JNK-IN-8

Bezeichnung:JNK-IN-8

CAS-Nr1410880-22-6

Englisch Name:JNK-IN-8

CBNumberCB82624190

SummenformelC29H29N7O2

Molgewicht507.59

MOL-Datei1410880-22-6.mol

JNK-IN-8 physikalisch-chemischer Eigenschaften

Dichte	1.283±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	≥25.4 mg/mL in DMSO; insoluble in H2O; ≥9.24 mg/mL in EtOH with gentle warming and ultrasonic
pka	13.34±0.70(Predicted)
Aggregatzustand	powder
Farbe	white to beige

Sicherheit

HS Code

2933599590

Gefahreninformationscode (GHS)

JNK-IN-8 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
JNK-IN-8 has been used as an inhibitor to address the importance of JNK signaling in withaferin A (WFA)-induced apoptosis of myelodysplastic syndromes (MDS)-L cells.
Definition
ChEBI: 3-[[4-(dimethylamino)-1-oxobut-2-enyl]amino]-N-[3-methyl-4-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide is a member of benzamides.
Biologische Aktivität
jnk-in-8 is a specific jnk1/2/3 inhibitor with ic50 value of 4.67, 18.7, 0.98 nm respectively [1].c-jun n-terminal kinase (jnk) 1, 2 and 3 belong to the mitogen-activated protein kinase (mapk) family, which are able to phosphorylate c-jun on the ser63 and ser73 residue.they are responsive for stress stimuli, including cytokines and heat shock, and get involved in t cell differentiation and cell apoptosis process. jnk 1 and 2 are ubiquitous in all cell types but jnk 3 is only found in cells of brain, heart and testes tissues.jnk-in-8 is a jnk1/2/3 inhibitor with high specificity. when jnk-in-8 was profiled with a panel of 400 kinases, it exhibited specific binding to jnk 1/2/3 but not to other kinases. crystallization study also found that jnk-in-8 forms covalent bonds with conserved cysteine residue of jnk 1/2/3, resulting in a conformational change of the activation loop that blocks the substrate binding, thereby inhibiting the activity of jnk 1/2/3 [1].in hela cells and a375 cells, pretreatment of cells with jnk-in-8 resulted in the inhibition of c-jun which is a direct phosphorylation substrate of jnk 1/2/3, confirming the inhibitory action of jnk-in-8 on jnk 1/2/3. in hek293-ilr1 cells following stimulation by anisomycin, the jnk-in-8 was observed to inhibit c-jun but not msk1 and p38, and the inhibition was not reversible by removing jnk-in-8 from culture medium. additionally, jnk-in-8 only exhibited on-pathway inhibition of jnk signaling pathway, which can be monitored by the phosphorylation of c-jun [1].
Biochem/physiol Actions
JNK-IN-8 is a potent, selective and irreversible inhibitor of JNK1/2/3 that inhibits phosphorylation of c-Jun. JNK-IN-8 forms covalent bonds with a conserved cysteine residue.
target
JNK1
Einzelnachweise
[1]. zhang t et al., discovery of potent and selective covalent inhibitors of jnk. chemical biology. 2012, 19(1):140-154.

JNK-IN-8 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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