货号：A485028同义名：
JAK3 Inhibitor V; Janus-Associated Kinase 3 Inhibitor V
Potent, selective JAK3 inhibitor
HazMat Fee +
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
The JAK/ATAT signaling pathway involves two protein families, the JAKs and the STATs. The JAK/STAT pathway forms a critical node affecting multiple signaling pathways in both the innate and adaptive immune responses. Janus kinase 2 (JAK2) belongs to the non-receptor tyrosine kinase family. Upon tyrosine receptor phosphorylation, JAKs are activated and, in turn, phosphorylate the tyrosine motifs in the cytoplasmic tail of the receptor, which allows for STAT binding . The JAK protein family consists of four members [JAK1, JAK2, JAK3, and tyrosine kinase 2 (TYK2)], whereas the STAT family consists of seven members (STAT1, STAT2, STAT3, STAT4, STAT5A, STAT5B, and STAT6). ZM39923 is a Janus kinase inhibitor with pIC50 values of 6.8 nM, 5.0 nM, 4.7 nM, and < 5.0 nM for JAK3, EGFR, JAK1 and CDK4 respectively, it can also inhibit human tissue transglutaminase (TGM2) with IC50 of 10 nM[1]. In a vivo study, rats were treated with vehicle, morphine (300 mg/kg), the delta-opioid agonist fentanyl isothiocynate (FIT, 10 mg/kg), or the GSK inhibitor SB-216763 (SB21, 600 mg/kg) 10 min before ischemia. Five minutes before opioid or SB21 treatment, some rats received JAK3 inhibitor ZM-449829 (3 mg/kg). ZM-449829, a more selective inhibitor for JAK3 that also inhibits the EGF receptor was shown not to affect opioid-induced cardioprotection. In a dialysis experiment, it was indicated that chemicals targeted Ca+2 - TGM2. In the absence of Ca+2, there was only 20%- 40% inhibition by ZM39923, vitamin K3, vitamin K2, and Me-3,4-dephostatin, whereas >90% inhibition was observed by ZM449829[1].
作用机制
ZM 449829 binds competitively to the JAK3 ATP-binding site.
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