SP600125 [129-56-6]

Katalog-Nummer HY-12041-50mg

Size : 50mg

Marke : MedChemExpress

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Beschreibung

SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis[1][2][3].

IC50 & Target[1]

JNK1

40 nM (IC50)

JNK2

40 nM (IC50)

JNK3

90 nM (IC50)

Autophagy

 

Cellular Effect
Cell Line Type Value Description References
786-0 IC50
27.1 μM
Compound: SP600125
Antiproliferative activity against human 786-0 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human 786-0 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
A498 IC50
7.03 μM
Compound: SP600125
Antiproliferative activity against human A498 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human A498 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
A549 IC50
14.93 μM
Compound: SP600125
Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
ACHN IC50
6.64 μM
Compound: SP600125
Antiproliferative activity against human ACHN cells measured after 48 hrs by SRB assay
Antiproliferative activity against human ACHN cells measured after 48 hrs by SRB assay
[PMID: 35764033]
BT-549 IC50
30.76 μM
Compound: SP600125
Antiproliferative activity against human BT-549 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human BT-549 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
CAKI-1 IC50
3.56 μM
Compound: SP600125
Antiproliferative activity against human CAKI-1 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human CAKI-1 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
CCRF-CEM IC50
16.03 μM
Compound: SP600125
Antiproliferative activity against human CCRF-CEM cells measured after 48 hrs by SRB assay
Antiproliferative activity against human CCRF-CEM cells measured after 48 hrs by SRB assay
[PMID: 35764033]
COLO 205 IC50
19.54 μM
Compound: SP600125
Antiproliferative activity against human COLO 205 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human COLO 205 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
DU-145 IC50
28.18 μM
Compound: SP600125
Antiproliferative activity against human DU-145 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human DU-145 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
EKVX IC50
20.04 μM
Compound: SP600125
Antiproliferative activity against human EKVX cells measured after 48 hrs by SRB assay
Antiproliferative activity against human EKVX cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HCC 2998 IC50
9.62 μM
Compound: SP600125
Antiproliferative activity against human HCC 2998 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HCC 2998 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HCT-116 IC50
44.57 μM
Compound: SP600125
Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HCT-15 IC50
8.04 μM
Compound: SP600125
Antiproliferative activity against human HCT-15 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HCT-15 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HL-60(TB) IC50
42.07 μM
Compound: SP600125
Antiproliferative activity against human HL-60(TB) cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HL-60(TB) cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HOP-62 IC50
69.34 μM
Compound: SP600125
Antiproliferative activity against human HOP-62 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HOP-62 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HOP-92 IC50
37.58 μM
Compound: SP600125
Antiproliferative activity against human HOP-92 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HOP-92 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
Hs-578T IC50
55.08 μM
Compound: SP600125
Antiproliferative activity against human Hs-578T cells measured after 48 hrs by SRB assay
Antiproliferative activity against human Hs-578T cells measured after 48 hrs by SRB assay
[PMID: 35764033]
HT-29 IC50
25.88 μM
Compound: SP600125
Antiproliferative activity against human HT-29 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human HT-29 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
IGROV-1 IC50
11.35 μM
Compound: SP600125
Antiproliferative activity against human IGROV-1 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human IGROV-1 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
K562 IC50
48.64 μM
Compound: SP600125
Antiproliferative activity against human K562 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human K562 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
KM12 IC50
2.62 μM
Compound: SP600125
Antiproliferative activity against human KM12 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human KM12 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
M14 IC50
> 100 μM
Compound: SP600125
Antiproliferative activity against human M14 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human M14 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
Malme-3M IC50
16.41 μM
Compound: SP600125
Antiproliferative activity against human Malme-3M cells measured after 48 hrs by SRB assay
Antiproliferative activity against human Malme-3M cells measured after 48 hrs by SRB assay
[PMID: 35764033]
MCF7 IC50
48.98 μM
Compound: SP600125
Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
MDA-MB-231 IC50
65.31 μM
Compound: SP600125
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
MDA-MB-435 IC50
12.82 μM
Compound: SP600125
Antiproliferative activity against human MDA-MB-435 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human MDA-MB-435 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
MOLT-4 IC50
20.37 μM
Compound: SP600125
Antiproliferative activity against human MOLT-4 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human MOLT-4 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
MONO-MAC-6 IC50
5.2 μM
Compound: SP600125
Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA
Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA
[PMID: 30347329]
NCI/ADR-RES IC50
22.59 μM
Compound: SP600125
Antiproliferative activity against human NCI-ADR-RES cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-ADR-RES cells measured after 48 hrs by SRB assay
[PMID: 35764033]
NCI-H226 IC50
22.86 μM
Compound: SP600125
Antiproliferative activity against human NCI-H226 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H226 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
NCI-H23 IC50
23.77 μM
Compound: SP600125
Antiproliferative activity against human NCI-H23 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H23 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
NCI-H322M IC50
24.95 μM
Compound: SP600125
Antiproliferative activity against human NCI-H322M cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H322M cells measured after 48 hrs by SRB assay
[PMID: 35764033]
NCI-H460 IC50
9.86 μM
Compound: SP600125
Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
NCI-H522 IC50
12.19 μM
Compound: SP600125
Antiproliferative activity against human NCI-H522 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H522 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
OVCAR-3 IC50
15.31 μM
Compound: SP600125
Antiproliferative activity against human OVCAR-3 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human OVCAR-3 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
OVCAR-4 IC50
31.91 μM
Compound: SP600125
Antiproliferative activity against human OVCAR-4 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human OVCAR-4 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
OVCAR-5 IC50
24.38 μM
Compound: SP600125
Antiproliferative activity against human OVCAR-5 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human OVCAR-5 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
OVCAR-8 IC50
22.03 μM
Compound: SP600125
Antiproliferative activity against human OVCAR-8 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human OVCAR-8 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
PC-3 IC50
23.28 μM
Compound: SP600125
Antiproliferative activity against human PC-3 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human PC-3 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
RPMI-8226 IC50
18.79 μM
Compound: SP600125
Antiproliferative activity against human RPMI-8226 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human RPMI-8226 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
RXF 393 IC50
20.75 μM
Compound: SP600125
Antiproliferative activity against human RXF 393 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human RXF 393 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SF-268 IC50
18.45 μM
Compound: SP600125
Antiproliferative activity against human SF-268 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SF-268 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SF-295 IC50
22.49 μM
Compound: SP600125
Antiproliferative activity against human SF-295 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SF-295 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SF-539 IC50
32.21 μM
Compound: SP600125
Antiproliferative activity against human SF-539 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SF-539 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SK-MEL-2 IC50
28.97 μM
Compound: SP600125
Antiproliferative activity against human SK-MEL-2 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SK-MEL-2 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SK-MEL-28 IC50
37.5 μM
Compound: SP600125
Antiproliferative activity against human SK-MEL-28 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SK-MEL-28 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SK-MEL-5 IC50
14.62 μM
Compound: SP600125
Antiproliferative activity against human SK-MEL-5 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SK-MEL-5 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SK-OV-3 IC50
20.99 μM
Compound: SP600125
Antiproliferative activity against human SK-OV-3 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SK-OV-3 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SN12C IC50
14.76 μM
Compound: SP600125
Antiproliferative activity against human SN12C cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SN12C cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SNB-19 IC50
50 μM
Compound: SP600125
Antiproliferative activity against human SNB-19 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SNB-19 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SNB-75 IC50
16.9 μM
Compound: SP600125
Antiproliferative activity against human SNB-75 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SNB-75 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SR IC50
13.09 μM
Compound: SP600125
Antiproliferative activity against human SR cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SR cells measured after 48 hrs by SRB assay
[PMID: 35764033]
SW-620 IC50
10.91 μM
Compound: SP600125
Antiproliferative activity against human SW-620 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human SW-620 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
T47D IC50
> 100 μM
Compound: SP600125
Antiproliferative activity against human T47D cells measured after 48 hrs by SRB assay
Antiproliferative activity against human T47D cells measured after 48 hrs by SRB assay
[PMID: 35764033]
TK-10 IC50
5.93 μM
Compound: SP600125
Antiproliferative activity against human TK-10 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human TK-10 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
U-251 IC50
23.07 μM
Compound: SP600125
Antiproliferative activity against human U-251 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human U-251 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
UACC-257 IC50
29.51 μM
Compound: SP600125
Antiproliferative activity against human UACC-257 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human UACC-257 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
UACC-62 IC50
14.55 μM
Compound: SP600125
Antiproliferative activity against human UACC-62 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human UACC-62 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
UO-31 IC50
10.54 μM
Compound: SP600125
Antiproliferative activity against human UO-31 cells measured after 48 hrs by SRB assay
Antiproliferative activity against human UO-31 cells measured after 48 hrs by SRB assay
[PMID: 35764033]
WI-38 IC50
> 20 μM
Compound: SP600125
Antiproliferative activity against human WI-38 cells measured by MTT assay
Antiproliferative activity against human WI-38 cells measured by MTT assay
[PMID: 35764033]
In Vitro

SP600125 is an ATP-competitive inhibitor of JNK2 with a Ki value of 0.19±0.06 μM. SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM in Jurkat T cells. 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-γ, and TNF-α, with IC50 of 5 μM to 12 μM[1].
In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation[2].
In HCT116 cells, SP600125 (20 μM) 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[3].

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

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 12.5 mg/mL (56.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5407 mL 22.7035 mL 45.4071 mL
5 mM 0.9081 mL 4.5407 mL 9.0814 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.08 mg/mL (9.44 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  Corn Oil

    Solubility: 1 mg/mL (4.54 mM); Suspended solution; Need ultrasonic and warming and heat to 80°C

  • Protocol 2

    Add each solvent one by one:  1% CMC-Na/saline water

    Solubility: 3.33 mg/mL (15.12 mM); Suspended solution; Need ultrasonic

Reinheit & Dokumentation
Verweise

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