL BSA, 200 uM P38-betatide substrate-peptide (KRQADEEMTGYVATRWYRAE), and 8 uM ATP with 1.5 nM 33P-gamma-ATP. Ten serial 1:3 dilutions (from 30 uM to 1.5 nM) of SP600125 are tested and IC50 determined.
Method
Cells are seeded in 384 well-plates. One day after seeding, the cells are treated with SP600125 for 72 hours and the plates are then processed using a CellTiter-Glo assay. Inhibitory activity is evaluated comparing treated versus control data and IC50 value of proliferation is calculated.
Solubility (25C)
DMSO 44 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information
SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis.
Chemical Name
2H-Dibenzo[cd, g]indazol-6-one

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 1 g
Available: In stock
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