JNK Inhibitor VIII
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货号：A872802同义名：
TCS JNK 6o;c-Jun N-terminal Kinase Inhibitor VIII
JNK Inhibitor VIII (TCSJNK 6o) is a c-Jun N-terminal kinases (JNK-1, -2, and -3) inhibitor with Ki values of 2 nM, 4 nM, 52 nM, respectively, and has IC50 values of 45 nM and 160 nM for JNK-1 and -2, respectively.
c-Jun N-terminal kinase-1 (JNK-1) is a member of the mitogen activated protein kinase (MAP kinase) family of enzymes responsible for the serine/threonine phosphorylation of intracellular targets. JNK-1 and the other JNK enzymes JNK-2 and JNK-3 are activated in response to cellular stresses and various cytokines, and they participate in the onset of apoptosis. TCS JNK 6o is a pan-JNK inhibitor with Ki values of 2, 4 and 52 nM for JNK-1, JNK-2 and JNK-3, respectively, and has IC50 values of 45 and 160 nM for JNK-1 and JNK-2, respectively. In Sprague-Dawley rats, TCS JNK 6o showed a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism was very rapid with this compound[2]. Moreover, inhibition of primordial follicle activation occurred in the presence of TCS JNK 6o when compared with controls (P < 0.05) after 2 days of culture[3].
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